Abstract

A compound of formula (I) A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m=0 then R3 is in position 2′, and if m=1 then R3 is on position 1′); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl, R2 is hydrogen or (C3-6)cycloalkyl, or unsubstituted (C1-6)alkyl, or (C1-6)alkyl substituted by one or more of hydroxy; preferably one or two, methoxy, halogen, and (C3-6)cycloalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatom e. g. selected from N or O, or R1 is hydroxy and R2 is formyl; R3 is OH, OR4, a halogen atom, or R3 is bound to 2′ and represents —O—(CH2)p—O— with p is 2 or 3; R4 is unsubstituted (C1-6)alkyl or (C3-6)cycloalkyl, or a pharmaceutically acceptable salt, solvate, prodrug or metabolite thereof for the specific use in the treatment or prevention of a bacterial infection mediated by spirochetes.

IPC Classes  ?

• A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• A61P 31/04 - Antibacterial agents

Abstract

The present invention relates to an injectable pharmaceutical formulation comprising a compound of formula (I) The present invention relates to an injectable pharmaceutical formulation comprising a compound of formula (I) The present invention relates to an injectable pharmaceutical formulation comprising a compound of formula (I) said formulation being buffered to a pharmaceutically acceptable pH-value, especially a pH-value of from 2 to 6, in particular a pH value of from 3 to 5.5, preferred a pH-value of about 4 to 5, particularly preferred about 5.

IPC Classes  ?

• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/08 - Solutions
• A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• 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

Abstract

A compound of formula (I) A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m=0 then R3 is in position 2′, and if m=1 then R3 is on position 1′); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl, R2 is hydrogen or (C3-6)cycloalkyl, or unsubstituted (C1-6)alkyl, or (C1-6)alkyl substituted by one or more of hydroxy; preferably one or two, methoxy, halogen, (C3-6)cycloalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatom e. g. selected from N or O, or R1 is hydroxy and R2 is formyl; R3 is OH, OR4, a halogen atom, or R3 is bound to 2′ and represents —O—(CH2)p—O— with p is 2 or 3; R4 is unsubstituted (C1-6)alkyl or (C3-6)cycloalkyl, or a pharmaceutically acceptable salt, solvate, prodrug or metabolite thereof for the specific use in the treatment or prevention of a disease mediated by a virus.

IPC Classes  ?

• A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

A compound of formula (I) A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m=0 then R3 is in position 2′, and if m=1 then R3 is on position 1′); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl, R2 is hydrogen or (C3-6)cycloalkyl, or unsubstituted (C1-6)alkyl, or (C1-6)alkyl substituted by one or more of hydroxy; preferably one or two, methoxy, halogen, (C3-6)cycloalkyl, or A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m=0 then R3 is in position 2′, and if m=1 then R3 is on position 1′); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl, R2 is hydrogen or (C3-6)cycloalkyl, or unsubstituted (C1-6)alkyl, or (C1-6)alkyl substituted by one or more of hydroxy; preferably one or two, methoxy, halogen, (C3-6)cycloalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatom e. g. selected from N or O, or R1 is hydroxy and R2 is formyl; R3 is OH, OR4, a halogen atom, or R3 is bound to 2′ and represents —O—(CH2)p—O— with p is 2 or 3; R4 is unsubstituted (C1-6)alkyl or (C3-6)cycloalkyl, or a pharmaceutically acceptable salt, solvate, prodrug or metabolite thereof A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m=0 then R3 is in position 2′, and if m=1 then R3 is on position 1′); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl, R2 is hydrogen or (C3-6)cycloalkyl, or unsubstituted (C1-6)alkyl, or (C1-6)alkyl substituted by one or more of hydroxy; preferably one or two, methoxy, halogen, (C3-6)cycloalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatom e. g. selected from N or O, or R1 is hydroxy and R2 is formyl; R3 is OH, OR4, a halogen atom, or R3 is bound to 2′ and represents —O—(CH2)p—O— with p is 2 or 3; R4 is unsubstituted (C1-6)alkyl or (C3-6)cycloalkyl, or a pharmaceutically acceptable salt, solvate, prodrug or metabolite thereof for the specific use in the treatment or prevention of an inflammatory disease which is not mediated by bacteria.

IPC Classes  ?

• C07C 321/16 - Sulfides, hydropolysulfides, or polysulfides having thio groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention is directed to compositions and methods for stabilizing a protein without a surfactant. The present invention is further directed to compositions comprising a protein and at least one excipient selected from the group consisting of hindered amines, anionic aromatics, functionalized amino acids, oligopeptides, low molecular weight aliphatic polyacids, zwitterions, phospholipids, cyclodextrins, polyethylene glycols, gelatins, urea, ethanol, glycerin, dextran, xanthan gum, 2-(2-ethoxyethoxy)ethanol, hydroxypropyl cellulose, propylene glycol, a short-chain organic acid, deoxycholate, sodium nitrate, sodium sulfate, proline and lysine.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 47/40 - CyclodextrinsDerivatives thereof
• A61K 47/42 - ProteinsPolypeptidesDegradation products thereofDerivatives thereof, e.g. albumin, gelatin or zein
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61K 47/02 - Inorganic compounds
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof

Abstract

The present invention provides methods and compositions for making proteins, preferably antibodies, more preferably anti-tumor necrosis factor alpha antibodies, and most preferably adalimumab. The present invention further provides methods and compositions for mammalian cell culture, preferably Chinese Hamster Ovary cells.

IPC Classes  ?

• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• C12N 5/02 - Propagation of single cells or cells in suspensionMaintenance thereofCulture media therefor
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C12N 5/00 - Undifferentiated human, animal or plant cells, e.g. cell linesTissuesCultivation or maintenance thereofCulture media therefor
• C12P 21/00 - Preparation of peptides or proteins

Abstract

Provided herein are methods of producing a recombinant protein that include fed-batch culturing a mammalian cell.

IPC Classes  ?

• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• C12N 5/071 - Vertebrate cells or tissues, e.g. human cells or tissues

Abstract

The present invention is directed to methods for filling a container wherein the filled container has no headspace. The present invention is further directed to methods for stabilizing an aqueous drug substance solution by filling a container with the aqueous drug substance solution wherein the filled container has no headspace. The present invention is further directed to methods for detecting headspace in a container.

IPC Classes  ?

• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 9/08 - Solutions
• B65B 31/00 - Packaging articles or materials under special atmospheric or gaseous conditionsAdding propellants to aerosol containers
• B65B 7/28 - Closing semi-rigid or rigid containers or receptacles not deformed by, or not taking-up shape of, contents, e.g. boxes or cartons by applying separate preformed closures, e.g. lids, covers
• B65B 3/00 - Packaging plastic material, semiliquids, liquids or mixed solids and liquids, in individual containers or receptacles, e.g. bags, sacks, boxes, cartons, cans or jars
• A61K 47/02 - Inorganic compounds
• A61J 1/06 - Ampoules or cartridges
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The present invention relates to aqueous pharmaceutical compositions comprising a high concentration (i.e., greater than 50 milligrams per milliliter) of adalimumab (including antibody proteins considered or intended as “biosimilar” or “bio-better” variants of commercially available adalimumab) suitable for long-term storage, and methods of manufacture of the compositions; methods of their administration; and articles containing the same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons

Goods & Services

pharmaceutical preparations for the treatment of autoimmune diseases

Abstract

The present invention relates to purification methods of pleuromutilin (I) by means of crystallisation and/or recrystallisation. The process according to the present invention is carried out in the presence of i-propylacetate.

IPC Classes  ?

• C07C 67/52 - SeparationPurificationStabilisationUse of additives by change in the physical state, e.g. crystallisation
• C07C 69/013 - Esters of alcohols having the esterified hydroxy group bound to a carbon atom of a ring other than a six-membered aromatic ring

Abstract

The present invention provides methods and compositions for making proteins, preferably antibodies, more preferably anti-tumor necrosis factor alpha antibodies, and most preferably adalimumab. The present invention further provides methods and compositions for mammalian cell culture, preferably Chinese Hamster Ovary cells.

IPC Classes  ?

• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• C12P 21/08 - Monoclonal antibodies
• C12P 21/00 - Preparation of peptides or proteins
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• C12N 5/00 - Undifferentiated human, animal or plant cells, e.g. cell linesTissuesCultivation or maintenance thereofCulture media therefor
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum

Abstract

The present invention relates to an injectable pharmaceutical formulation comprising a compound of formula (I) the formulation being buffered to a pharmaceutically acceptable pH-value, especially a pH-value of from 2 to 6, in particular a pH value of from 3 to 5.5, preferred a pH-value of about 4 to 5, particularly preferred about 5.

IPC Classes  ?

• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/08 - Solutions
• A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• 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

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The present invention is directed to methods for filling a container wherein the filled container has no headspace. The present invention is further directed to methods for stabilizing an aqueous drug substance solution by filling a container with the aqueous drug substance solution wherein the filled container has no headspace. The present invention is further directed to methods for detecting headspace in a container.

IPC Classes  ?

• B65B 31/00 - Packaging articles or materials under special atmospheric or gaseous conditionsAdding propellants to aerosol containers
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 9/08 - Solutions
• B65B 7/28 - Closing semi-rigid or rigid containers or receptacles not deformed by, or not taking-up shape of, contents, e.g. boxes or cartons by applying separate preformed closures, e.g. lids, covers
• B65B 3/00 - Packaging plastic material, semiliquids, liquids or mixed solids and liquids, in individual containers or receptacles, e.g. bags, sacks, boxes, cartons, cans or jars
• A61K 47/02 - Inorganic compounds
• A61J 1/06 - Ampoules or cartridges
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides aqueous pharmaceutical adalimumab compositions suitable for long-term storage of adalimumab, methods of manufacture of these compositions, methods of administration, and kits containing same.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/08 - Solutions
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.

IPC Classes  ?

• C07C 323/52 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
• A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61K 31/235 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

Process for the preparation of a compound of formula I in the form of a single stereoisomer in crystalline form, comprising deprotecting the amine group in a compound of formula IIa or in a mixture of a compound of formula IIa with a compound of formula IIb and isolating a compound of formula I from the reaction mixture; compounds and salts of compounds of formula I in crystalline form; pharmaceutical compositions comprising such salts; processes for the preparation of intermediates and intermediates in a process for the preparation of a compound of formula I.

IPC Classes  ?

• C07C 205/00 - Compounds containing nitro groups bound to a carbon skeleton
• C07C 229/00 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton
• C07C 319/20 - Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides by reactions not involving the formation of sulfide groups
• A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• C07C 53/10 - Salts thereof
• C07C 57/145 - Maleic acid
• C07C 59/08 - Lactic acid
• C07C 319/14 - Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
• C07C 323/41 - Y being a hydrogen or an acyclic carbon atom
• C07C 323/43 - Y being a hetero atom
• C07C 323/52 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
• A01N 37/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
• A61K 31/21 - Esters, e.g. nitroglycerine, selenocyanates

Abstract

A compound of formula wherein PROT is an amine protecting group and PROT′ is hydrogen; or PROT and PROT′ together with the nitrogen atom to which they are attached form a heterocyclic ring as an amine protecting group, and PROT″ is a thiol protecting group, processes for its production, intermediates in their production and production of intermediates in stereoisomerically pure form, and their use for the production of pharmaceutically active compounds.

IPC Classes  ?

• C07C 321/00 - Thiols, sulfides, hydropolysulfides or polysulfides
• C07C 271/24 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07C 61/22 - Unsaturated compounds having a carboxyl group bound to a six-membered ring
• C07C 211/40 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing only non-condensed rings
• C07C 247/22 - Compounds containing azido groups with azido groups acylated by carboxylic acids with the acylating carboxyl groups bound to hydrogen atoms, to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
• C07C 265/10 - Derivatives of isocyanic acid having isocyanate groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 323/41 - Y being a hydrogen or an acyclic carbon atom
• C07C 323/43 - Y being a hetero atom
• C07C 327/30 - Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
• C07D 303/36 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
• C07C 231/14 - Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
• C07C 233/63 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings 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
• C07C 269/04 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
• C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups

Abstract

A process for the preparation of 14-O—[(N-(3-methyl-2-amino-butyryl-piperidinyl)sulfanyl)acetyl]mutilins of formula feasible for large-scale production of high purity products, and wherein the carbon atom at the piperidine ring attached to the sulphur atom is either in the (S)-configuration or in the (R)-configuration, and a new crystalline form of 14-O—[(N-3-methyl-2-(R)-amino-butyryl-piperidine-3(S)-yl)sulfanyl)acetyl]mutilin-hydrochloride.

IPC Classes  ?

• C07D 211/40 - Oxygen atoms

Abstract

Disclosed are pleuromutilin derivatives of formula (I) and their use in the treatment of diseases mediated by microbes.

IPC Classes  ?

• A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• C07C 323/00 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups

Abstract

Compounds of formula (I), which are 14-O-{[(optionally substituted hydroxy)cyclohexyl)sulfanyl]acetyl}mutilins further substituted at the cyclohexyl group by an acylated amino group, salts and solvates thereof, pharmaceutical compositions comprising such compounds and their use as a pharmaceutical, e.g. for the treatment of diseases mediated by microbes and for the treatment of inflammation where microbes are mediating said inflammation.

IPC Classes  ?

• C07C 205/00 - Compounds containing nitro groups bound to a carbon skeleton
• A01N 37/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids

Abstract

3 are hydrogen.

IPC Classes  ?

• C07C 69/712 - Ethers the hydroxy group of the ester being etherified with a hydroxy compound having the hydroxy group bound to a carbon atom of a six-membered aromatic ring
• C07C 323/52 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
• C07C 71/00 - Esters of oxyacids of halogens
• A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate

Abstract

A pleuromutilin derivative compound of general formula (I)

IPC Classes  ?

• A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• C07C 323/00 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups

Abstract

8 are hydrogen, halogen or deuterium; m is a number selected from 0 to 4, n is a number selected from 0 to 10, and p is a number selected from 0 to 10; with the proviso that n plus p are at least 1. These Compounds are usefül as pharmaceuticals, particularly as antimicrobials.

IPC Classes  ?

• A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• C07C 69/74 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring

Abstract

A process for the preparation of 14-O-[(N-(3-methyl-2-amino-butyryl-piperidinyl)sulfanyl) acetyl]mutilins of formula (I) feasible for large-scale production of high purity products, and wherein the carbon atom at the piperidine ring attached to the sulphur atom is either in the (S)-configuration or in the (R)-configuration, and a new crystalline form of 14-O-[(N-3-methyl-2-(R)-amino-butyryl-piperidine-3(S)-yl)sulfanyl)acetyl]mutilin-hydrochloride.

IPC Classes  ?

• C07D 211/40 - Oxygen atoms