Zevra Therapeutics, Inc.

United States of America

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        Patent 86
        Trademark 13
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        United States 84
        Canada 11
        World 4
Date
2025 June 1
2025 (YTD) 3
2024 2
2023 15
2022 5
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IPC Class
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine 31
A61K 9/00 - Medicinal preparations characterised by special physical form 30
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound 27
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca 23
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates 21
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NICE Class
42 - Scientific, technological and industrial services, research and design 8
05 - Pharmaceutical, veterinary and sanitary products 6
Status
Pending 19
Registered / In Force 80

1.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number 19053080
Status Pending
Filing Date 2025-02-13
First Publication Date 2025-06-12
Owner Zevra Therapeutics, Inc. (USA)
Inventor
  • Bera, Sanjib
  • Guenther, Sven
  • Smith, Adam
  • Mickle, Travis

Abstract

Disclosed are one or more compounds comprising chemically modified gamma-hydroxybutyrate (GHB), 2-hydroxytetrahydrofuran, and/or 1,4-butanediol, and salts of such compounds (GHB delivering compounds and salts thereof). Also disclosed are compositions comprising at least one GHB delivering compound, or a salt thereof, methods of making such compounds, and methods of using such GHB delivering compounds and compositions. Methods of treatment using the compounds are also disclosed.

IPC Classes  ?

  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 25/20 - HypnoticsSedatives
  • C07C 69/14 - Acetic acid esters of monohydroxylic compounds
  • C07C 69/88 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with esterified carboxyl groups
  • C07C 69/96 - Esters of carbonic or haloformic acids
  • C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
  • C07C 271/64 - Y being a hydrogen or a carbon atom, e.g. benzoylcarbamates
  • C07C 271/66 - Y being a hetero atom
  • C07C 301/00 - Esters of sulfurous acid
  • C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
  • C07C 307/06 - Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
  • C07C 333/10 - Monothiocarbamic acidsDerivatives thereof having nitrogen atoms of thiocarbamic groups being part of any of the groups X being a hetero atom, Y being any atom, e.g., N-acyl-thiocarbamates
  • C07D 307/20 - Oxygen atoms
  • C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07F 9/09 - Esters of phosphoric acids
  • C07F 9/24 - Esteramides

2.

APADAZ

      
Serial Number 99037684
Status Pending
Filing Date 2025-02-11
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of pain

3.

LEVORPHANOL PRODRUGS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number 18787677
Status Pending
Filing Date 2024-07-29
First Publication Date 2025-01-30
Owner ZEVRA THERAPEUTICS INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides compositions of one or more of oxoacids, amino acids, polyethylene glycols, and/or vitamin compounds chemically conjugated to levorphanol ((-)-17-methylmorphinan-3-ol) to form novel prodrugs and compositions of levorphanol.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound

4.

DEXTRORPHAN PRODRUGS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number 18655883
Status Pending
Filing Date 2024-05-06
First Publication Date 2024-09-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides compositions of one or more of oxoacids, polyethylene glycols, and vitamin compounds chemically conjugated to dextrorphan, (+)-17-methylmorphinan-3-ol), to form novel prodrugs and compositions of levorphanol.

IPC Classes  ?

  • C07D 221/28 - Morphinans
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound

5.

D-AMPHETAMINE COMPOUNDS, COMPOSITIONS, AND PROCESSES FOR MAKING AND USING THE SAME

      
Application Number 18432949
Status Pending
Filing Date 2024-02-05
First Publication Date 2024-06-20
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Mickle, Travis

Abstract

Discloses are d-amphetamine compounds and compositions comprising at least on organic acid covalently bound to d-amphetamine, having the structure of Formula I, a salt thereof, a derivative thereof, or a combination thereof. Methods of making and using the same are also disclosed.

IPC Classes  ?

  • C07D 213/79 - AcidsEsters
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • C07D 213/80 - AcidsEsters in position 3
  • C07D 213/81 - AmidesImides
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • A61K 9/02 - SuppositoriesBougiesBases for suppositories or bougies

6.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number 18303200
Status Pending
Filing Date 2023-04-19
First Publication Date 2023-11-30
Owner Zevra Therapeutics, Inc. (USA)
Inventor
  • Bera, Sanjib
  • Dana, Dibyendu
  • Guenther, Sven
  • Smith, Adam
  • Mickle, Travis

Abstract

Disclosed are one or more compounds comprising chemically modified gamma-hydroxybutyrate (GHB), 2-hydroxytetrahydrofuran, and/or 1,4-butanediol, and salts of such compounds (GHB delivering compounds and salts thereof). Also disclosed are compositions comprising at least one GHB delivering compound, or a salt thereof, methods of making such compounds, and methods of using such GHB delivering compounds and compositions. Methods of treatment using the compounds are also disclosed.

IPC Classes  ?

  • C07C 307/06 - Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
  • C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
  • C07C 333/10 - Monothiocarbamic acidsDerivatives thereof having nitrogen atoms of thiocarbamic groups being part of any of the groups X being a hetero atom, Y being any atom, e.g., N-acyl-thiocarbamates
  • C07F 9/24 - Esteramides

7.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number 18303220
Status Pending
Filing Date 2023-04-19
First Publication Date 2023-11-30
Owner Zevra Therapeutics, Inc. (USA)
Inventor
  • Bera, Sanjib
  • Dana, Dibyendu
  • Guenther, Sven
  • Smith, Adam
  • Mickle, Travis

Abstract

Disclosed are one or more compounds comprising chemically modified gamma-hydroxybutyrate (GHB), 2-hydroxytetrahydrofuran, and/or 1,4-butanediol, and salts of such compounds (GHB delivering compounds and salts thereof). Also disclosed are compositions comprising at least one GHB delivering compound, or a salt thereof, methods of making such compounds, and methods of using such GHB delivering compounds and compositions. Methods of treatment using the compounds are also disclosed.

IPC Classes  ?

  • C07D 307/58 - One oxygen atom, e.g. butenolide
  • C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links

8.

Gamma-hydroxybutyrate delivering compounds and processes for making and using them

      
Application Number 18303226
Grant Number 12251445
Status In Force
Filing Date 2023-04-19
First Publication Date 2023-11-30
Grant Date 2025-03-18
Owner Zevra Therapeutics, Inc. (USA)
Inventor
  • Bera, Sanjib
  • Guenther, Sven
  • Smith, Adam
  • Mickle, Travis

Abstract

Disclosed are one or more compounds comprising chemically modified gamma-hydroxybutyrate (GHB), 2-hydroxytetrahydrofuran, and/or 1,4-butanediol, and salts of such compounds (GHB delivering compounds and salts thereof). Also disclosed are compositions comprising at least one GHB delivering compound, or a salt thereof, methods of making such compounds, and methods of using such GHB delivering compounds and compositions. Methods of treatment using the compounds are also disclosed.

IPC Classes  ?

  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 25/20 - HypnoticsSedatives
  • C07C 69/14 - Acetic acid esters of monohydroxylic compounds
  • C07C 69/88 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with esterified carboxyl groups
  • C07C 69/96 - Esters of carbonic or haloformic acids
  • C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
  • C07C 271/64 - Y being a hydrogen or a carbon atom, e.g. benzoylcarbamates
  • C07C 271/66 - Y being a hetero atom
  • C07C 301/00 - Esters of sulfurous acid
  • C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
  • C07C 307/06 - Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
  • C07C 333/10 - Monothiocarbamic acidsDerivatives thereof having nitrogen atoms of thiocarbamic groups being part of any of the groups X being a hetero atom, Y being any atom, e.g., N-acyl-thiocarbamates
  • C07D 307/20 - Oxygen atoms
  • C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07F 9/09 - Esters of phosphoric acids
  • C07F 9/24 - Esteramides
  • A61K 9/00 - Medicinal preparations characterised by special physical form

9.

KETAMINE COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number 18355983
Status Pending
Filing Date 2023-07-20
First Publication Date 2023-11-09
Owner Zevra Therapeutics, Inc. (USA)
Inventor
  • Chi, Guochen
  • Guenther, Sven
  • Mickle, Travis
  • Smith, Adam

Abstract

Disclosed are compounds comprising ketamine (2-(2-chlorophenyl)-2-(methylamino)-cyclohexanone) chemically conjugated to one or more oxoacids, amino acids, polyethylene glycols (PEG or PEO), peptides, phosphates, and/or vitamin compounds, and salts of such compounds. Also disclosed are compositions comprising at least one ketamine compound, or a salt thereof, methods of making such compounds, and methods of using such ketamine compounds and compositions.

IPC Classes  ?

  • A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds

10.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Document Number 03249689
Status Pending
Filing Date 2023-04-19
Open to Public Date 2023-10-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Bera, Sanjib
  • Dana, Dibyendu
  • Guenther, Sven
  • Smith, Adam
  • Mickle, Travis

IPC Classes  ?

  • A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
  • A61P 25/20 - HypnoticsSedatives
  • C07C 69/675 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids of saturated hydroxy-carboxylic acids
  • C07C 69/88 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with esterified carboxyl groups
  • C07C 69/96 - Esters of carbonic or haloformic acids
  • C07C 235/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
  • C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
  • C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 307/20 - Oxygen atoms
  • C07F 9/09 - Esters of phosphoric acids
  • C07K 5/06 - Dipeptides

11.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Document Number 03255515
Status Pending
Filing Date 2023-04-19
Open to Public Date 2023-10-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Smith, Adam
  • Guenther, Sven
  • Mickle, Travis
  • Bera, Sanjib

IPC Classes  ?

  • A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
  • A61P 25/20 - HypnoticsSedatives
  • C07D 307/20 - Oxygen atoms
  • C07D 307/30 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

12.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number US2023019101
Publication Number 2023/205237
Status In Force
Filing Date 2023-04-19
Publication Date 2023-10-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Bera, Sanjib
  • Dana, Dibyendu
  • Guenther, Sven
  • Smith, Adam
  • Mickle, Travis

Abstract

Disclosed are one or more compounds comprising chemically modified gamma-hydroxybutyrate (GHB), 2-hydroxytetrahydrofuran, and/or 1,4-butanediol, and salts of such compounds (GHB delivering compounds and salts thereof). Also disclosed are compositions comprising at least one GHB delivering compound, or a salt thereof, methods of making such compounds, and methods of using such GHB delivering compounds and compositions. Methods of treatment using the compounds are also disclosed.

IPC Classes  ?

  • C07C 69/675 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids of saturated hydroxy-carboxylic acids
  • C07C 271/64 - Y being a hydrogen or a carbon atom, e.g. benzoylcarbamates
  • C07C 271/66 - Y being a hetero atom
  • C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
  • C07C 307/06 - Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
  • C07C 311/53 - X and Y not being nitrogen atoms, e.g. N-sulfonylcarbamic acid
  • C07C 333/10 - Monothiocarbamic acidsDerivatives thereof having nitrogen atoms of thiocarbamic groups being part of any of the groups X being a hetero atom, Y being any atom, e.g., N-acyl-thiocarbamates
  • C07F 9/24 - Esteramides
  • C07K 5/06 - Dipeptides
  • A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
  • A61P 25/20 - HypnoticsSedatives

13.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number US2023019112
Publication Number 2023/205245
Status In Force
Filing Date 2023-04-19
Publication Date 2023-10-26
Owner
  • ZEVRA THERAPEUTICS, INC. (USA)
  • GUENTHER, Sven (USA)
Inventor
  • Bera, Sanjib
  • Smith, Adam
  • Mickle, Travis

Abstract

Disclosed are one or more compounds of formula (V) comprising chemically modified gamma-hydroxybutyrate (GHB), 2-hydroxy tetra hydrofuran, and/or 1,4-butanediol, and salts of such compounds (GHB delivering compounds and salts thereof). Also disclosed are compositions comprising at least one GHB delivering compound, or a salt thereof, methods of making such compounds, and methods of using such GHB delivering compounds and compositions. Methods of treatment using the compounds are also disclosed.

IPC Classes  ?

  • A61P 25/20 - HypnoticsSedatives
  • C07D 307/20 - Oxygen atoms
  • C07D 307/30 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
  • A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide

14.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Document Number 03249691
Status Pending
Filing Date 2023-04-19
Open to Public Date 2023-10-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib
  • Dana, Dibyendu
  • Smith, Adam

IPC Classes  ?

  • A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
  • A61P 25/20 - HypnoticsSedatives
  • C07C 69/675 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids of saturated hydroxy-carboxylic acids
  • C07C 271/64 - Y being a hydrogen or a carbon atom, e.g. benzoylcarbamates
  • C07C 271/66 - Y being a hetero atom
  • C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
  • C07C 307/06 - Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
  • C07C 311/53 - X and Y not being nitrogen atoms, e.g. N-sulfonylcarbamic acid
  • C07C 333/10 - Monothiocarbamic acidsDerivatives thereof having nitrogen atoms of thiocarbamic groups being part of any of the groups X being a hetero atom, Y being any atom, e.g., N-acyl-thiocarbamates
  • C07F 9/24 - Esteramides
  • C07K 5/06 - Dipeptides

15.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Document Number 03249693
Status Pending
Filing Date 2023-04-19
Open to Public Date 2023-10-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Smith, Adam
  • Dana, Dibyendu
  • Bera, Sanjib
  • Mickle, Travis

IPC Classes  ?

  • A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
  • A61P 25/20 - HypnoticsSedatives
  • C07D 307/20 - Oxygen atoms

16.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number US2023019097
Publication Number 2023/205233
Status In Force
Filing Date 2023-04-19
Publication Date 2023-10-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Bera, Sanjib
  • Dana, Dibyendu
  • Guenther, Sven
  • Smith, Adam
  • Mickle, Travis

Abstract

Disclosed are compounds comprising chemically modified gamma-hydroxybutyrate (GHB) having the structure of Formula I, and salts of such compounds (GHB delivering compounds and salts thereof). Also disclosed are compositions comprising at least one GHB delivering compound, or a salt thereof, methods of making such compounds, and methods of using such GHB delivering compounds and compositions. Methods of treatment are also disclosed.

IPC Classes  ?

  • C07C 69/675 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids of saturated hydroxy-carboxylic acids
  • C07C 69/88 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with esterified carboxyl groups
  • C07C 69/96 - Esters of carbonic or haloformic acids
  • C07C 235/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
  • C07C 301/00 - Esters of sulfurous acid
  • C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
  • C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 307/20 - Oxygen atoms
  • C07F 9/09 - Esters of phosphoric acids
  • C07K 5/06 - Dipeptides
  • A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
  • A61P 25/20 - HypnoticsSedatives

17.

GAMMA-HYDROXYBUTYRATE DELIVERING COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number US2023019107
Publication Number 2023/205241
Status In Force
Filing Date 2023-04-19
Publication Date 2023-10-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Bera, Sanjib
  • Dana, Dibyendu
  • Guenther, Sven
  • Smith, Adam
  • Mickle, Travis

Abstract

Disclosed are one or more compounds III comprising chemically modified gamma-hydroxybutyrate (GHB), 2-hydroxytetrahydrofuran, and/or 1,4-butanediol, and salts of such compounds (GHB delivering compounds and salts thereof). Also disclosed are compositions comprising at least one GHB delivering compound, or a salt thereof, methods of making such compounds, and methods of using such GHB delivering compounds and compositions. Methods of treatment using the compounds are also disclosed formula (III).

IPC Classes  ?

  • A61P 25/20 - HypnoticsSedatives
  • C07D 307/20 - Oxygen atoms
  • A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide

18.

COMPOSITIONS COMPRISING METHYLPHENIDATE-PRODRUGS, PROCESSES OF MAKING AND USING THE SAME

      
Application Number 17798491
Status Pending
Filing Date 2021-02-23
First Publication Date 2023-04-20
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Mickle, Travis

Abstract

The present technology is directed serdexmethylphenidate compounds and methods for synthesizing a compound having the formula

IPC Classes  ?

  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

19.

ZEVRA THERAPEUTICS

      
Serial Number 97772957
Status Registered
Filing Date 2023-01-30
Registration Date 2024-09-17
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 42 - Scientific, technological and industrial services, research and design

Goods & Services

Drug discovery services; Medical research; Research and development in the field of drug discovery

20.

ZEVRA THERAPEUTICS

      
Serial Number 97772964
Status Registered
Filing Date 2023-01-30
Registration Date 2024-09-17
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 42 - Scientific, technological and industrial services, research and design

Goods & Services

Drug discovery services; Medical research; Research and development in the field of drug discovery

21.

ZEVRA

      
Serial Number 97683618
Status Registered
Filing Date 2022-11-18
Registration Date 2024-09-17
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 42 - Scientific, technological and industrial services, research and design

Goods & Services

Drug discovery services; Medical research; Research and development in the field of drug discovery

22.

Ketamine compounds and processes for making and using them

      
Application Number 17723189
Grant Number 11753378
Status In Force
Filing Date 2022-04-18
First Publication Date 2022-11-03
Grant Date 2023-09-12
Owner Zevra Therapeutics, Inc. (USA)
Inventor
  • Chi, Guochen
  • Guenther, Sven
  • Mickle, Travis
  • Smith, Adam

Abstract

Disclosed are compounds comprising ketamine (2-(2-chlorophenyl)-2-(methylamino)-cyclohexanone) chemically conjugated to one or more oxoacids, amino acids, polyethylene glycols (PEG or PEO), peptides, phosphates, and/or vitamin compounds, and salts of such compounds. Also disclosed are compositions comprising at least one ketamine compound, or a salt thereof, methods of making such compounds, and methods of using such ketamine compounds and compositions.

IPC Classes  ?

  • C07D 213/79 - AcidsEsters
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07F 9/10 - Phosphatides, e.g. lecithin
  • C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
  • C07D 213/80 - AcidsEsters in position 3

23.

Levorphanol prodrugs and processes for making and using them

      
Application Number 17550328
Grant Number 12076316
Status In Force
Filing Date 2021-12-14
First Publication Date 2022-03-31
Grant Date 2024-09-03
Owner ZEVRA THERAPEUTICS INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides compositions of one or more of oxoacids, amino acids, polyethylene glycols, and/or vitamin compounds chemically conjugated to levorphanol ((−)-17-methylmorphinan-3-ol) to form novel prodrugs and compositions of levorphanol.

IPC Classes  ?

  • C07D 221/28 - Morphinans
  • A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

24.

Dextrorphan prodrugs and processes for making and using them

      
Application Number 17537291
Grant Number 12012384
Status In Force
Filing Date 2021-11-29
First Publication Date 2022-03-24
Grant Date 2024-06-18
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides compositions of one or more of oxoacids, polyethylene glycols, and/or vitamin compounds chemically conjugated to dextrorphan, (+)-17-methylmorphinan-3-ol), to form novel prodrugs and compositions of dextrorphan.

IPC Classes  ?

  • C07D 221/28 - Morphinans
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound

25.

D-amphetamine compounds, compositions, and processes for making and using the same

      
Application Number 17500680
Grant Number 12091386
Status In Force
Filing Date 2021-10-13
First Publication Date 2022-03-03
Grant Date 2024-09-17
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Mickle, Travis

Abstract

Disclosed are d-amphetamine compounds and compositions comprising at least one organic acid covalently bound to d-amphetamine, having the structure of a salt thereof, a derivative thereof, or a combination thereof. Methods of making and using the same are also disclosed.

IPC Classes  ?

  • C07D 213/56 - Amides
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • C07D 213/79 - AcidsEsters
  • C07D 213/80 - AcidsEsters in position 3
  • C07D 213/81 - AmidesImides
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • A61K 9/02 - SuppositoriesBougiesBases for suppositories or bougies

26.

COMPOSITIONS COMPRISING METHYLPHENIDATE-PRODRUGS, PROCESSES OF MAKING AND USING THE SAME

      
Document Number 03172050
Status Pending
Filing Date 2021-02-23
Open to Public Date 2021-09-02
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Mickle, Travis

Abstract

The invention pertains to a method for manufacture of a serdexmethylphenidate chloride compound having formula I:

IPC Classes  ?

  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61P 25/26 - Psychostimulants, e.g. nicotine, cocaine
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

27.

D-AMPHETAMINE COMPOUNDS, COMPOSITIONS, AND PROCESSES FOR MAKING AND USING THE SAME

      
Document Number 03158404
Status Pending
Filing Date 2020-02-21
Open to Public Date 2021-05-06
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Mickle, Travis

Abstract

The invention pertains to compounds of formula I:

IPC Classes  ?

  • A61K 31/4425 - Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 38/05 - Dipeptides
  • C07D 213/79 - AcidsEsters
  • C07D 213/81 - AmidesImides
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

28.

D-AMPHETAMINE COMPOUNDS, COMPOSITIONS, AND PROCESSES FOR MAKING AND USING THE SAME

      
Document Number 03158405
Status Pending
Filing Date 2020-02-21
Open to Public Date 2021-05-06
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Mickle, Travis

Abstract

The present invention relates to compounds, compositions and kits comprising the compound, methods of manufacture therefor, and uses thereof to treat a patient having a disease, disorder or condition mediated by controlling, preventing, limiting, or inhibiting neurotransmitter uptake. More particularly, the present invention relates to a d-amphetamine compound in which an embodiment of the compound has the structure of or a pharmaceutically acceptable salt thereof, in which X is selected from the group consisting of esters, carboxylic acids, amino acids, amino acid residues, and amides, and Y is selected from the group consisting of hydrogen, alkenyl, alkoxy, alkyl, alkynyl, aryl, alkylaryl, cycloalkenyl, cycloalkyl, cycloalkynyl, heteroalkyl, heteroaryl, and heterocycle.

IPC Classes  ?

  • A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K 31/4425 - Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61P 25/00 - Drugs for disorders of the nervous system
  • C07D 213/79 - AcidsEsters
  • C07D 213/81 - AmidesImides

29.

LEVORPHANOL PRODRUGS AND PROCESSES FOR MAKING AND USING THEM

      
Application Number 16604626
Status Pending
Filing Date 2018-04-12
First Publication Date 2021-01-07
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides compositions of one or more of oxoacids, polyethylene glycols, and vitamin compounds chemically conjugated to levorphanol ((−)-17-methylmorphinan-3-ol) to form novel prodrugs and compositions of levorphanol.

IPC Classes  ?

  • C07D 215/06 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom

30.

Levorphanol prodrugs and processes for making and using them

      
Application Number 16604710
Grant Number 11234975
Status In Force
Filing Date 2018-04-12
First Publication Date 2020-12-17
Grant Date 2022-02-01
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides compositions of one or more of oxoacids, amino acids, polyethylene glycols, and/or vitamin compounds chemically conjugated to levorphanol ((−)-17-methylmorphinan-3-ol) to form novel prodrugs and compositions of levorphanol.

IPC Classes  ?

  • C07D 221/28 - Morphinans
  • A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

31.

Dextrorphan prodrugs and processes for making and using them

      
Application Number 16604755
Grant Number 11214544
Status In Force
Filing Date 2018-04-12
First Publication Date 2020-12-17
Grant Date 2022-01-04
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides compositions of one or more of oxoacids, polyethylene glycols, and/or vitamin compounds chemically conjugated to dextrorphan, (+)-17-methylmorphinan-3-ol), to form novel prodrugs and compositions of dextrorphan.

IPC Classes  ?

  • C07D 221/28 - Morphinans
  • A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound

32.

Compositions comprising methylphenidate-prodrugs, processes of making and using the same

      
Application Number 16793923
Grant Number 10858341
Status In Force
Filing Date 2020-02-18
First Publication Date 2020-06-11
Grant Date 2020-12-08
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen

Abstract

The present technology is directed to compositions comprising d-threo-methylphenidate conjugates and unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate

33.

Compositions comprising methylphenidate-prodrugs, processes of making and using the same

      
Application Number 16794170
Grant Number 10954213
Status In Force
Filing Date 2020-02-18
First Publication Date 2020-06-11
Grant Date 2021-03-23
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen

Abstract

The present technology is directed to compositions comprising d-threo-methylphenidate conjugates and unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

34.

D-amphetamine compounds, compositions, and processes for making and using the same

      
Application Number 16667804
Grant Number 11136295
Status In Force
Filing Date 2019-10-29
First Publication Date 2020-04-30
Grant Date 2021-10-05
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Mickle, Travis

Abstract

Disclosed are d-amphetamine compounds and compositions comprising at least one organic acid covalently bound to d-amphetamine, a salt thereof, a derivative thereof, or a combination thereof. Methods of making and using the same are also disclosed.

IPC Classes  ?

  • C07D 213/56 - Amides
  • A61K 31/4425 - Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
  • C07D 213/79 - AcidsEsters
  • C07D 213/81 - AmidesImides
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • C07D 213/80 - AcidsEsters in position 3
  • A61K 9/02 - SuppositoriesBougiesBases for suppositories or bougies

35.

D-amphetamine compounds, compositions, and processes for making and using the same

      
Application Number 16667807
Grant Number 11174229
Status In Force
Filing Date 2019-10-29
First Publication Date 2020-04-30
Grant Date 2021-11-16
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Mickle, Travis

Abstract

Disclosed are d-amphetamine compounds and compositions comprising at least one organic acid covalently bound to d-amphetamine, having the structure of a salt thereof, a derivative thereof, or a combination thereof. Methods of making and using the same are also disclosed.

IPC Classes  ?

  • C07D 213/56 - Amides
  • A61K 31/4425 - Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
  • C07D 213/79 - AcidsEsters
  • C07D 213/81 - AmidesImides
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • C07D 213/80 - AcidsEsters in position 3
  • A61K 9/02 - SuppositoriesBougiesBases for suppositories or bougies

36.

Compositions comprising methylphenidate-prodrugs, processes of making and using the same

      
Application Number 16588914
Grant Number 10954212
Status In Force
Filing Date 2019-09-30
First Publication Date 2020-02-27
Grant Date 2021-03-23
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen

Abstract

The present technology is directed to d-threo-methylphenidate conjugates and a composition comprising d-threomethylphenidate conjugated to nicotinoyl-L-serine, or salt thereof. The present technology also relates to a composition comprising at least one conjugate of d-methylphenidate having at least two or more chiral centers. The composition is optically active. The present technology additionally relates to oral formulations and pharmaceutical kits comprising at least one d-threo-methylphenidate conjugate. The pharmaceutical kit may comprise a specified amount of individual doses in a package. Each individual dose in the package may contain a pharmaceutically effective amount of a conjugate of d-threo methylphenidate.

IPC Classes  ?

  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate

37.

Methylphenidate-prodrugs, processes of making and using the same

      
Application Number 16431468
Grant Number 10759778
Status In Force
Filing Date 2019-06-04
First Publication Date 2020-02-27
Grant Date 2020-09-01
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen

Abstract

The present technology is directed to compositions comprising d-threo-methylphenidate conjugates and unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

38.

Therapeutic formulation for reduced drug side effects

      
Application Number 16579054
Grant Number 10912744
Status In Force
Filing Date 2019-09-23
First Publication Date 2020-02-20
Grant Date 2021-02-09
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor Desai, Subhash

Abstract

The present invention provides drug therapy formulations for reducing the side effects associated with a therapeutic. In some embodiments, the present invention provides a reduction in sleep- and diet-related side effects associated with a therapeutic.

IPC Classes  ?

  • A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
  • A61K 9/14 - Particulate form, e.g. powders
  • A61K 31/155 - Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (HN=C(OH)NH2), isothiourea (HN=C(SH)—NH2)
  • A61K 31/4168 - 1,3-Diazoles having a nitrogen atom attached in position 2, e.g. clonidine
  • A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K 9/19 - Particulate form, e.g. powders lyophilised
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
  • A61K 9/51 - Nanocapsules

39.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods of making and use thereof

      
Application Number 16573313
Grant Number 10758528
Status In Force
Filing Date 2019-09-17
First Publication Date 2020-01-30
Grant Date 2020-09-01
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib
  • Kanski, Jaroslaw
  • Martin, Andrea

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxymorphone (4,5-α-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxymorphone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxymorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • C07D 489/08 - Oxygen atom
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • C07D 221/28 - Morphinans

40.

Compositions comprising methylphenidate-prodrugs, processes of making and using the same

      
Application Number 16577946
Grant Number 11021460
Status In Force
Filing Date 2019-09-20
First Publication Date 2020-01-16
Grant Date 2021-06-01
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen

Abstract

The present technology is directed to d-threo-methylphenidate conjugates and a composition comprising d-threomethylphenidate conjugated to nicotinoyl-L-serine, or salt thereof. The present technology also relates to a composition comprising at least one conjugate of d-methylphenidate having at least two or more chiral centers. The composition is optically active. The present technology additionally relates to oral formulations and pharmaceutical kits comprising at least one d-threo-methylphenidate conjugate. The pharmaceutical kit may comprise a specified amount of individual doses in a package. Each individual dose in the package may contain a pharmaceutically effective amount of a conjugate of d-threo methylphenidate.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate

41.

Compositions comprising methylphenidate-prodrugs, processes of making and using the same

      
Application Number 16577876
Grant Number 11021459
Status In Force
Filing Date 2019-09-20
First Publication Date 2020-01-16
Grant Date 2021-06-01
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen

Abstract

The present technology is directed to d-threo-methylphenidate conjugates and a composition comprising d-threomethylphenidate conjugated to nicotinoyl-L-serine, or salt thereof. The present technology also relates to a composition comprising at least one conjugate of d-methylphenidate having at least two or more chiral centers. The composition is optically active. The present technology additionally relates to oral formulations and pharmaceutical kits comprising at least one d-threo-methylphenidate conjugate. The pharmaceutical kit may comprise a specified amount of individual doses in a package. Each individual dose in the package may contain a pharmaceutically effective amount of a conjugate of d-threo methylphenidate.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

42.

Pharmaceutically acceptable salts and polymorphic forms of hydrocodone benzoic acid enol ester and processes for making same

      
Application Number 16356938
Grant Number 10870654
Status In Force
Filing Date 2019-03-18
First Publication Date 2019-09-19
Grant Date 2020-12-22
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

Compositions comprising hydrocodone benzoic acid enol ester to form novel prodrugs including hydrocodone benzoic acid enol ester salts, and various polymorphs. Also provided are processes for the preparation of hydrocodone benzoic acid enol ester salts, and various polymorphs.

IPC Classes  ?

  • A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

43.

Methylphenidate-prodrugs, processes of making and using the same

      
Application Number 16431275
Grant Number 10584112
Status In Force
Filing Date 2019-06-04
First Publication Date 2019-09-19
Grant Date 2020-03-10
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen

Abstract

The present technology is directed to compositions comprising d-threo-methylphenidate conjugates and unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine

44.

Methylphenidate-prodrugs, processes of making and using the same

      
Application Number 16431422
Grant Number 10584113
Status In Force
Filing Date 2019-06-04
First Publication Date 2019-09-19
Grant Date 2020-03-10
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen

Abstract

The present technology is directed to compositions comprising d-threo-methylphenidate conjugates and unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine

45.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof

      
Application Number 16290496
Grant Number 10441661
Status In Force
Filing Date 2019-03-01
First Publication Date 2019-06-27
Grant Date 2019-10-15
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/616 - Salicylic acidDerivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
  • A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K 31/70 - CarbohydratesSugarsDerivatives thereof

46.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof

      
Application Number 16166954
Grant Number 10849981
Status In Force
Filing Date 2018-10-22
First Publication Date 2019-05-30
Grant Date 2020-12-01
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides methods of treating a patient having moderate to severe pain, narcotic or opioid abuse or narcotic or opioid withdrawal. The presently described methods are carried out by comprising administering to the patient a pharmaceutically effective amount of a composition comprising acetaminophen and benzoate-hydrocodone hydrochloride. The composition has reduced side effects when compared with unconjugated hydrocodone.

IPC Classes  ?

  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • C07D 491/08 - Bridged systems
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

47.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone, prodrugs, methods of making and use thereof

      
Application Number 16165194
Grant Number 10544153
Status In Force
Filing Date 2018-10-19
First Publication Date 2019-02-14
Grant Date 2020-01-28
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib
  • Bera, Bindu
  • Kanski, Jaroslaw
  • Martin, Andrea

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxycodone (4,5-α-epoxy-14-hydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxycodone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxycodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

48.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof

      
Application Number 16054575
Grant Number 10258696
Status In Force
Filing Date 2018-08-03
First Publication Date 2018-11-29
Grant Date 2019-04-16
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/616 - Salicylic acidDerivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
  • A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids

49.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods of making and use thereof

      
Application Number 16054578
Grant Number 10463660
Status In Force
Filing Date 2018-08-03
First Publication Date 2018-11-29
Grant Date 2019-11-05
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib
  • Kanski, Jaroslaw
  • Martin, Andrea

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxymorphone (4,5-α-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxymorphone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxymorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • C07D 489/08 - Oxygen atom
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • C07D 221/28 - Morphinans

50.

Miscellaneous Design

      
Serial Number 88177869
Status Registered
Filing Date 2018-11-01
Registration Date 2020-07-14
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of pain

51.

Miscellaneous Design

      
Serial Number 88177876
Status Registered
Filing Date 2018-11-01
Registration Date 2020-07-14
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of pain

52.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof

      
Application Number 15901828
Grant Number 10654863
Status In Force
Filing Date 2018-02-21
First Publication Date 2018-06-28
Grant Date 2020-05-19
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides methods of treating a patient having moderate to severe pain, narcotic or opioid abuse or narcotic or opioid withdrawal. The presently described methods are carried out by comprising administering to the patient a pharmaceutically effective amount of a composition comprising acetaminophen and benzoate-hydrocodone hydrochloride. The composition has reduced side effects when compared with unconjugated hydrocodone.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 491/08 - Bridged systems
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 9/00 - Medicinal preparations characterised by special physical form

53.

COMPOSITIONS COMPRISING METHYLPHENIDATE-PRODRUGS, PROCESSES OF MAKING AND USING THE SAME

      
Document Number 03046486
Status Pending
Filing Date 2017-12-09
Open to Public Date 2018-06-14
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven M.
  • Chi, Guochen

Abstract

The present technology is directed to compositions comprising d-threomethylphenidate conjugates and unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threomethylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07F 9/59 - Hydrogenated pyridine rings

54.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof

      
Application Number 15843875
Grant Number 10577376
Status In Force
Filing Date 2017-12-15
First Publication Date 2018-04-19
Grant Date 2020-03-03
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides methods of treating a patient having moderate to severe pain, narcotic or opioid abuse or narcotic or opioid withdrawal. The presently described methods are carried out by comprising administering to the patient a pharmaceutically effective amount of a composition comprising acetaminophen and benzoate-hydrocodone hydrochloride. The composition has reduced side effects when compared with unconjugated hydrocodone.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • C07D 491/08 - Bridged systems
  • C07D 489/04 - SaltsOrganic complexes
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 9/20 - Pills, lozenges or tablets
  • A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 9/00 - Medicinal preparations characterised by special physical form

55.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone, prodrugs, methods of making and use thereof

      
Application Number 15812730
Grant Number 10144740
Status In Force
Filing Date 2017-11-14
First Publication Date 2018-03-08
Grant Date 2018-12-04
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib
  • Bera, Bindu
  • Kanski, Jaroslaw
  • Martin, Andrea

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxycodone (4,5-α-epoxy-14-hydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxycodone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxycodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

56.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof

      
Application Number 15812823
Grant Number 10064956
Status In Force
Filing Date 2017-11-14
First Publication Date 2018-03-08
Grant Date 2018-09-04
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • A61K 9/00 - Medicinal preparations characterised by special physical form

57.

Pharmaceutically acceptable salts and polymorphic forms of hydrocodone benzoic acid enol ester and processes for making same

      
Application Number 15730885
Grant Number 10351574
Status In Force
Filing Date 2017-10-12
First Publication Date 2018-03-01
Grant Date 2019-07-16
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

Compositions comprising hydrocodone benzoic acid enol ester to form novel prodrugs including hydrocodone benzoic acid enol ester salts, and various polymorphs. Also provided are processes for the preparation of hydrocodone benzoic acid enol ester salts, and various polymorphs.

IPC Classes  ?

  • A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

58.

KP

      
Serial Number 87980082
Status Registered
Filing Date 2018-02-15
Registration Date 2019-07-23
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of pain

59.

KEMPHARM

      
Serial Number 87980730
Status Registered
Filing Date 2018-02-15
Registration Date 2019-06-18
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of pain

60.

KEMPHARM INC

      
Serial Number 87980838
Status Registered
Filing Date 2018-02-15
Registration Date 2020-01-14
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 42 - Scientific, technological and industrial services, research and design

Goods & Services

Drug discovery services; Medical research; Research and development in the field of drug discovery

61.

KEMPHARM INC

      
Serial Number 87980858
Status Registered
Filing Date 2018-02-15
Registration Date 2019-06-25
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ?
  • 05 - Pharmaceutical, veterinary and sanitary products
  • 42 - Scientific, technological and industrial services, research and design

Goods & Services

Pharmaceutical preparations for the treatment of pain Drug discovery services; Medical research; Research and development in the field of drug discovery

62.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods of making and use thereof

      
Application Number 15589158
Grant Number 10071091
Status In Force
Filing Date 2017-05-08
First Publication Date 2017-11-02
Grant Date 2018-09-11
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib
  • Kanski, Jaroslaw
  • Martin, Andrea

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxymorphone (4,5-α-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxymorphone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxymorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • C07D 489/08 - Oxygen atom
  • C07D 221/28 - Morphinans

63.

PALATABLE COMPOSITIONS INCLUDING SODIUM PHENYLBUTYRATE AND USES THEREOF

      
Document Number 03017573
Status Pending
Filing Date 2016-10-17
Open to Public Date 2017-09-21
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Appel, Leah E.
  • Shockey, Joshua R.
  • Schelling, D. Christopher

Abstract

The present invention features palatable pharmaceutical compositions including sodium phenylbutyrate and methods for the treatment of inborn errors of metabolism (e.g., Maple Syrup Urine Disease or Urea Cycle Disorders), neurodegenerative disorders such as Parkinson's disease, spinal muscular atrophy, dystonia, or inclusion-body myositis with such compositions.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid

64.

FOCUSEDONATTENTION

      
Serial Number 87608559
Status Registered
Filing Date 2017-09-14
Registration Date 2021-11-02
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 42 - Scientific, technological and industrial services, research and design

Goods & Services

Providing educational information in the field of new product research and development, medical clinical trial research, medical laboratories and medical research, and pharmaceutical research and development; Providing a website featuring educational information in the field of new product research and development, medical clinical trial research, medical laboratories and medical research, and pharmaceutical research and development

65.

Fatty acid conjugates of quetiapine, process for making and using the same

      
Application Number 15595336
Grant Number 09889198
Status In Force
Filing Date 2017-05-15
First Publication Date 2017-08-31
Grant Date 2018-02-13
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating fatty acids to quetiapine. Pharmaceutical compositions and methods of synthesizing conjugates of the present technology are also provided. Methods of treating patients with the compositions of the present technology are also provided.

IPC Classes  ?

  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
  • A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates

66.

Fatty acid conjugates of quetiapine, process for making and using the same

      
Application Number 15595358
Grant Number 09890150
Status In Force
Filing Date 2017-05-15
First Publication Date 2017-08-31
Grant Date 2018-02-13
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating fatty acids to quetiapine. Pharmaceutical compositions and methods of synthesizing conjugates of the present technology are also provided. Methods of treating patients with the compositions of the present technology are also provided.

IPC Classes  ?

  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • C07D 285/36 - Seven-membered rings

67.

Amino acid conjugates of quetiapine, process for making and using the same

      
Application Number 15595374
Grant Number 10010615
Status In Force
Filing Date 2017-05-15
First Publication Date 2017-08-31
Grant Date 2018-07-03
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates

68.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and uses thereof

      
Application Number 15487757
Grant Number 10351573
Status In Force
Filing Date 2017-04-14
First Publication Date 2017-08-10
Grant Date 2019-07-16
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • C07D 489/04 - SaltsOrganic complexes
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 491/08 - Bridged systems
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence

69.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof

      
Application Number 15395475
Grant Number 09849185
Status In Force
Filing Date 2016-12-30
First Publication Date 2017-05-25
Grant Date 2017-12-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • A61K 9/00 - Medicinal preparations characterised by special physical form

70.

LAT

      
Serial Number 87463922
Status Registered
Filing Date 2017-05-25
Registration Date 2019-09-24
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 42 - Scientific, technological and industrial services, research and design

Goods & Services

Drug discovery services; Drug discovery services conducted by means of a scientific laboratory computer software platform used for research and development in the field of drugs; Medical research; Research and development in the field of drug discovery

71.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and uses thereof

      
Application Number 15376211
Grant Number 10358452
Status In Force
Filing Date 2016-12-12
First Publication Date 2017-05-25
Grant Date 2019-07-23
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 491/08 - Bridged systems
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence

72.

Methylphenidate-prodrugs, processes of making and using the same

      
Application Number 15249088
Grant Number 10231960
Status In Force
Filing Date 2016-08-26
First Publication Date 2017-02-23
Grant Date 2019-03-19
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Bera, Bindu
  • Mickle, Travis
  • Bera, Sanjib

Abstract

The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.

IPC Classes  ?

  • C07D 211/68 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
  • C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • A61K 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
  • C07F 9/59 - Hydrogenated pyridine rings
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07K 5/02 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link
  • C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent

73.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and uses thereof

      
Application Number 15076586
Grant Number 09650387
Status In Force
Filing Date 2016-03-21
First Publication Date 2016-07-14
Grant Date 2017-05-16
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • C07D 489/04 - SaltsOrganic complexes
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
  • C07D 491/08 - Bridged systems
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates

74.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and uses thereof

      
Application Number 14817581
Grant Number 09549923
Status In Force
Filing Date 2015-08-04
First Publication Date 2016-07-07
Grant Date 2017-01-24
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • C07D 491/08 - Bridged systems
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 9/00 - Medicinal preparations characterised by special physical form

75.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone, prodrugs, methods of making and use thereof

      
Application Number 14952348
Grant Number 09850252
Status In Force
Filing Date 2015-11-25
First Publication Date 2016-06-16
Grant Date 2017-12-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib
  • Bera, Bindu
  • Kanski, Jaroslaw
  • Martin, Andrea

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxycodone (4,5-α-epoxy-14-hydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxycodone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxycodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
  • C07D 489/04 - SaltsOrganic complexes

76.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods of making and use thereof

      
Application Number 14956642
Grant Number 09682076
Status In Force
Filing Date 2015-12-02
First Publication Date 2016-06-02
Grant Date 2017-06-20
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib
  • Kanski, Jaroslaw
  • Martin, Andrea

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxymorphone (4,5-α-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxymorphone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxymorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • C07D 221/28 - Morphinans

77.

Pharmaceutically acceptable salts and polymorphic forms of hydrocodone benzoic acid enol ester and processes for making same

      
Application Number 14773628
Grant Number 09815844
Status In Force
Filing Date 2014-03-10
First Publication Date 2016-02-11
Grant Date 2017-11-14
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Heinrich, Brian W.
  • Gou, Da-Ming
  • Mirmehrabi, Mahmoud
  • Paul, Bernhard
  • Coughlin, Daniel James

Abstract

Compositions comprising hydrocodone benzoic acid enol ester to form novel prodrugs including hydrocodone benzoic acid enol ester salts, and various polymorphs. Also provided are processes for the preparation of hydrocodone benzoic acid enol ester salts, and various polymorphs.

IPC Classes  ?

  • A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

78.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof

      
Application Number 14816915
Grant Number 09872915
Status In Force
Filing Date 2015-08-03
First Publication Date 2015-11-26
Grant Date 2018-01-23
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides methods of treating a patient having moderate to severe pain, narcotic or opioid abuse or narcotic or opioid withdrawal. The presently described methods are carried out by comprising administering to the patient a pharmaceutically effective amount of a composition comprising acetaminophen and benzoate-hydrocodone hydrochloride. The composition has reduced side effects when compared with unconjugated hydrocodone.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • C07D 491/08 - Bridged systems
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 9/20 - Pills, lozenges or tablets

79.

Methylphenidate-prodrugs, processes of making and using the same

      
Application Number 14727498
Grant Number 09453037
Status In Force
Filing Date 2015-06-01
First Publication Date 2015-09-24
Grant Date 2016-09-27
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Bera, Bindu
  • Mickle, Travis
  • Bera, Sanjib

Abstract

The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.

IPC Classes  ?

  • C07D 211/68 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
  • C07F 9/59 - Hydrogenated pyridine rings
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07K 5/02 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link
  • C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

80.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof

      
Application Number 14557570
Grant Number 09132125
Status In Force
Filing Date 2014-12-02
First Publication Date 2015-03-26
Grant Date 2015-09-15
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • C07D 491/08 - Bridged systems
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol

81.

Phenylethanoic acid, phenylpropanoic acid and phenylpropenoic acid conjugates and prodrugs of hydrocodone, method of making and use thereof

      
Application Number 14493611
Grant Number 09125947
Status In Force
Filing Date 2014-09-23
First Publication Date 2015-02-19
Grant Date 2015-09-08
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal

Abstract

The presently described technology provides phenylethanoic acid, phenylpropanoic acid, phenylpropenoic acid, a salt thereof, a derivative thereof or a combination thereof chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs or compositions of hydrocodone which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/19 - Carboxylic acids, e.g. valproic acid
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine

82.

Fatty acid conjugates of quetiapine, process for making and using the same

      
Application Number 14525836
Grant Number 09511149
Status In Force
Filing Date 2014-10-28
First Publication Date 2015-02-12
Grant Date 2016-12-06
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating fatty acids to quetiapine. Pharmaceutical compositions and methods of synthesizing conjugates of the present technology are also provided. Methods of treating patients with the compositions of the present technology are also provided.

IPC Classes  ?

  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

83.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof

      
Application Number 14336549
Grant Number 09566343
Status In Force
Filing Date 2014-07-21
First Publication Date 2014-11-06
Grant Date 2017-02-14
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 31/616 - Salicylic acidDerivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
  • A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

84.

Amino acid conjugates of quetiapine, process for making and using the same

      
Application Number 14216342
Grant Number 09597403
Status In Force
Filing Date 2014-03-17
First Publication Date 2014-09-25
Grant Date 2017-03-21
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
  • A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
  • C07D 267/18 - [b, e]-condensed

85.

Methylphenidate-oxoacid conjugates, processes of making and using the same

      
Application Number 14234440
Grant Number 09079928
Status In Force
Filing Date 2012-07-27
First Publication Date 2014-08-28
Grant Date 2015-07-14
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Bera, Bindu
  • Mickle, Travis
  • Bera, Sanjib

Abstract

The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.

IPC Classes  ?

  • C07D 211/68 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
  • C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07F 9/59 - Hydrogenated pyridine rings
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07K 5/02 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link
  • C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

86.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof

      
Application Number 13888578
Grant Number 08748413
Status In Force
Filing Date 2013-05-07
First Publication Date 2013-10-03
Grant Date 2014-06-10
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine

87.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof

      
Application Number 13888583
Grant Number 08828978
Status In Force
Filing Date 2013-05-07
First Publication Date 2013-09-26
Grant Date 2014-09-09
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine

88.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof

      
Application Number 13888587
Grant Number 08927716
Status In Force
Filing Date 2013-05-07
First Publication Date 2013-09-19
Grant Date 2015-01-06
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • C07D 491/08 - Bridged systems
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • C07D 489/04 - SaltsOrganic complexes
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates

89.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof

      
Application Number 13660112
Grant Number 08816083
Status In Force
Filing Date 2012-10-25
First Publication Date 2013-06-13
Grant Date 2014-08-26
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
  • A61K 31/625 - Salicylic acidDerivatives thereof having heterocyclic substituents, e.g. 4-salicyloylmorpholine

90.

Fatty acid conjugates of quetiapine, process for making and using the same

      
Application Number 13581496
Grant Number 08900604
Status In Force
Filing Date 2011-03-09
First Publication Date 2013-02-21
Grant Date 2014-12-02
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating fatty acids to quetiapine. Pharmaceutical compositions and methods of synthesizing conjugates of the present technology are also provided. Methods of treating patients with the compositions of the present technology are also provided.

IPC Classes  ?

  • A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
  • A61K 33/00 - Medicinal preparations containing inorganic active ingredients
  • A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
  • A61P 25/24 - Antidepressants
  • A61P 25/32 - Alcohol-abuse
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

91.

Compositions for reduction of side effects

      
Application Number 13656415
Grant Number 09511037
Status In Force
Filing Date 2012-10-19
First Publication Date 2013-02-14
Grant Date 2016-12-06
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor Desai, Subhash

Abstract

The present invention provides drug therapy formulations. In some embodiments, the present invention provides combinations of pharmaceutical agents (e.g., stimulant and non-stimulant), pharmaceutical formulations (e.g., nanoparticualte, non-nanoparticualte, etc.), and release profiles (e g, immediate release, delayed release, sustained release, etc.) to provide therapeutic benefit with reduced side effects.

IPC Classes  ?

  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 9/14 - Particulate form, e.g. powders
  • A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
  • A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
  • A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K 31/4168 - 1,3-Diazoles having a nitrogen atom attached in position 2, e.g. clonidine

92.

METHYLPHENIDATE-PRODRUGS, PROCESSES OF MAKING AND USING THE SAME

      
Document Number 02837732
Status In Force
Filing Date 2012-07-27
Open to Public Date 2013-01-31
Grant Date 2018-03-20
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Guenther, Sven
  • Chi, Guochen
  • Bera, Bindu
  • Mickle, Travis
  • Bera, Sanjib

Abstract

The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.

IPC Classes  ?

  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 25/26 - Psychostimulants, e.g. nicotine, cocaine
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

93.

METHYLPHENIDATE-PRODRUGS, PROCESSES OF MAKING AND USING THE SAME

      
Document Number 02984544
Status In Force
Filing Date 2012-07-27
Open to Public Date 2013-01-31
Grant Date 2021-08-31
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Chi, Guochen
  • Guenther, Sven
  • Bera, Bindu
  • Mickle, Travis
  • Bera, Sanjib

Abstract

The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of mcthylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof. An example conjugate has the structure ofwherein Gm is an amino acid and m = 1-5, or Gm may be replaced by repeating subunitsindependently selected from alcohol, amine, amino acid, ammonium, oxoacid, thiol,peptide, poly(ethylene glycols), and derivatives thereof.

IPC Classes  ?

  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61P 25/26 - Psychostimulants, e.g. nicotine, cocaine
  • C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

94.

Amino acid conjugates of quetiapine, process for making and using the same

      
Application Number 13518981
Grant Number 08715699
Status In Force
Filing Date 2010-12-22
First Publication Date 2012-11-01
Grant Date 2014-05-06
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Bera, Sanjib

Abstract

The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 33/00 - Medicinal preparations containing inorganic active ingredients
  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
  • A61P 25/24 - Antidepressants
  • A61P 25/22 - Anxiolytics

95.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof

      
Application Number 13378800
Grant Number 08759368
Status In Force
Filing Date 2010-07-01
First Publication Date 2012-06-07
Grant Date 2014-06-24
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine

96.

Therapeutic formulation for reduced drug side effects

      
Application Number 13093662
Grant Number 10463633
Status In Force
Filing Date 2011-04-25
First Publication Date 2011-10-27
Grant Date 2019-11-05
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor Desai, Subhash

Abstract

The present invention provides drug therapy formulations for reducing the side effects associated with a therapeutic. In some embodiments, the present invention provides a reduction in sleep- and diet-related side effects associated with a therapeutic.

IPC Classes  ?

  • A61P 25/26 - Psychostimulants, e.g. nicotine, cocaine
  • A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
  • A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
  • A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K 31/4168 - 1,3-Diazoles having a nitrogen atom attached in position 2, e.g. clonidine
  • A61K 9/14 - Particulate form, e.g. powders
  • A61K 9/19 - Particulate form, e.g. powders lyophilised
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

97.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof

      
Application Number 12828381
Grant Number 08461137
Status In Force
Filing Date 2010-07-01
First Publication Date 2011-01-06
Grant Date 2013-06-11
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 47/48038 -

98.

Phenylethanoic acid, phenylpropanoic acid and phenylpropenoic acid conjugates and prodrugs of hydrocodone, method of making and use thereof

      
Application Number 12828456
Grant Number 08871780
Status In Force
Filing Date 2010-07-01
First Publication Date 2011-01-06
Grant Date 2014-10-28
Owner ZEVRA THERAPEUTICS, INC. (USA)
Inventor
  • Mickle, Travis
  • Guenther, Sven
  • Mickle, Christal
  • Chi, Guochen
  • Kanski, Jaroslaw
  • Martin, Andrea K.
  • Bera, Bindu

Abstract

The presently described technology provides phenylethanoic acid, phenylpropanoic acid, phenylpropenoic acid, a salt thereof, a derivative thereof or a combination thereof chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs or compositions of hydrocodone which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

IPC Classes  ?

  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates

99.

KEMPHARM

      
Serial Number 78910382
Status Registered
Filing Date 2006-06-16
Registration Date 2008-04-01
Owner ZEVRA THERAPEUTICS, INC. ()
NICE Classes  ? 42 - Scientific, technological and industrial services, research and design

Goods & Services

MEDICAL RESEARCH