Synthon BV

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A61K 9/20 - Pills, lozenges or tablets 76
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10 - Medical apparatus and instruments 10
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1.

A PROCESS FOR MAKING OSIMERTINIB

      
Application Number EP2024084148
Publication Number 2025/124936
Status In Force
Filing Date 2024-11-29
Publication Date 2025-06-19
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Buchlovic, Marian
  • Bednar, Lukas

Abstract

The invention relates to a process for preparation of compounds of formula (6) and (7), key intermediates for preparation of Osimetrtinib, compound of formula (1).

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen 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

2.

CRYSTALLINE FORMS OF ACALABRUTINIB HYDROGEN MALEATE

      
Application Number EP2024085803
Publication Number 2025/125383
Status In Force
Filing Date 2024-12-11
Publication Date 2025-06-19
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Hegedus, Michal

Abstract

The invention relates to mixed ethanol water solvate and methanol solvate of Acalabrutinib hydrogen maleate, compound of formula (1), solid forms thereof and processes for preparation thereof.

IPC Classes  ?

  • A61P 35/00 - Antineoplastic agents
  • A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
  • C07D 487/04 - Ortho-condensed systems

3.

CABOZANTINIB SALT WITH L-(+)-TARTARIC ACID AND SOLID FORMS THEREOF

      
Application Number 18842577
Status Pending
Filing Date 2023-02-28
First Publication Date 2025-05-29
Owner Synthon B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Jelinkova, Katerina

Abstract

The invention relates to solid forms of Cabozantinib, compound of formula (1), salt with L-(+)-tartaric acid and processes for preparation thereof, The invention relates to solid forms of Cabozantinib, compound of formula (1), salt with L-(+)-tartaric acid and processes for preparation thereof,

IPC Classes  ?

  • C07D 215/22 - Oxygen atoms attached in position 2 or 4

4.

A PROCESS FOR MAKING OSIMERTINIB

      
Application Number 18686210
Status Pending
Filing Date 2022-09-01
First Publication Date 2025-05-15
Owner Synthon B.V. (Netherlands)
Inventor
  • Vyklicky, Libor
  • Zabadal, Miroslav

Abstract

The invention deals with a novel process for preparation of the pharmaceutically useful product Osimertinib of formula (1). The invention deals with a novel process for preparation of the pharmaceutically useful product Osimertinib of formula (1).

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen 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

5.

PHARMACEUTICAL COMPOSITION COMPRISING IBRUTINIB

      
Application Number 18717130
Status Pending
Filing Date 2022-12-06
First Publication Date 2025-05-08
Owner Synthon B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising Ibrutinib and one ore more pharmaceutically acceptable excipients. The invention further relates to the use of said composition as a medicament, particularly in the treatment of lymphocytic leukaemia (CLL), mantle cell lymphoma (MCL), Waldenström's macroglobulinaemia (WM) and chronic graft versus host disease (cGVHD).

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 9/20 - Pills, lozenges or tablets

6.

PHARMACEUTICAL COMPOSITION OF BEMPEDOIC ACID

      
Application Number 18690975
Status Pending
Filing Date 2022-09-12
First Publication Date 2025-05-01
Owner Synthon B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The presented invention relates to pharmaceutical composition comprising Bempedoic acid and processes for preparation thereof.

IPC Classes  ?

  • A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
  • A61K 9/20 - Pills, lozenges or tablets

7.

PHARMACEUTICAL COMPOSITION COMPRISING ENZALUTAMIDE

      
Application Number 18762066
Status Pending
Filing Date 2024-07-02
First Publication Date 2024-10-24
Owner Synthon B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising a granulate consisting of a co-precipitate on a substrate, wherein the co-precipitate comprises enzalutamide in amorphous form and a cellulosic concentration enhancing polymer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of castration-resistant prostate cancer.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61J 3/00 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
  • A61J 3/10 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin

8.

PROLONGED RELEASE TOFACITINIB COMPOSITIONS

      
Application Number 18566329
Status Pending
Filing Date 2022-06-03
First Publication Date 2024-08-29
Owner Synthon B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a monolithic tablet composition for oral administration of tofacitinib, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets

9.

PROCESS FOR MAKING MELFLUFEN OR A SALT THEREOF

      
Application Number 18565888
Status Pending
Filing Date 2022-06-01
First Publication Date 2024-08-15
Owner Synthon B.V. (Netherlands)
Inventor
  • Bartos, Petr
  • Castulik, Jakub

Abstract

The present invention relates to process for preparing Melflufen, compound of formula (1) or a salt thereof, and to intermediates used in the process and solid forms thereof. The present invention relates to process for preparing Melflufen, compound of formula (1) or a salt thereof, and to intermediates used in the process and solid forms thereof.

IPC Classes  ?

  • C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
  • C07C 237/20 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
  • C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated

10.

PHARMACEUTICAL COMPOSITION COMPRISING PALBOCICLIB

      
Application Number EP2023085226
Publication Number 2024/132652
Status In Force
Filing Date 2023-12-11
Publication Date 2024-06-27
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a pharmaceutical granulate composition comprising Palbociclib free base with a high surface area having improving processability.

IPC Classes  ?

  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

11.

PHARMACEUTICAL COMPOSITION COMPRISING PALBOCICLIB

      
Application Number EP2023087324
Publication Number 2024/133726
Status In Force
Filing Date 2023-12-21
Publication Date 2024-06-27
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a pharmaceutical granulate composition comprising Palbociclib free base with a high surface area having improving processability.

IPC Classes  ?

  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

12.

PHARMACEUTICAL COMPOSITION OF SIPONIMOD

      
Application Number EP2023085195
Publication Number 2024/126409
Status In Force
Filing Date 2023-12-11
Publication Date 2024-06-20
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to pharmaceutical composition comprising siponimod and processes for preparation thereof.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • C07B 63/00 - PurificationSeparation specially adapted for the purpose of recovering organic compoundsStabilisationUse of additives
  • A61K 9/14 - Particulate form, e.g. powders

13.

FORMULATION COMPRISING EDOXABAN AND PREPARATION THEREOF

      
Application Number EP2023084960
Publication Number 2024/121413
Status In Force
Filing Date 2023-12-08
Publication Date 2024-06-13
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The invention relates to the tablet composition comprising edoxaban obtained by the direct compression process comprising the step of co-blending edoxaban and first portion of mannitol, wherein the weight ratio of edoxaban and first portion of mannitol is from 1:1 to 1:2.5.

IPC Classes  ?

14.

A PROCESS FOR PREPARATION OF CABOZANTINIB OR TIVOZANIB

      
Application Number EP2023082902
Publication Number 2024/110606
Status In Force
Filing Date 2023-11-23
Publication Date 2024-05-30
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Hylse, Ondrej
  • Partl, Jiri

Abstract

The presented invention relates to a process for preparation of Cabozantinib, compound of formula (1), or Tivozanib, compound of formula (10) or a salr or a solvate thereof: Formula (1); Formula (10).

IPC Classes  ?

  • C07D 215/20 - Oxygen atoms
  • C07D 413/12 - 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 chain containing hetero atoms as chain links
  • C07C 235/74 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of a saturated carbon skeleton

15.

STABLE FORMULATION COMPRISING OBETICHOLIC ACID

      
Application Number EP2023081607
Publication Number 2024/104960
Status In Force
Filing Date 2023-11-13
Publication Date 2024-05-23
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a stable pharmaceutical formulation comprising obeticholic acid in a primary packaging, wherein the primary packaging further comprises adsorbing material. The formulation is preferably in the form of tablets for oral administration.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol

16.

CRYSTALLINE FORM OF ASCIMINIB HYDROCHLORIDE

      
Application Number EP2023081342
Publication Number 2024/100212
Status In Force
Filing Date 2023-11-09
Publication Date 2024-05-16
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Hegedus, Michal

Abstract

The application relates to the crystalline Form 1S of Asciminib hydrochloride and processes for the preparation thereof. Also described are solvates of Asciminib with 2-butanol, isobutanol, tert- butanol, 2-methyl tetra hydrofuran and cyclohexanol from which the crystalline Form 1S of Asciminib hydrochloride can be prepared.

IPC Classes  ?

  • C07D 401/14 - 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 three or more hetero rings
  • A61P 35/02 - Antineoplastic agents specific for leukemia
  • 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

17.

CAPILLARY GEL ELECTROPHORESIS SEPARATION OF DIASTEREOMERS OF PHOSPHOROTHIOATED OLIGONUCLEOTIDES

      
Application Number EP2023079519
Publication Number 2024/088984
Status In Force
Filing Date 2023-10-23
Publication Date 2024-05-02
Owner SYNTHON B.V. (Netherlands)
Inventor Durc, Pavol

Abstract

Method of identification and/or characterization of diastereomers mixtures of phosphorothioate oligonucleotides by capillary gel electrophoresis with a background electrolyte that has a pH 6 to 8, comprising the steps of: a) Preparing a gel matrix by dissolving a water soluble polymer containing a side chain having a functional group that interacts with diastereomers mixture to be analysed in a background electrolyte; b) Introducing the gel matrix in the capillary; c) Introducing the sample of diastereomers mixture of phosphorothioate to capillary; d) Applying an electric field greater than 200 volts/cm of capillary across the gel matrix in the capillary; e) Detecting the individual diastereomers and/or the characteristic groups of partially separated diastereomers of phosphorothioate oligonucleotides.

IPC Classes  ?

18.

PROCESS FOR MAKING IBRUTINIB

      
Application Number 18261896
Status Pending
Filing Date 2022-01-20
First Publication Date 2024-03-21
Owner Synthon B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Vyklicky, Libor
  • Bartl, Jiri
  • Smekal, Oldrich

Abstract

The presented invention relates to a process for preparation of Ibrutinib, comprising: a. Reacting compound of Formula (2) with compound of Formula (3) in a presence of Lewis acid to provide compound of Formula (4); b. Contacting compound of Formula (4) with toluene; c. Isolate a solid form of compound of Formula (4); d. Transforming compound of Formula (4) into Ibrutinib. The presented invention relates to a process for preparation of Ibrutinib, comprising: a. Reacting compound of Formula (2) with compound of Formula (3) in a presence of Lewis acid to provide compound of Formula (4); b. Contacting compound of Formula (4) with toluene; c. Isolate a solid form of compound of Formula (4); d. Transforming compound of Formula (4) into Ibrutinib.

IPC Classes  ?

19.

PROLONGED RELEASE TOFACITINIB COMPOSITIONS WITHOUT FUNCTIONAL COATING

      
Application Number EP2023073382
Publication Number 2024/042218
Status In Force
Filing Date 2023-08-25
Publication Date 2024-02-29
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a monolithic tablet composition for oral administration of tofacitinib or a pharmaceutically acceptable salt thereof, without a functional coating.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

20.

Process for making palbociclib

      
Application Number 18474840
Grant Number 12240847
Status In Force
Filing Date 2023-09-26
First Publication Date 2024-02-01
Grant Date 2025-03-04
Owner Synthon B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Smekal, Oldrich

Abstract

The present invention relates to a process for preparation of palbociclib, compound of formula (1) or a salt thereof, wherein an intermediate, compound (2), is formed by reacting a compound of formula (3) and a compound of formula (4) in a solvent mixture comprising methanol and butanol: The intermediate (2) can be transformed into palbociclib or a salt thereof.

IPC Classes  ?

21.

BUDESONIDE TWO LAYERS CAPSULE FORMULATION

      
Application Number EP2023069160
Publication Number 2024/013154
Status In Force
Filing Date 2023-07-11
Publication Date 2024-01-18
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a Budesonide formulation with one or more layers comprising organic acid and Budesonide in the same layer.

IPC Classes  ?

  • A61K 9/50 - Microcapsules
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin

22.

SIPONIMOD SALTS AND COCRYSTALS

      
Application Number 18246566
Status Pending
Filing Date 2021-09-24
First Publication Date 2024-01-11
Owner Synthon B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Partl, Jiri
  • Tesson, Nicolas
  • Trilla Castano, Montserrat

Abstract

The presented invention relates to solid forms of Siponimod adipic acid salt and cocrystal.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
  • C07C 55/14 - Adipic acid

23.

SOLID FORMS OF COPANLISIB SALTS

      
Application Number EP2023062757
Publication Number 2023/218032
Status In Force
Filing Date 2023-05-12
Publication Date 2023-11-16
Owner SYNTHON B.V. (Netherlands)
Inventor Dymacek, Bohumil

Abstract

The invention relates to solid forms of Copanlisib hydrogen phosphate salt or Copanlisib fumarate salt or Copanlisib ditosylate salt or Copanlisib hydrogen citrate salt or Copanlisib maleate salt or Copanlisib malate salt or Copanlisib tartrate salt or Copanlisib dilactate salt or Copanlisib diacetate salt or Copanlisib dihydrochloride salt.

IPC Classes  ?

24.

Synthon

      
Application Number 1757730
Status Registered
Filing Date 2023-05-30
Registration Date 2023-05-30
Owner Synthon B.V. (Netherlands)
NICE Classes  ?
  • 05 - Pharmaceutical, veterinary and sanitary products
  • 10 - Medical apparatus and instruments
  • 35 - Advertising and business services
  • 40 - Treatment of materials; recycling, air and water treatment,
  • 42 - Scientific, technological and industrial services, research and design
  • 45 - Legal and security services; personal services for individuals.

Goods & Services

Pharmaceutical preparations, substances and compositions; biological and biochemical drug and cultures for medical use; pharmaceutical active substances; pharmaceutical components and ingredients. Surgical and medical devices, apparatus and instruments; orthopedic articles; injection apparatus for medical purposes. Office functions relating to the registration of pharmaceutical preparations; compiling registration files, for others; procurement of contracts for others; commercial administration of the licensing of goods; advertising, marketing and promotional services for the sale of pharmaceutical drugs, pharmaceutical preparations and medical devices; retail and wholesale services for pharmaceutical drugs, pharmaceutical preparations and medical devices; retail and online sale of pharmaceutical drugs, pharmaceutical preparations and medical devices. Treatment of materials, including on request, for others, for the purpose of manufacturing pharmaceutical and biopharmaceutical preparations; manufacture, for others, of pharmaceutical and biopharmaceutical preparations and raw materials for the pharmaceutical industry. Consulting services in the field of pharmaceutical research; biomedical research services; chemistry and biology laboratories; scientific laboratory services; pharmaceutical research and development in the pharmaceutical field; information relating to medical and scientific research in the field of pharmaceutical preparations; providing information on the results of clinical trials for pharmaceutical preparations; quality control of products for the purpose of certification; laboratory research and laboratory analysis; research and design for the pharmaceutical industry; research and development of new products for others; drug discovery testing in the context of quality control; conducting clinical trials for pharmaceutical preparations; conducting quality control of pharmaceutical preparations; providing information and data relating to medical research and developments; scientific and medical research and development; development of medicines to be sold by and under the trademark of third parties; development of pharmaceutical ingredients for the pharmaceutical industry. Legal services relating to obtaining pharmaceutical registrations and compiling pharmaceutical registration files; management of industrial property and copyright by means of license agreements (legal services); licensing of intellectual property; management of industrial property and copyright by issuing licenses to others (legal services); legal extensions relating to the retention of intellectual property, for others; legal advice in the field of intellectual property.

25.

PHARMACEUTICAL COMPOSITION COMPRISING IBRUTINIB

      
Application Number 18043176
Status Pending
Filing Date 2021-08-23
First Publication Date 2023-10-12
Owner Synthon B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a coated tablet composition comprising ibrutinib and one or more pharmaceutically acceptable excipients, characterized in that: ⋅Ibmtinib is form C, having characteristic peaks in the X-ray powder diffraction pattern at the following 2 theta (±0.2) angles: 6.9°, 18.2°, 19.2°, 19.6° and 23.0°, measured using a Cu Kα radiation; and ⋅The coating is free of plasticizer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of chronic lymphocytic leukaemia (CLL), mantle cell lymphoma (MCL), Waldenström's macroglobulinaemia (WM) and chronic graft-versus-host disease (cGVHD).

IPC Classes  ?

  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

26.

SOLID FORMS OF VISMODEGIB

      
Application Number EP2023058668
Publication Number 2023/194300
Status In Force
Filing Date 2023-04-03
Publication Date 2023-10-12
Owner SYNTHON B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

Presented invention relates to solid forms of Vismodegib, compound of formula (1) and processes for preparation thereof.

IPC Classes  ?

27.

IMPROVED PROCESS FOR PREPARATION OF APALUTAMIDE

      
Application Number 18043777
Status Pending
Filing Date 2021-09-03
First Publication Date 2023-10-05
Owner Synthon B.V. (Netherlands)
Inventor
  • Hylse, Ondrej
  • Chalupa, David
  • Dymacek, Bohumil
  • Buchlovic, Marian

Abstract

The presented invention relates to a process for preparation of Apalutamide, compound (1) (Formula 1) or a salt or a solvate thereof: The presented invention further relates to solid forms of Apalutamide, solvates of Apalutamide and to processes for preparation thereof. The presented invention also relates to solid forms of intermediates used in the process for preparing Compound (1). The presented invention relates to a process for preparation of Apalutamide, compound (1) (Formula 1) or a salt or a solvate thereof: The presented invention further relates to solid forms of Apalutamide, solvates of Apalutamide and to processes for preparation thereof. The presented invention also relates to solid forms of intermediates used in the process for preparing Compound (1).

IPC Classes  ?

  • C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
  • C07C 229/48 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring

28.

CABOZANTINIB SALT WITH L-(+)-TARTARIC ACID AND SOLID FORMS THEREOF

      
Application Number EP2023054897
Publication Number 2023/165948
Status In Force
Filing Date 2023-02-28
Publication Date 2023-09-07
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Jelinkova, Katerina

Abstract

The invention relates to solid forms of Cabozantinib, compound of formula (1), salt with L-(+)-tartaric acid and processes for preparation thereof,

IPC Classes  ?

29.

SOLID FORMS OF ALECTINIB AND ALECTINIB SALTS

      
Application Number EP2023054326
Publication Number 2023/161233
Status In Force
Filing Date 2023-02-21
Publication Date 2023-08-31
Owner SYNTHON B.V. (Netherlands)
Inventor Dymacek, Bohumil

Abstract

The invention relates to Alectinib, compound of formula (1), solid forms thereof, salts thereof, solid forms of the salts and processes for preparation thereof,.

IPC Classes  ?

  • C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/04 - Antineoplastic agents specific for metastasis

30.

IMPROVED PROCESS FOR PREPARATION OF COPANLISIB

      
Application Number EP2023051132
Publication Number 2023/139125
Status In Force
Filing Date 2023-01-18
Publication Date 2023-07-27
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dragounova, Kristyna
  • Benovsky, Petr

Abstract

The presented invention relates to a process for preparation of Copanlisib, compound of formula (1), or a salt or a solvate thereof comprising:.

IPC Classes  ?

31.

CRYSTALLINE FORM OF OZANIMOD HYDROCHLORIDE

      
Application Number 17995180
Status Pending
Filing Date 2021-03-17
First Publication Date 2023-06-15
Owner Synthon B.V. (Netherlands)
Inventor Westheim, Raymond

Abstract

The presented invention relates to crystalline form, Form A of Ozanimod hydrochloride, processes for preparation thereof and pharmaceutical compositions comprising the Ozanimod hydrochloride Form A.

IPC Classes  ?

  • C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles

32.

PHARMACEUTICAL COMPOSITION COMPRISING IBRUTINIB

      
Application Number EP2022084622
Publication Number 2023/104808
Status In Force
Filing Date 2022-12-06
Publication Date 2023-06-15
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising Ibrutinib and one or more pharmaceutically acceptable excipients. The invention further relates to the use of said composition as a medicament, particularly in the treatment of chronic lymphocytic leukaemia (CLL), mantle cell lymphoma (MCL), Waldenstrӧm's macroglobulinaemia (WM) and chronic graft versus host disease (cGVHD).

IPC Classes  ?

33.

PHARMACEUTICAL COMPOSITION OF BEMPEDOIC ACID

      
Document Number 03231425
Status Pending
Filing Date 2022-09-12
Open to Public Date 2023-03-16
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The presented invention relates to pharmaceutical composition comprising Bempedoic acid and processes for preparation thereof.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid

34.

PHARMACEUTICAL COMPOSITION OF BEMPEDOIC ACID

      
Application Number EP2022075272
Publication Number 2023/036980
Status In Force
Filing Date 2022-09-12
Publication Date 2023-03-16
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The presented invention relates to pharmaceutical composition comprising Bempedoic acid and processes for preparation thereof.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid

35.

A PROCESS FOR MAKING OSIMERTINIB

      
Document Number 03229553
Status Pending
Filing Date 2022-09-01
Open to Public Date 2023-03-09
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vyklicky, Libor
  • Zabadal, Miroslav

Abstract

The invention deals with a novel process for preparation of the pharmaceutically useful product Osimertinib of formula (1).

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen 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

36.

A PROCESS FOR MAKING OSIMERTINIB

      
Application Number EP2022074288
Publication Number 2023/031316
Status In Force
Filing Date 2022-09-01
Publication Date 2023-03-09
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vyklicky, Libor
  • Zabadal, Miroslav

Abstract

The invention deals with a novel process for preparation of the pharmaceutically useful product Osimertinib of formula (1).

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen 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

37.

CRYSTALLINE FORMS OF TAFAMIDIS NICOTINAMIDE ADDUCT

      
Application Number EP2022070086
Publication Number 2023/020762
Status In Force
Filing Date 2022-07-18
Publication Date 2023-02-23
Owner SYNTHON B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

The presented invention relates to Tafamidis nicotinamide adduct, solid form thereof, crystalline form thereof, processes for preparation thereof and a composition comprising it.

IPC Classes  ?

  • C07D 213/82 - AmidesImides in position 3
  • C07D 263/57 - Aryl or substituted aryl radicals
  • A61P 17/00 - Drugs for dermatological disorders
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 43/00 - Drugs for specific purposes, not provided for in groups
  • A61K 31/423 - Oxazoles condensed with carbocyclic rings

38.

CRYSTALLINE FORMS OF SODIUM SALT OF BEMPEDOIC ACID

      
Application Number 17781915
Status Pending
Filing Date 2020-12-04
First Publication Date 2023-02-02
Owner SYNTHON B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

The presented invention relates to crystalline Forms (I) or (II) or (III) or (IV) of sodium salt of Bempedoic acid, processes for preparation thereof and a composition comprising it.

IPC Classes  ?

  • C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups

39.

PHARMACEUTICAL COMPOSITION COMPRISING ELTROMBOPAG BIS(MONOETHANOLAMINE)

      
Application Number 17782425
Status Pending
Filing Date 2020-12-04
First Publication Date 2023-01-26
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a film-coated swallowable tablet comprising eltrombopag bis(monoethanolamine) and pharmaceutically acceptable excipients comprising calcium silicate as diluent. The invention further relates to the use of said tablet as a medicament, particularly in the treatment of immune thrombocytopenia (ITP), thrombocytopenia in patients with chronic hepatitis C virus (HCV) and severe aplastic anaemia (SAA).

IPC Classes  ?

  • A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/28 - DrageesCoated pills or tablets

40.

PHARMACEUTICAL COMPOSITION COMPRISING ELTROMBOPAG BIS(MONOETHANOLAMINE)

      
Application Number 17782408
Status Pending
Filing Date 2020-12-04
First Publication Date 2023-01-26
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a film-coated swallowable tablet comprising eltrombopag bis(monoethanolamine) and pharmaceutically acceptable excipients comprising maltose and isomalt as diluents. The invention further relates to the use of said tablet as a medicament, particularly in the treatment of immune thrombocytopenia (ITP), thrombocytopenia inpatients with chronic hepatitis C virus (HCV) and severe aplastic anaemia (SAA).

IPC Classes  ?

  • A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
  • A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers

41.

CONTROLLED RELEASE TOFACITINIB COMPOSITIONS

      
Application Number 17638448
Status Pending
Filing Date 2020-08-27
First Publication Date 2022-12-22
Owner Synthon B.V. (Netherlands)
Inventor
  • Alvarez Fernandez, Lisardo
  • Nogueiras Nieto, Luis
  • Kumar, Rohit

Abstract

The present invention relates to a monolithic tablet composition for oral administration of tofacitinib, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/50 - Microcapsules
  • A61K 9/20 - Pills, lozenges or tablets

42.

PROCESS FOR MAKING MELFLUFEN OR A SALT THEREOF

      
Application Number EP2022064901
Publication Number 2022/253894
Status In Force
Filing Date 2022-06-01
Publication Date 2022-12-08
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Bartos, Petr
  • Castulik, Jakub

Abstract

The present invention relates to process for preparing Melflufen, compound of formula (1) or a salt thereof, and to intermediates used in the process and solid forms thereof.

IPC Classes  ?

43.

PROLONGED RELEASE TOFACITINIB COMPOSITIONS

      
Application Number EP2022065209
Publication Number 2022/254017
Status In Force
Filing Date 2022-06-03
Publication Date 2022-12-08
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a monolithic tablet composition for oral administration of tofacitinib, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis

44.

PHARMACEUTICAL COMPOSITION COMPRISING ENZALUTAMIDE

      
Application Number 17765934
Status Pending
Filing Date 2020-10-01
First Publication Date 2022-11-03
Owner Synthon B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising a granulate consisting of a co-precipitate on a substrate, wherein the co-precipitate comprises enzalutamide in amorphous form and a cellulosic concentration enhancing polymer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of castration-resistant prostate cancer.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
  • A61J 3/10 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
  • A61J 3/00 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms

45.

CRYSTALLINE FORMS OF BEMPEDOIC ACID

      
Application Number 17765956
Status Pending
Filing Date 2020-10-02
First Publication Date 2022-11-03
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Hegedus, Michal
  • Westheim, Raymond

Abstract

The presented invention relates to crystalline Form A and Form B of Bempedoic acid, a process for preparation thereof and a composition comprising the Form A or Form B.

IPC Classes  ?

  • C07C 51/43 - SeparationPurificationStabilisationUse of additives by change of the physical state, e.g. crystallisation

46.

SALTS OF OMECAMTIV MECARBIL AND SOLID FORMS THEREOF

      
Application Number 17761900
Status Pending
Filing Date 2020-09-18
First Publication Date 2022-11-03
Owner SYNTHON B.V. (Netherlands)
Inventor Jelinkova, Katerina

Abstract

The presented invention relates to Omecamtiv mecarbil salts with methane sulfonic acid, benzene sulfonic acid and p-toluene sulfonic acid and to processes for preparation thereof.

IPC Classes  ?

  • C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates

47.

SALTS OF OMECAMTIV MECARBIL AND SOLID FORMS THEREOF

      
Application Number 17761944
Status Pending
Filing Date 2020-09-18
First Publication Date 2022-10-27
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Jelinkova, Katerina
  • Hegedus, Michal

Abstract

The presented invention relates to Omecamtiv mecarbil salts, solid forms thereof and to processes for preparation 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

48.

LYOPHILIZED COMPOSITION OF COPANLISIB SALT

      
Application Number EP2022058763
Publication Number 2022/214400
Status In Force
Filing Date 2022-04-01
Publication Date 2022-10-13
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Zaludek, Borek
  • Lobl, Jiri

Abstract

The presented invention relates to a lyophilized pharmaceutical formulation comprising copanlisib salt and a bulking agent selected from lactose or trehalose and to a process for preparation thereof.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/19 - Particulate form, e.g. powders lyophilised
  • A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

49.

ISAVUCONAZONIUM SALTS AND PROCESS FOR PREPARING THEREOF

      
Application Number 17638102
Status Pending
Filing Date 2020-08-17
First Publication Date 2022-09-15
Owner Synthon B.V. (Netherlands)
Inventor Bartos, Petr

Abstract

The present invention relates to the process of preparation of salts of compound of formula (1). The present invention relates to the process of preparation of salts of compound of formula (1).

IPC Classes  ?

  • 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

50.

IMPROVED PROCESS FOR PREPARING OZANIMOD

      
Application Number 17627386
Status Pending
Filing Date 2020-07-16
First Publication Date 2022-08-18
Owner Synthon B.V. (Netherlands)
Inventor
  • Chalupova, Lenka
  • Buchlovic, Marian

Abstract

The present invention relates to the process of preparation of compound of formula (I) or a salt thereof. Further it relates to the solid form of compound (I).

IPC Classes  ?

  • C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles

51.

PROCESS FOR PREPARATION OF ENZALUTAMIDE

      
Application Number 17620314
Status Pending
Filing Date 2020-06-25
First Publication Date 2022-08-04
Owner Synthon B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Smekal, Oldrich

Abstract

The presented invention relates to a process for preparation of Enzalutamide, compound (1) or a salt or a solvate thereof Formula (1). The presented invention also related to 1,4-dioxane solvate of compound (1). The presented invention relates to a process for preparation of Enzalutamide, compound (1) or a salt or a solvate thereof Formula (1). The presented invention also related to 1,4-dioxane solvate of compound (1).

IPC Classes  ?

  • C07D 233/86 - Oxygen and sulfur atoms, e.g. thiohydantoin

52.

PROCESS FOR MAKING IBRUTINIB

      
Application Number EP2022051250
Publication Number 2022/157250
Status In Force
Filing Date 2022-01-20
Publication Date 2022-07-28
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Vyklicky, Libor
  • Bartl, Jiri
  • Smekal, Oldrich

Abstract

The presented invention relates to a process for preparation of Ibrutinib, comprising: a. Reacting compound of Formula (2) with compound of Formula (3) in a presence of Lewis acid to provide compound of Formula (4); b. Contacting compound of Formula (4) with toluene; c. Isolate a solid form of compound of Formula (4); d. Transforming compound of Formula (4) into Ibrutinib.

IPC Classes  ?

53.

Pharmaceutical composition comprising axitinib

      
Application Number 17609545
Grant Number 12290601
Status In Force
Filing Date 2020-05-08
First Publication Date 2022-07-21
Grant Date 2025-05-06
Owner Synthon B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Kumar, Rohit
  • Alvarez Fernandez, Lisardo

Abstract

The present invention relates to an immediate release tablet composition comprising axitinib form IV characterized by an XRPD pattern comprising the peaks at about 8.9, 12.0, 14.6, 15.2, 15.7, 17.8, 19.1, 20.6, 21.6, 23.2, 24.2, 24.9, 26.1 and 27.5±0.1 degrees 2θ, when measured with Cu Kα1 radiation and one or more pharmaceutically acceptable excipients, wherein the composition exhibits a dissolution rate between 40% and 70% in 30 minutes when tested in 900 ml 0.01 N hydrochloric acid pH 2.0 at 37° C., 75 rpm in a USP apparatus II.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • 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
  • A61P 35/00 - Antineoplastic agents

54.

PROCESS FOR MAKING SIPONIMOD AND INTERMEDIATE THEREOF

      
Application Number 17599868
Status Pending
Filing Date 2020-03-29
First Publication Date 2022-06-30
Owner Synthon B.V. (Netherlands)
Inventor
  • Keltjens, Rolf
  • Hylse, Ondrej
  • Partl, Jiri

Abstract

The presented invention relates to a process for preparation of compound of formula (I) or a salt or a solvate thereof (i.e.) siponimod. The invention also relates to intermediates used in the process and solid forms of these intermediates. The presented invention relates to a process for preparation of compound of formula (I) or a salt or a solvate thereof (i.e.) siponimod. The invention also relates to intermediates used in the process and solid forms of these intermediates.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
  • C07C 17/16 - Preparation of halogenated hydrocarbons by replacement by halogens of hydroxyl groups
  • C07C 249/08 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes by reaction of hydroxylamines with carbonyl compounds
  • C07C 249/12 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes by reactions not involving the formation of oxyimino groups
  • C07C 303/28 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof

55.

PROCESS FOR PREPARATION OF AXITINIB

      
Application Number 17604322
Status Pending
Filing Date 2020-04-09
First Publication Date 2022-06-23
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Castulik, Jakub
  • Skoumal, Radomir

Abstract

1) A process for preparing Axitinib (N-methyl-2-({3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl}sulfanyl)benzamide; compound of formula (I)) 2) A process for purifying the intermediate 2-((3-iodo-1H-indazol-6-yl)thio)-N-methylbenzamide (compound of formula (IIa)) 3) A process for purifying Axitinib using the Axitinib HCI salt (compound of formula (VIII)) as an intermediate 4) A solid form of the Axitinib HCI salt (form J) characterized by an XRPD pattern 1) A process for preparing Axitinib (N-methyl-2-({3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl}sulfanyl)benzamide; compound of formula (I)) 2) A process for purifying the intermediate 2-((3-iodo-1H-indazol-6-yl)thio)-N-methylbenzamide (compound of formula (IIa)) 3) A process for purifying Axitinib using the Axitinib HCI salt (compound of formula (VIII)) as an intermediate 4) A solid form of the Axitinib HCI salt (form J) characterized by an XRPD pattern

IPC Classes  ?

  • 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 231/56 - BenzopyrazolesHydrogenated benzopyrazoles

56.

SOLID FORMS OF BALOXAVIR, SALTS OF BALOXAVIR AND COCRYSTALS OF BALOXAVIR

      
Application Number EP2021085526
Publication Number 2022/128934
Status In Force
Filing Date 2021-12-13
Publication Date 2022-06-23
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Hegedus, Michal
  • Tesson, Nicolas

Abstract

The presented invention relates to Baloxavir, salts of Baloxavir, cocrystals of Baloxavir, to solid forms of thereof and to processes for preparation thereof.

IPC Classes  ?

  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
  • C07D 498/04 - Ortho-condensed systems
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole

57.

SIPONIMOD SALTS AND COCRYSTALS

      
Document Number 03197026
Status Pending
Filing Date 2021-09-24
Open to Public Date 2022-03-31
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Partl, Jiri
  • Tesson, Nicolas
  • Trilla Castano, Montserrat

Abstract

The presented invention relates to solid forms of Siponimod adipic acid salt and cocrystal.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

58.

SIPONIMOD SALTS AND COCRYSTALS

      
Application Number EP2021076406
Publication Number 2022/064007
Status In Force
Filing Date 2021-09-24
Publication Date 2022-03-31
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Partl, Jiri
  • Tesson, Nicolas
  • Trilla Castano, Montserrat

Abstract

The presented invention relates to solid forms of Siponimod adipic acid salt and cocrystal.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • A61P 37/00 - Drugs for immunological or allergic disorders

59.

IMPROVED PROCESS FOR PREPARATION OF APALUTAMIDE

      
Application Number EP2021074415
Publication Number 2022/049265
Status In Force
Filing Date 2021-09-03
Publication Date 2022-03-10
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Hylse, Ondrej
  • Chalupa, David
  • Dymacek, Bohumil
  • Buchlovic, Marian

Abstract

The presented invention relates to a process for preparation of Apalutamide, compound (1) (Formula 1) or a salt or a solvate thereof: The presented invention further relates to solid forms of Apalutamide, solvates of Apalutamide and to processes for preparation thereof. The presented invention also relates to solid forms of intermediates used in the process for preparing Compound (1).

IPC Classes  ?

  • C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
  • C07C 229/48 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring

60.

Crystalline forms and processes of lenvatinib besylate

      
Application Number 17282505
Grant Number 12102630
Status In Force
Filing Date 2019-10-01
First Publication Date 2022-03-03
Grant Date 2024-10-01
Owner Synthon B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Westheim, Raymond
  • Jelinkova, Katerina

Abstract

The present invention relates to lenvatinib besylate, its crystalline forms and processes for making them. Furthermore, to a pharmaceutical composition comprising a therapeutically effective dose of lenvatinib besylate.

IPC Classes  ?

  • A61K 31/47 - QuinolinesIsoquinolines
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • C07D 215/48 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

61.

PHARMACEUTICAL COMPOSITION COMPRISING IBRUTINIB

      
Application Number EP2021073253
Publication Number 2022/043251
Status In Force
Filing Date 2021-08-23
Publication Date 2022-03-03
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a coated tablet composition comprising ibrutinib and one or more pharmaceutically acceptable excipients, characterized in that: • Ibrutinib is form C, having characteristic peaks in the X-ray powder diffraction pattern at the following 2 theta (± 0.2) angles: 6.9º, 18.2º, 19.2º, 19.6º and 23.0º, measured using a Cu Kα radiation; and • The coating is free of plasticizer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of chronic lymphocytic leukaemia (CLL), mantle cell lymphoma (MCL), Waldenstrӧm's macroglobulinaemia (WM) and chronic graft-versus-host disease (cGVHD).

IPC Classes  ?

  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia
  • A61K 9/20 - Pills, lozenges or tablets

62.

PHARMACEUTICAL COMPOSITION COMPRISING IVACAFTOR

      
Application Number EP2021069774
Publication Number 2022/013360
Status In Force
Filing Date 2021-07-15
Publication Date 2022-01-20
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to an immediate release tablet composition comprising free particles of ivacaftor a pH dependent polymer and surfactant extragranularly and intragranularly.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

63.

SALTS OF BEMPEDOIC ACID

      
Application Number EP2021066439
Publication Number 2021/255180
Status In Force
Filing Date 2021-06-17
Publication Date 2021-12-23
Owner SYNTHON B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

The present invention relates to 2-aminoethanol, piperazine and L- lysine salts of Bempedoic acid and processes for the preparation thereof.

IPC Classes  ?

  • C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups
  • C07D 295/027 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
  • C07C 215/08 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with only one hydroxy group and one amino group bound to the carbon skeleton
  • C07C 229/26 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine

64.

GRIPMATE

      
Serial Number 97185273
Status Pending
Filing Date 2021-12-22
Owner Synthon B.V. (Netherlands)
NICE Classes  ? 10 - Medical apparatus and instruments

Goods & Services

Medical apparatus, namely, infusion and injection devices for administering drugs

65.

Process for preparing ozanimod

      
Application Number 17311094
Grant Number 11390593
Status In Force
Filing Date 2019-12-05
First Publication Date 2021-11-25
Grant Date 2022-07-19
Owner Synthon B.V. (Netherlands)
Inventor
  • Buchlovic, Marian
  • Chalupova, Lenka
  • Vyklicky, Libor
  • Bartl, Jiri

Abstract

The presented invention relates to a process for preparation of compound of formula (1) or a salt thereof (i.e.) ozanimod: (1). The invention also relates to intermediates used in the process.

IPC Classes  ?

  • C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles
  • C07D 263/22 - Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms

66.

CRYSTALLINE FORM OF OZANIMOD HYDROCHLORIDE

      
Application Number EP2021056821
Publication Number 2021/197852
Status In Force
Filing Date 2021-03-17
Publication Date 2021-10-07
Owner SYNTHON B.V. (Netherlands)
Inventor Westheim, Raymond

Abstract

The presented invention relates to crystalline form, Form A of Ozanimod hydrochloride, processes for preparation thereof and pharmaceutical compositions comprising the Ozanimod hydrochloride Form A.

IPC Classes  ?

67.

PHARMACEUTICAL COMPOSITIONS COMPRISING ELAGOLIX SODIUM

      
Application Number EP2021056219
Publication Number 2021/180862
Status In Force
Filing Date 2021-03-11
Publication Date 2021-09-16
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Garcia Jimenez, Sonia
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to pharmaceutical compositions comprising a therapeutically effective dose of elagolix sodium and pharmaceutically acceptable excipients comprising a super disintegrant. The compositions can further comprise an alkalizer and/or a non-ionic surfactant.

IPC Classes  ?

68.

Process for making palbociclib

      
Application Number 17057425
Grant Number 11858928
Status In Force
Filing Date 2019-05-21
First Publication Date 2021-07-08
Grant Date 2024-01-02
Owner Synthon B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Smekal, Oldrich

Abstract

The present invention related to a process for preparation of compound of formula (1) or a salt thereof (i.e.) palbociclib: The invention also relates to a solid crystalline form of intermediate of formula (2) used in the process:

IPC Classes  ?

69.

Purification of sugammadex

      
Application Number 17045736
Grant Number 11225565
Status In Force
Filing Date 2019-04-08
First Publication Date 2021-06-17
Grant Date 2022-01-18
Owner Synthon B.V. (Netherlands)
Inventor
  • Buchlovic, Marian
  • Cernova, Lenka

Abstract

The invention deals with a novel process for purification of the pharmaceutically useful product sugammadex of formula (1).

IPC Classes  ?

  • C08L 5/16 - CyclodextrinDerivatives thereof

70.

PHARMACEUTICAL COMPOSITION COMPRISING ELTROMBOPAG BIS(MONOETHANOLAMINE)

      
Application Number EP2020084690
Publication Number 2021/110942
Status In Force
Filing Date 2020-12-04
Publication Date 2021-06-10
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a film-coated swallowable tablet comprising eltrombopag bis(monoethanolamine) and pharmaceutically acceptable excipients comprising maltose and isomalt as diluents. The invention further relates to the use of said tablet as a medicament, particularly in the treatment of immune thrombocytopenia (ITP), thrombocytopenia in patients with chronic hepatitis C virus (HCV) and severe aplastic anaemia (SAA).

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid

71.

PHARMACEUTICAL COMPOSITION COMPRISING ELTROMBOPAG BIS(MONOETHANOLAMINE)

      
Document Number 03160779
Status Pending
Filing Date 2020-12-04
Open to Public Date 2021-06-10
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a film-coated swallowable tablet comprising eltrombopag bis(monoethanolamine) and pharmaceutically acceptable excipients comprising calcium silicate as diluent. The invention further relates to the use of said tablet as a medicament, particularly in the treatment of immune thrombocytopenia (ITP), thrombocytopenia in patients with chronic hepatitis C virus (HCV) and severe aplastic anaemia (SAA).

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid

72.

CRYSTALLINE FORMS OF SODIUM SALT OF BEMPEDOIC ACID

      
Application Number EP2020084664
Publication Number 2021/110929
Status In Force
Filing Date 2020-12-04
Publication Date 2021-06-10
Owner SYNTHON B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

The presented invention relates to crystalline Forms (I) or (II) or (III) or (IV) of sodium salt of Bempedoic acid, processes for preparation thereof and a composition comprising it.

IPC Classes  ?

  • C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups
  • C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part

73.

PHARMACEUTICAL COMPOSITION COMPRISING ELTROMBOPAG BIS(MONOETHANOLAMINE)

      
Application Number EP2020084723
Publication Number 2021/110959
Status In Force
Filing Date 2020-12-04
Publication Date 2021-06-10
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a film-coated swallowable tablet comprising eltrombopag bis(monoethanolamine) and pharmaceutically acceptable excipients comprising calcium silicate as diluent. The invention further relates to the use of said tablet as a medicament, particularly in the treatment of immune thrombocytopenia (ITP), thrombocytopenia in patients with chronic hepatitis C virus (HCV) and severe aplastic anaemia (SAA).

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid

74.

PHARMACEUTICAL COMPOSITION COMPRISING ENZALUTAMIDE

      
Document Number 03152909
Status Pending
Filing Date 2020-10-01
Open to Public Date 2021-04-08
Owner SYNTHON BV (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising a granulate consisting of a co-precipitate on a substrate, wherein the co-precipitate comprises enzalutamide in amorphous form and a cellulosic concentration enhancing polymer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of castration-resistant prostate cancer.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

75.

PHARMACEUTICAL COMPOSITION COMPRISING ENZALUTAMIDE

      
Application Number EP2020077565
Publication Number 2021/064123
Status In Force
Filing Date 2020-10-01
Publication Date 2021-04-08
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising a granulate consisting of a co-precipitate on a substrate, wherein the co-precipitate comprises enzalutamide in amorphous form and a cellulosic concentration enhancing polymer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of castration-resistant prostate cancer.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

76.

CRYSTALLINE FORMS OF BEMPEDOIC ACID

      
Application Number EP2020077645
Publication Number 2021/064166
Status In Force
Filing Date 2020-10-02
Publication Date 2021-04-08
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Hegedus, Michal
  • Westheim, Raymond

Abstract

The presented invention relates to crystalline Form A and Form B of Bempedoic acid, a process for preparation thereof and a composition comprising the Form A or Form B.

IPC Classes  ?

  • C07C 51/43 - SeparationPurificationStabilisationUse of additives by change of the physical state, e.g. crystallisation
  • C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups

77.

SALTS OF OMECAMTIV MECARBIL AND SOLID FORMS THEREOF

      
Application Number EP2020076162
Publication Number 2021/053175
Status In Force
Filing Date 2020-09-18
Publication Date 2021-03-25
Owner SYNTHON B.V. (Netherlands)
Inventor Jelinkova, Katerina

Abstract

The presented invention relates to Omecamtiv mecarbil salts with methane sulfonic acid, benzene sulfonic acid and p-toluene sulfonic acid and to processes for preparation 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
  • A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins

78.

SALTS OF OMECAMTIV MECARBIL AND SOLID FORMS THEREOF

      
Application Number EP2020076180
Publication Number 2021/053189
Status In Force
Filing Date 2020-09-18
Publication Date 2021-03-25
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Jelinkova, Katerina
  • Hegedus, Michal

Abstract

The presented invention relates to Omecamtiv mecarbil salts, solid forms thereof and to processes for preparation 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
  • A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins

79.

ISAVUCONAZONIUM SALTS AND PROCESS FOR PREPARING THEREOF

      
Application Number EP2020072988
Publication Number 2021/037597
Status In Force
Filing Date 2020-08-17
Publication Date 2021-03-04
Owner SYNTHON B.V. (Netherlands)
Inventor Bartos, Petr

Abstract

The present invention relates to the process of preparation of salts of compound of formula (1).

IPC Classes  ?

  • A61P 31/10 - Antimycotics
  • 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 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

80.

CONTROLLED RELEASE TOFACITINIB COMPOSITIONS

      
Application Number EP2020074032
Publication Number 2021/038014
Status In Force
Filing Date 2020-08-27
Publication Date 2021-03-04
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Alvarez Fernandez, Lisardo
  • Nogueiras Nieto, Luis
  • Kumar, Rohit

Abstract

The present invention relates to a monolithic tablet composition for oral administration of tofacitinib, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/20 - Pills, lozenges or tablets

81.

Tablet compositions comprising abiraterone acetate

      
Application Number 17044698
Grant Number 11865215
Status In Force
Filing Date 2019-01-25
First Publication Date 2021-02-11
Grant Date 2024-01-09
Owner Synthon B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Gago Guillan, Manuel
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition for oral administration of abiraterone acetate, particularly to pharmaceutical granulates and tablets giving immediate release of abiraterone acetate in the stomach.

IPC Classes  ?

  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin

82.

IMPROVED PROCESS FOR PREPARING OZANIMOD

      
Application Number EP2020070188
Publication Number 2021/009306
Status In Force
Filing Date 2020-07-16
Publication Date 2021-01-21
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Chalupova, Lenka
  • Buchlovic, Marian

Abstract

The present invention relates to the process of preparation of compound of formula (I) or a salt thereof. Further it relates to the solid form of compound (I).

IPC Classes  ?

  • C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles

83.

PROCESS FOR PREPARATION OF ENZALUTAMIDE

      
Application Number EP2020067854
Publication Number 2020/260469
Status In Force
Filing Date 2020-06-25
Publication Date 2020-12-30
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Mitaš, Petr
  • Smekal, Oldrich

Abstract

The presented invention relates to a process for preparation of Enzalutamide, compound (1) or a salt or a solvate thereof Formula (1). The presented invention also related to 1,4-dioxane solvate of compound (1).

IPC Classes  ?

  • C07D 233/86 - Oxygen and sulfur atoms, e.g. thiohydantoin

84.

PROCESS FOR PREPARATION OF ENZALUTAMIDE

      
Document Number 03143111
Status Pending
Filing Date 2020-06-25
Open to Public Date 2020-12-30
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Smekal, Oldrich

Abstract

The presented invention relates to a process for preparation of Enzalutamide, compound (1) or a salt or a solvate thereof Formula (1). The presented invention also related to 1,4-dioxane solvate of compound (1).

IPC Classes  ?

  • C07D 233/86 - Oxygen and sulfur atoms, e.g. thiohydantoin

85.

SIPONIMOD MALEIC ACID AND FUMARIC ACID SALT

      
Application Number EP2020064211
Publication Number 2020/234423
Status In Force
Filing Date 2020-05-21
Publication Date 2020-11-26
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Partl, Jiri

Abstract

The presented invention relates to salts of Siponimod with Fumaric acid (1:1) and solid Forms 1 and 2 thereof. The presented invention further relates to salts of Siponimod with Maleic acid (1:1) and solid Forms 1, 2, 3, 4, 5, 6, 7, 8 and 9 thereof.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system

86.

PHARMACEUTICAL COMPOSITION COMPRISING AXITINIB

      
Application Number EP2020062840
Publication Number 2020/225413
Status In Force
Filing Date 2020-05-08
Publication Date 2020-11-12
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Kumar, Rohit
  • Alvarez Fernandez, Lisardo

Abstract

The present invention relates to an immediate release tablet composition comprising axitinib form IV characterized by an XRPD pattern comprising the peaks at about 8.9, 12.0, 14.6, 15.2, 15.7, 17.8, 19.1, 20.6, 21.6, 23.2, 24.2, 24.9, 26.1 and 27.5 ± 0.1 degrees 2θ, when measured with Cu Kα1 radiation and one or more pharmaceutically acceptable excipients, wherein the composition exhibits a dissolution rate between 40% and 70% in 30 minutes when tested in 900 ml 0.01 N hydrochloric acid pH 2.0 at 37ºC, 75 rpm in a USP apparatus II.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • 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

87.

PHARMACEUTICAL COMPOSITION COMPRISING AMORPHOUS SUNITINIB

      
Application Number EP2019060682
Publication Number 2020/216450
Status In Force
Filing Date 2019-04-25
Publication Date 2020-10-29
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Garcia Jimenez, Sonia
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a pharmaceutical composition comprising a solid dispersion of sunitinib L-malate and polyvinylpyrrolidone in a primary packaging comprising means to absorb water. The invention further relates to the use of said composition as a medicament, particularly in the treatment of a tyrosine kinase-related disorder.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61J 1/00 - Containers specially adapted for medical or pharmaceutical purposes

88.

PROCESS FOR PREPARING AXITINIB, PROCESS FOR PURIFYING THE INTERMEDIATE 2-((3-IODO-1H-INDAZOL-6-YL)THIO)-N-METHYLBENZAMIDE, PROCESS FOR PURIFYING AXITINIB VIA THE AXITINIB HCL SALT, SOLID FORM OF THE AXITINIB HCL SALT

      
Application Number EP2020060193
Publication Number 2020/212253
Status In Force
Filing Date 2020-04-09
Publication Date 2020-10-22
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Castulik, Jakub
  • Skoumal, Radomir

Abstract

1) A process for preparing Axitinib ( N-methyl-2-({3-[(E)-2-pyridin-2- ylethenyl]-lH-indazol-6-yl}sulfanyl)benzamide; compound of formula (l)) 2) A process for purifying the intermediate 2-((3-iodo-lH-indazol-6- yl)thio)-N-methylbenzamide (compound of formula (lla)) 3) A process for purifying Axitinib using the Axitinib HCI salt (compound of formula (VIII)) as an intermediate 4) A solid form of the Axitinib HCI salt (form J) characterized by an XRPD pattern

IPC Classes  ?

  • 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 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
  • 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
  • A61P 35/00 - Antineoplastic agents

89.

SOLID FORMS OF SIPONIMOD

      
Application Number EP2020060213
Publication Number 2020/208167
Status In Force
Filing Date 2020-04-09
Publication Date 2020-10-15
Owner SYNTHON B.V. (Netherlands)
Inventor Dymacek, Bohumil

Abstract

The present invention relates to solid Form 1, Form 2, Form 3 and Form 6 of the compound Siponimod and processes for preparation thereof. The present invention further relates to processes for preparation of solid Form A of the compound Siponimod.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

90.

PROCESS FOR MAKING SIPONIMOD AND INTERMEDIATE THEREOF

      
Application Number EP2020058884
Publication Number 2020/201172
Status In Force
Filing Date 2020-03-29
Publication Date 2020-10-08
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Keltjens, Rolf
  • Hylse, Ondrej
  • Partl, Jiri

Abstract

The presented invention relates to a process for preparation of compound of formula (I) or a salt or a solvate thereof (i.e.) siponimod. The invention also relates to intermediates used in the process and solid forms of these intermediates.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

91.

Process for making sugammadex

      
Application Number 16624708
Grant Number 10919988
Status In Force
Filing Date 2018-06-29
First Publication Date 2020-07-09
Grant Date 2021-02-16
Owner Synthon B.V. (Netherlands)
Inventor
  • Buchlovic, Marian
  • Cernova, Lenka

Abstract

The invention deals with a novel process for making intermediates of the pharmaceutically useful product Sugammadex of formula (1).

IPC Classes  ?

  • C08B 37/16 - CyclodextrinDerivatives thereof
  • C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof

92.

PHARMACEUTICAL COMPOSITION COMPRISING IBRUTINIB

      
Application Number EP2019086585
Publication Number 2020/127912
Status In Force
Filing Date 2019-12-20
Publication Date 2020-06-25
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit
  • Vivancos Martinez, Marta

Abstract

The present invention relates to a tablet composition comprising ibrutinib and one or more pharmaceutically acceptable excipients, characterized in that: • Ibrutinib is form C, having characteristic peaks in the X-ray powder diffraction pattern at the following 2 theta (±0.2) angles: 6.9º, 18.2º, 19.2º, 19.6º and 23.0º, measured using a Cu Kα radiation; and • Ibrutinib form C is present in an amount from 60 to 80% w/w relative to the total weight of the tablet; and • The composition is free of surfactant; and • The composition exhibits a dissolution rate of at least 65% in 20 minutes when tested in 900 ml 0.01 N hydrochloric acid pH 2.0 (+1% Tween 20) at 37ºC, 75 rpm and/or in 900 ml phosphate buffer pH 6.8 (+3% Tween 20) at 37ºC, 75 rpm in a USP apparatus II. The invention further relates to the use of said composition as a medicament, particularly in the treatment of chronic lymphocytic leukaemia (CLL), mantle cell lymphoma (MCL) and Waldenstrӧm's macroglobulinaemia (WM).

IPC Classes  ?

  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/50 - Microcapsules
  • A61K 47/38 - CelluloseDerivatives thereof
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 35/00 - Antineoplastic agents

93.

Pharmaceutical composition comprising ibrutinib

      
Application Number 16229282
Grant Number 10688050
Status In Force
Filing Date 2018-12-21
First Publication Date 2020-06-23
Grant Date 2020-06-23
Owner Synthon B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

the composition exhibits a dissolution rate of at least 65% in 20 minutes when tested in 900 ml 0.01 N hydrochloric acid pH 2.0 (+1% Tween 20) at 37° C., 75 rpm and/or in 900 ml phosphate buffer pH 6.8 (+3% Tween 20) at 37° C., 75 rpm in a USP apparatus II. The invention further relates to the use of said composition as a medicament, particularly in the treatment of chronic lymphocytic leukaemia (CLL), mantle cell lymphoma (MCL) and Waldenström's macroglobulinaemia (WM).

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61P 35/02 - Antineoplastic agents specific for leukemia
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

94.

Pharmaceutical composition comprising Lenvatinib mesylate

      
Application Number 16603031
Grant Number 11911509
Status In Force
Filing Date 2018-04-04
First Publication Date 2020-06-18
Grant Date 2024-02-27
Owner Synthon B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Velada Calzada, Jose
  • Kumar, Rohit

Abstract

The present invention relates to a pharmaceutical composition comprising a therapeutically effective dose of Lenvatinib mesylate having sodium wherein the weight ratio of Lenvatinib mesylate to sodium carbonates ranges from 1:1.5 to 1:5.

IPC Classes  ?

  • A61K 31/47 - QuinolinesIsoquinolines
  • A61K 47/02 - Inorganic compounds
  • A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
  • A61K 47/38 - CelluloseDerivatives thereof
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/00 - Medicinal preparations characterised by special physical form

95.

IMPROVED PROCESS FOR PREPARING OZANIMOD

      
Application Number EP2019083801
Publication Number 2020/115200
Status In Force
Filing Date 2019-12-05
Publication Date 2020-06-11
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Buchlovic, Marian
  • Chalupova, Lenka
  • Vyklicky, Libor
  • Bartl, Jiri

Abstract

The presented invention relates to a process for preparation of compound of formula (1) or a salt thereof (i.e.) ozanimod : (1). The invention also relates to intermediates used in the process.

IPC Classes  ?

96.

Pharmaceutical composition comprising Palbociclib

      
Application Number 16633339
Grant Number 11529353
Status In Force
Filing Date 2018-07-25
First Publication Date 2020-05-14
Grant Date 2022-12-20
Owner Synthon B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit
  • Velada Calzada, Jose

Abstract

The present invention relates to a pharmaceutical granulate composition comprising Palbociclib free base, having improved bioavailability.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets

97.

CRYSTALLINE FORMS AND PROCESSES OF LENVATINIB BESYLATE

      
Document Number 03113549
Status Pending
Filing Date 2019-10-01
Open to Public Date 2020-04-09
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Westheim, Raymond
  • Jelinkova, Katerina

Abstract

The present invention relates to lenvatinib besylate, its crystalline forms and processes for making them. Furthermore, to a pharmaceutical composition comprising a therapeutically effective dose of lenvatinib besylate.

IPC Classes  ?

98.

CRYSTALLINE FORMS AND PROCESSES OF LENVATINIB BESYLATE

      
Application Number EP2019076622
Publication Number 2020/070144
Status In Force
Filing Date 2019-10-01
Publication Date 2020-04-09
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Westheim, Raymond
  • Jelinkova, Katerina

Abstract

The present invention relates to lenvatinib besylate, its crystalline forms and processes for making them. Furthermore, to a pharmaceutical composition comprising a therapeutically effective dose of lenvatinib besylate.

IPC Classes  ?

99.

PHARMACEUTICAL COMPOSITION COMPRISING LENVATINIB ESYLATE OR TOSYLATE

      
Application Number EP2019076625
Publication Number 2020/070147
Status In Force
Filing Date 2019-10-01
Publication Date 2020-04-09
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo

Abstract

The present invention relates to a pharmaceutical composition comprising a therapeutically effective dose of lenvatinib esylate or tosylate having sodium wherein the weight ratio of lenvatinib esylate or tosylate to sodium carbonates ranges from 1:.5 to 1:10.

IPC Classes  ?

100.

CONTROLLED RELEASE TOFACITINIB COMPOSITIONS

      
Application Number EP2019062390
Publication Number 2019/224058
Status In Force
Filing Date 2019-05-14
Publication Date 2019-11-28
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet into tablet composition for oral administration of tofacitinib, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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