05 - Pharmaceutical, veterinary and sanitary products
16 - Paper, cardboard and goods made from these materials
Goods & Services
Pharmaceutical preparations and substances, all for human use. Paper, cardboard; printed matter; publications; books, brochures, catalogues, journals, magazines, manuals, pamphlets, handbooks, trade and technical publications; photographs; stationery; paperweights; greeting cards and postcards; letter openers; document files and folders; notepads and message pads; plastic materials for packaging (not included in other classes); packaging materials and packaging products made of plastic film, plastic film laminates, plastics, paper, card and cardboard; packing paper and tissue; boxes and containers of paper, card and cardboard; printed advertising, promotional and publicity materials; calendars; charts; diagrams; diaries; printed forms; graphic prints, representations and reproductions; posters; writing pads and paper; parts and fittings for all the aforesaid goods.
The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
The present invention relates to a novel form of anhydrous tiotropium bromide, processes for the preparation of anhydrous tiotropium bromide, pharmaceutical compositions comprising anhydrous tiotropium bromide and uses of the compositions.
The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient vorinostat. In particular it relates to a process for preparing vorinostat substantially free from impurities.
A01N 37/28 - 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 containing the group —CO—N, e.g. carboxylic acid amides or imidesThio-analogues thereof containing the group Thio-analogues thereof
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
C07D 401/00 - 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
The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to an improved process for the preparation of Letrozole (I) and its synthetic intermediate 4-[(1-(1,2,4-triazolyl)methyl]benzonitrile (III). In particular, it relates to a process to prepare Letrozole and its intermediate (III) substantially free from regioisomeric impurities. The present invention further relates to acid addition salts of 4-[(1-(1,2,4-triazolyl)methyl]benzonitrile (III) such as the oxalate salt, and also to Letrozole (I), the intermediate (III) and salts thereof preparable by the processes of the present invention.
The present invention relates to crystalline forms of thalidomide having a high polymorphic purity and to processes for their preparation. The present invention also relates to pharmaceutical preparations comprising the crystalline forms for the treatment of patients suffering from autoimmune, inflammatory or angiogenic disorders.
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 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
The present invention relates to the active pharmaceutical ingredient dipyridamole. In particular, it relates to efficient processes for the preparation of dipyridamole which are amenable to large scale commercial production and provide the required product with improved yield and purity. The present invention also relates to a novel crystallization method for the purification of dipyridamole.
The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient vorinostat. In particular it relates to a process for preparing vorinostat substantially free from impurities, involving suberic acid, aniline and hydroxylamine as starting materials.
A01N 37/28 - 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 containing the group —CO—N, e.g. carboxylic acid amides or imidesThio-analogues thereof containing the group Thio-analogues thereof
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
The present invention relates to novel processes tor the preparation of sunitinib and salts thereof, in particular sunitinib (2S)-2-hvdroxybutanedioate. The invention further relates to novel intermediates, their use in the preparation of sunitinib or salts thereof and to processes for the preparation of said intermediates. The invention also relates to compositions comprising sunitinib or its pharmaceutically acceptable salts.Formula (IV).
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
13.
PROCESS FOR THE PREPARATION OF SUNITINIB MALATE FORM I
The present invention relates to an improved process for preparing acid addition salts of sunitinib, in particular sunitinib (2S)-2-hydroxybutanedioate (I). The invention also relates to compositions comprising sunitinib acid addition salts such as sunitinib (2S)-2- hydroxybutanedioate (I) and to the use of said compositions in the treatment of disease.
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
The present invention relates a one step process for the preparation of capecitabine and analogues thereof, such as galocitabine, sapacitabine, 5'-deoxy-5-fiuoro-N- [(cyclohexyloxy)carbonyl]cytidine, and N-[(heptyloxy)carbonyl]cytarabine.
The present invention relates to a new HPLC method for the analysis of the drug substance tiotropium and related substances. In particular, the present invention relates to a new HPLC method for the analysis of the salt tiotropium bromide and related substances. In a first method the mobile phase comprises two or more liquids and the relative concentration of the liquids is varied to a predetermined gradient. In a second method the mobile phase comprises a phosphate salt, a dihydrogen phosphate salt, a phosphoric acid, or a mixture thereof. A third method comprises the detection and optional quantification of methyl-di-2-thienyl glycolate. The present invention also relates to tiotropium and associated pharmaceutical compositions from which samples have been analysed by the methods of the invention and/or which are substantially free of specific impurities.
The present invention relates to a new HPLC method for the analysis of the drug substance sunitinib and related substances. In particular, the present invention relates to a new HPLC method for the analysis of the salt sunitinib malate and related substances. In a first method the mobile phase comprises two or more liquids and the relative concentration of the liquids is varied to a predetermined gradient. In a second method the mobile phase comprises an alcohol. In a third method the mobile phase comprises acetic acid. A fourth method comprises the detection and optional quantification of 5-fluoro-2,3-dihydro-1H- indole-2-one and/or N-[2-(diethylamino)ethyl]-2,4-dimethyl-5-formyl-lH-pyriOle-3- carboxamide. The present invention also relates to sunitinib and associated pharmaceutical compositions from which samples have been analysed by the methods of the invention and/ or which are substantially free of specific impurities.
G01N 30/34 - Control of physical parameters of the fluid carrier of fluid composition, e.g. gradient
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
The present invention relates to a new HPLC method for the analysis of the drug substance frovatriptan and related substances. In particular, the present invention relates to a new HPLC method for the analysis of the drug substance frovatriptan monosuccinate monohydrate and related substances. In a first method the mobile phase comprises two or more liquids and the relative concentration of the liquids is varied to a predetermined gradient. In other methods the stationary phase is reverse phase and the mobile phase comprises an alcohol and/or an alkylamine. In yet another method the mobile phase comprises a formate salt. A final method comprises the detection and optional quantification of specific impurities. The present invention also relates to frovatriptan and associated pharmaceutical compositions from which samples have been analysed by the methods of the invention and/ or which are substantially free of specific impurities.
G01N 30/34 - Control of physical parameters of the fluid carrier of fluid composition, e.g. gradient
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
The present invention relates to a novel polymorph of 4-methyl-N-[3-(4-methyl-imidazol- 1-yl)-5-(trifluoromethyl)-phenyl]-3-[(4-pyridin-3-yl-pyrimidin-2-yl)amino] benzamide (nilotinib) monohydrochloride monohydrate, and to methods for preparing, pharmaceutical compositions comprising, and methods of treatment using said polymorph.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 35/02 - Antineoplastic agents specific for leukemia
The present invention relates to novel intermediates and to an improved process for the preparation of N- functionalised cytidine derivatives such as capecitabine, galocitabine and sapacitabine. Said intermediates are se from a copound of formula (A- 2), (A-3), (A-6), (A-7). wherein: R1 and R3 arc each independendy selected from hydrogen, -F, -CI, -Br, -I, -CN, -NO2, -N3, -O-R7, -S-R7, -N(R7)2, -N(R7)3+ or -0-Si(R7)3; R4 and R5 arc each independendy selected from hydrogen, -F, -CI, -Br and -I; R6 is selected from an alkyl, alkenyl, alkynyl, atyl, aiylalkyl, arylalkenyl, arylalkynyl, alkylaiyl, alkenylaryl or alkynylaryl group, each of which may optionally be substituted, and each of which may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and each R7 is independendy selected from hydrogen, or an alkyl, alkenyl, alkynyl, atyl, aiylalkyl, arylalkenyl, arylalkynyl, alkylaiyl, alkenylaryl or alkynylaryl group, each of which may optionally he substituted, and each of which may optionally include one or more heteroatoms N, O or S in its carbon skeleton, and wherein any two or more R7 groups may, together with rhe atom or atoms to which they are attached, form a cyclic alkyl, alkenyl, alkynyl, aryl, aiylalkyl, arylalkcnyl, arylalkynyl, alkylaiyl, alkenylaryl or alkynylaryl group, each of which may optionally be substituted, and each of which may optionally include one or more heteroatoms N, O or S in its carbon skeleton.
The present invention relates to new HPLC methods for the analysis of the drug substance lenaliclomide and related substances. In a first method the mobile phase comprises two or mote liquids and the relative concentration of the liquids is varied to a predetermined gradient. In a second method the mobile phase comprises formic acid, a formate salt or a mixture thereof. The current invention also relates to lenalidomide and associated pharmaceutical compositions that have been analysed by the methods of the current invention and/or are substantially free of specific impurities.
G01N 30/36 - Control of physical parameters of the fluid carrier in high pressure liquid systems
G01N 30/34 - Control of physical parameters of the fluid carrier of fluid composition, e.g. gradient
G01N 30/96 - Investigating or analysing materials by separation into components using adsorption, absorption or similar phenomena or using ion-exchange, e.g. chromatography using ion-exchange
A61K 31/00 - Medicinal preparations containing organic active ingredients
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
The current invention relates to new HPLC methods for the analysis of the drug substance vorinostat and related substances. In a first method the mobile phase comprises two or more liquids and the relative concentration of the liquids is varied to a predetermined gradient. In a second method the mobile phase comprises an alcohol. In a third method the mobile phase comprises a phosphate salt, a phosphoric acid or an anhydride thereof. The current invention also relates to a method for analysing a substance, comprising the detection and optional quantification of one or more specific impurities. The current invention further relates to the use of specific substances as reference standards and markers, and to vorinostat and associated pharmaceutical compositions that have been analysed by the methods of the current invention and/or are substantially free of specific impurities.
The present invention relates to nilotinib dihydrochloride and its hydrates, to methods for preparing nilotinib dihydrochloride and its hydrates, pharmaceutical compositions comprising nilotinib dihydrochloride and its hydrates, and methods of treatment using the same.
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
Novel Anhydrate The present invention relates to a novel form of anhydrous tiotropium bromide, processes for the preparation of anhydrous tiotropium bromide, pharmaceutical compositions comprising anhydrous tiotropium bromide and uses of the compositions.
C07D 451/10 - Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61P 11/00 - Drugs for disorders of the respiratory system
24.
DICHLOROMETHANE SOLVATE OF TIOTROPIUM BROMIDE AND ITS USE
The present invention relates to a novel solvate of tiotropiumbromide, a process to prepare this solvate and the use of this and other solvates in processes for the preparation of anhydrous tiotropium bromide. The present invention also relates to pharmaceutical compositions comprising anhydrous tiotropium bromide and uses of the compositions.
The present invention relates to novel processes for the preparation of scopine esters and their quaternary salts. In particular, the present invention relates to a process for the preparation of tiotropium bromide, pharmaceutical compositions comprising tiotropium bromide and the use of such compositions in the treatment of respiratory disorders.
The present invention relates to pharmaceutical compositions and in particular to suspension aerosol pharmaceutical compositions, processes to obtain them and their use in inhalation therapy.
The present invention relates to novel salts of pyrrole derivatives, their preparation and their use in the preparation of sunitinib salts, in particular sunitinib malate (IIa), and sunitinib base. The invention also relates to compositions comprising sunitinib salts or sunitinib base and the use of these compositions in the treatment of cancer.
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
The present invention relates to an improved process for the preparation of letrozole (I) and its pharmaceutically acceptable salts, to compositions comprising letrozole or a pharmaceutically acceptable salt thereof, and to uses of such compositions. In particular it relates to a process and to novel intermediates for preparing letrozole and its salts substantially free from regioisomeric impurities.
The present invention relates to intermediates and their preparation, for use in the manufacture of pure dasatinib, in particularly dasatinib monohydrate and anhydrous dasatinib. The invention also relates to pharmaceutical compositions comprising pure dasatinib and their use in the treatment of cancer.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to processes for the preparation of crystalline N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5- thiazolecarboxamide (dasatinib) monohydrate. The invention further relates to pure polymorphs, to pharmaceutical compositions comprising said polymorphs and to uses thereof.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to processes for the preparation of dasatinib and to crystalline monohydrate and anhydrous polymorphic forms of dasatinib. The invention further relates to pure polymorphs, to pharmaceutical compositions comprising said polymorphs and to uses thereof.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to novel processes for the preparation of enantiomerically enriched β -amino acid derivatives such as β -amino esters useful for the synthesis of enantiomerically enriched biologically active molecules such as sitagliptin. The key step involves the resolution of the racemate with mandelic acid.
C07C 227/16 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
C07C 227/34 - Preparation of optical isomers by separation of optical isomers
C07C 229/34 - 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 containing six-membered aromatic rings
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
33.
NOVEL CRYSTALLINE POLYMORPH OF SITAGLIPTIN DIHYDROGEN PHOSPHATE
The present invention relates to a novel anhydrous crystalline form of sitagliptin dihydrogenphosphate (I), to processes for its preparation and to its use in pharmaceutical compositions.
The present invention relates to the active pharmaceutical ingredient frovatriptan and pharmaceutically acceptable salts thereof. In particular, it relates to efficient processes for the preparation of frovatriptan and its synthetic intermediates, which are amenable to large scale commercial production and provide the required products with improved yield and purity.
C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention relates to improved processes for preparing 3-(4-amino-1-oxo-1,3- dihydro-isoindol-2-yl)-piperidine-2,6-dione (I) (lenalidomide) and its intermediate 3-(1-oxo- 4-nitro-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to improved processes for preparing lenalidomide crystalline form A, use of said crystalline form A as an active pharmaceutical ingredient or as an intermediate in the preparation of further crystalline or amorphous forms of lenalidomide, compositions comprising lenalidomide crystalline form A and their use in the treatment of disease.
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 31/45 - Non-condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
The present invention relates to crystalline forms of the active pharmaceutical ingredient vorinostat, processes for their preparation and their use in pharmaceutical compositions. Formula (I).
C07C 239/14 - Hydroxylamino compounds or their ethers or esters having nitrogen atoms of hydroxylamino groups further bound to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
37.
A CRYSTALLINE FORM OF LENALIDOMIDE AND A PROCESS FOR ITS PREPARATION
The present invention relates to a novel crystalline form of lenalidomide having formula (I) and chemically known as 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to a process for the preparation of said novel form and its use in pharmaceutical preparations for the treatment of autoimmune disease, inflammation, inflammatory disease and diseases such as cancer, in particular the management of multiple myeloma.
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
38.
HPLC METHOD FOR THE ANALYSIS OF BOSENTAN AND RELATED SUBSTANCES AND USE OF THESE SUBSTANCES AS REFERENCE STANDARDS AND MARKERS
The present invention relates to a new HPLC method for the analysis of the drug substance bosentan and related substances and to the use of said substances as reference standards and markers.
The present invention relates to crystalline forms of the active pharmaceutical ingredient vorinostat, processes for their preparation and their use in pharmaceutical compositions.
C07C 239/14 - Hydroxylamino compounds or their ethers or esters having nitrogen atoms of hydroxylamino groups further bound to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient vorinostat. In particular it relates to a process for preparing vorinostat substantially free from impurities, involving suberic acid, aniline and hydroxylamine as starting materials.
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
41.
CRYSTALLINE FORM OF SUNITINIB AND PROCESSES FOR ITS PREPARATION
The present invention relates to a novel crystalline form of sunitinib free base designated form I and to processes for its preparation. The invention also relates to its use as an API and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising the novel crystalline form and salts, solvates and hydrates prepared according to the invention, and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer.
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
The present invention relates to novel polymorphs of sunitinib free base designated form II and form III and to processes for their preparation. The invention also relates to their use as APIs and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising said novel polymorphs and salts, solvates and hydrates prepared according to the invention,and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer.
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
The present invention relates to novel crystalline forms of tegaserod base and to processes tor the preparation of these novel crystalline forms. The invention also relates to pharmaceutical compositions comprising these, novel crystalline forms and to uses of said compositions in the treatment of patients suffering from gastrointestinal disorders. Formula (I)
The present invention relates to a novel crystalline form of rasagiline mesylate and a pure form of rasagiline mesylate and processes for their preparation. Further, the invention relates to pharmaceutical compositions comprising said forms and use of said compositions in the treatment of patients suffering from Parkinson's Disease, dementia, Alzheimer's Disease, depression, hyperactive syndrome, stroke, brain ischemia, neurotrauma, schizophrenia and multiple sclerosis.
C07C 211/42 - 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 condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
C07C 309/04 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
The present invention provides a convenient and efficient process for the preparation of O-desmethylvenlafaxine (ODV) or a salt thereof, comprising the reaction of venlafaxine, or a salt thereof, with a thiourea or a mixture of thioureas.
C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C07C 215/64 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
The present invention, relates to novel processes for the preparation of sunitinib malate formula (I), pharmaceutical compositions comprising said polymorph and the use of the said pharmaceutical compositions in the treatment of various forms of cancer.
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
The present invention relates to novel intermediates and further to the use of said intermediates in processes for the preparation of indolinone derivatives, in particular 3- pyrrole substituted 2-indolinones having amide moieties on the pyrrole ring. Such compounds are useful in die treatment of abnormal cell growth, such as cancer, in mammals.
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
48.
A PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE AMINES
The present invention relates to an improved process for the preparation of (R)-1-5 aminoindan (2), rasagiline (1) and pharmaceutically acceptable salts of rasagiline.
C07C 211/42 - 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 condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
The present invention relates to an improved process for the preparation of rasagiline (1) 5 and its pharmaceutically acceptable salts. In particular it relates to a process for preparing rasagiline (1) and its salts substantially free from impurities.
C07C 209/08 - Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups by substitution of halogen atoms with formation of amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
C07C 209/16 - Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups by substitution of hydroxy groups or of etherified or esterified hydroxy groups with formation of amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
C07C 211/42 - 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 condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C07C 217/20 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms
C07C 211/27 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by saturated carbon chains
50.
A NOVEL AND EFFICIENT METHOD FOR THE SYNTHESIS OF AN AMINO ACID
The present invention relates to a novel process for the preparation of γ-amino acids, such 5 as (±)-3-(aminomethyl)-5-methyl-hexanoic acid (1), which is a key intermediate in the preparation of the potent anticonvulsant pregabalin, (S)-(+)-3-(aminomethyl)-5-methyl- hexanoic acid (2), and its analogues.
C07C 227/04 - Formation of amino groups in compounds containing carboxyl groups
C07C 229/08 - 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 only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
C07C 205/51 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being saturated
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
A61P 25/00 - Drugs for disorders of the nervous system
C07C 205/15 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by hydroxy groups having nitro groups and hydroxy groups bound to acyclic carbon atoms of a saturated carbon skeleton
The present invention provides processes for preparing suspension aerosol formulations, wherein the particles for inhalation are formed in situ during the process of manufacturing the formulation. In one aspect of the invention, a process for preparing a suspension aerosol formulation comprises the steps of: (a) dissolving one or more medicaments in one or more solvents to form a solution; and (b) mixing one or more propellants with the solution under conditions effective to precipitate, entirely or partially, at least one of the medicaments.
The present invention relates to a novel crystalline form of tegaserod hydrochloride and to processes for preparing said form. The invention also relates to pharmaceutical compositions comprising said crystalline form and to the use of said compositions in the treatment of gastrointestinal disorders, in particular irritable bowel syndrome.
The present invention relates to a novel crystalline form of tegaserod mesylate and to processes for preparing said form. The invention also relates to pharmaceutical compositions comprising said crystalline form and to the use of said compositions in the treatment of gastrointestinal disorders, in particular irritable bowel syndrome.
The present invention relates to a novel crystalline form of tegaserod adipate and to processes for preparing said form. The invention also relates to pharmaceutical compositions comprising said crystalline form and to the use of said compositions in the treatment of gastrointestinal disorders, in particular irritable bowel syndrome.
The present invention relates to a novel process of preparing an enantiomerically enriched γ-amino acid, such as enantiomerically enriched (S)-pregabalin.
C07C 227/34 - Preparation of optical isomers by separation of optical isomers
C07C 229/08 - 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 only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
The present invention relates to two novel crystalline forms of zofenopril calcium, to processes for their preparation and their use in pharmaceutical compositions.
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
The present invention relates to novel polymorph forms III and IV of sunitinib malate, pharmaceutical compositions comprising the novel polymorphs and the use of the pharmaceutical compositions. The present invention further relates to processes for the preparation of polymorph form I, III and IV of sunitinib malate.
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient, vorinostat. In particular it relates to an efficient process for the preparation of vorinostat of high purity without the requirement to isolate any synthetic intermediate compounds.
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
The present invention relates to a novel intermediate useful in the preparation of bosentan and to processes for the preparation of said intermediate and bosentan. The invention further relates to compositions comprising bosentan prepared according to the processes of the invention and their use in the treatment of endothelin-receptor mediated disorders.
The present invention relates to a novel salt of tegaserod, namely tegaserod pimelate,and to processes for the preparation thereof. The invention also relates to crystalline forms of the novel salt and to pharmaceutical compositions comprising the novel salt. Further, the invention relates to uses of said compositions to provide methods of treating patients suffering from gastrointestinal disorders.
The present invention relates to a novel salt of tegaserod, namely tegaserod suberate,and to processes for the preparation thereof. The invention also relates to crystalline forms of the novel salt and to pharmaceutical compositions comprising thenovel salt. Further, the invention relates to uses of said compositions in treating patients suffering from gastrointestinal disorders.
The present invention relates to novel processes for the preparation of scopine esters and their quaternary salts. In particular, the present invention relates to a process for the preparation of tiotropium bromide, pharmaceutical compositions comprising tiotropium bromide and the use of such compositions in the treatment of respiratory disorders.
The present invention relates to a process for the preparation of steroidal 17β-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17β-carboxylic thioates, such as fluticasone propionate I, using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds II resulting in selective and controlled fluorination. The present invention also relates to intermediates II and their preparation.
The present invention relates to a novel method for the preparation of racemic pregabalin (1) or a single enantiomer thereof, (S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid (2).
C07C 227/04 - Formation of amino groups in compounds containing carboxyl groups
C07C 227/32 - Preparation of optical isomers by stereospecific synthesis
C07C 67/307 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of halogenPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by substitution of halogen atoms by other halogen atoms
C07C 67/31 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of functional groups containing oxygen only in singly bound form
C07C 67/343 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisationPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by change of size of the carbon skeleton by increase in the number of carbon atoms
C07C 69/63 - Halogen-containing esters of saturated acids
C07C 69/675 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids of saturated hydroxy-carboxylic acids
C07C 201/12 - Preparation of nitro compounds by reactions not involving the formation of nitro 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
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61P 25/00 - Drugs for disorders of the nervous system
The present invention relates to new HPLC methods for the analysis of the drug substance clopidogrel and related substances. In a first method the mobile phase comprises two or more liquids, and the relative concentration of the liquids is varied to a predetermined gradient. In a second method the mobile phase comprises a polar protic organic solvent, and the stationary phase comprises a gel. The present invention also relates to a method for analysing a substance, comprising the detection and optional quantification of one or more specific impurities.
The present invention relates to novel crystalline forms of the salicylate salt of tegaserod, and to processes for the preparation of these novel forms. The invention also relates to pharmaceutical compositions containing these novel polymorphs,and to uses of said compositions to provide methods of treating patients suffering from gastrointestinal disorders.
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
The present invention relates to novel crystalline forms of the glutarate salt of tegaserod, and to processes for the preparation of these novel forms. The invention also relates to pharmaceutical compositions containing these novel polymorphs,and to uses of said compositions to provide methods of treating patients suffering from gastrointestinal disorders.
The present invention relates tonovel HPLC methods for the analysis of the API formoterol and related substances. In a first method the mobile phase comprises two or more liquids, and the relative concentration of the liquids is varied to a predetermined gradient. In a second method the mobile phase comprises a first liquid A comprising an aqueous solution of ammonium acetate and a second liquid B comprising a dipolar aprotic solvent. In a third method the mobile phase comprises a first liquid A comprising an aqueous solution of ammonium acetate with a concentration of 0.001 to 0.025M, and a second liquid B. The present invention also relates to a method for analysing a substance, comprising the detection and optional quantification of one or more specific impurities.
The present invention provides a convenient and efficient process for the preparation of O-desmethylvenlafaxine (ODV), comprising the reaction of venlafaxine, or a salt thereof, with a thiol reagent such as a dithiol, an aminothiol or an inorganic thiol. The present invention also provides a process for purifying ODV base,said process comprising the steps of mixing crude ODV base with an alcohol to form a suspension and adding acid followed by base to generate ODV base with high purity.
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07C 215/64 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
The present invention relates to a novel salt of tegaserod, namely the dihydrogen phosphate salt. The present invention also relates to novel amorphous and crystalline forms of the dihydrogen phosphate salt of tegaserod. The invention further relates to processes for the preparation of the novel salt and the novel amorphous and crystalline forms. The invention also relates to pharmaceutical compositions containing the novel salt or the novel amorphous or crystalline forms, and to uses of said compositions to provide methods of treating patients suffering from gastrointestinal disorders.
The present invention relates to novel crystalline forms of bosentan and processes for their preparation. Further, the invention relates to pharmaceutical compositions comprising said crystalline forms and use of said compositions in the treatment of patientssuffering from endothelin receptor mediated disorders, for example,cardiovascular disorders such as hypertension, pulmonary hypertension, ischemia, vasospasm and angina pectoris.
The present invention relates to novel crystalline forms of the citrate salt of tegaserod, and to processes for the preparation of these novel crystalline forms. The invention also relates to pharmaceutical compositions containing these novel polymorphs, and to uses of said compositions to provide methods of treating patients suffering from gastrointestinal disorders.
The present invention relates to novel crystalline forms of the succinate salt of tegaserod, and to processes for the preparation of these novel crystalline forms. The invention also relates to pharmaceutical compositions containing these novel polymorphs, and to uses of said compositions to provide methods of treating patients suffering from gastrointestinal disorders.
The present invention relates to novel amorphous and crystalline forms of the tartrate salt of tegaserod, and to processes for the preparation of these novel forms. The invention also relates to pharmaceutical compositions containing these novel forms, and to uses of said compositions to provide methods of treatingpatients suffering from gastrointestinal disorders.
The present invention relates to an improved process for the preparation of the activepharmaceutical ingredient zolmitriptan. In particular, it relates to an efficient process for the preparation of zolmitriptan and its pharmaceutically acceptable salts and solvates.
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
The present invention relates to a novel anhydrous crystalline form of zofenopril calcium of formula (I), chemically known as (4S)-1-[(2S)-3-(benzoylthio)-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt or hemi-calcium salt. The present invention further relates to a process for the preparation of the new crystalline form of zofenopril calcium, its use in pharmaceutical compositions and the use of the new crystalline form and compositions in the treatment of hypertension and various other diseases.
The present invention relates to stable solid pharmaceutical compositions comprising valsartan as the active pharmaceutical ingredient. Optionally the compositions comprise one or more further active pharmaceutical ingredients. The invention further relates to methods for preparing said compositions and to the use of said compositions in the treatment or prevention of angiotensin receptor mediated disorders, in particular hypertension and related disorders.
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
The present invention relates to a novel process for the preparation of almotriptan and pharmaceutically acceptable salts thereof, which affords product conveniently and efficiently with commercially acceptable yields and purity. The present invention also relates to a novel synthetic intermediate used in the process.
The present invention relates to stable pharmaceutical compositions comprising one or more HMG-CoA reductase inhibitors, processes for preparing the stable compositions and uses for the compositions. The stable pharmaceutical compositions of the invention may be used, in particular, for the treatment of hyperlipoproteinemia and atherosclerosis.
C07C 211/38 - 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 a saturated carbon skeleton containing condensed ring systems
G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups
81.
PROCESS FOR INTRODUCTION OF HYDROXYETHOXY SIDE CHAIN IN BOSENTAN
The present invention relates to an improved process for the preparation of bosentan. In particular it relates to a process for preparing bosentan substantially free from the dirner impurity of formula (II) and the 6-hydroxy impurity of formula (III). The invention also relates to a pharmaceutical composition comprising bosentan and its use in the treatment of endothelin-receptor mediated disorders.
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
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61P 11/00 - Drugs for disorders of the respiratory system
The present invention relates to pharmaceutical compositions and in particular to suspension aerosol pharmaceutical compositions, processes to obtain them and their use in inhalation therapy.
The present invention relates to a novel salt of tegaserod, tegaserod besylate,and also to polymorphic forms of this salt. The invention further relates to processes for the preparation of the salt and polymorphic forms. The invention also relates to pharmaceutical compositions comprising the salt, optionally in a polymorphic form, and to uses of said compositions for treating patients suffering from gastrointestinal disorders.
The present invention relates to a novel salt of tegaserod, tegaserod benzoate, and also to polymorphic forms of this salt. The invention further relates to processes for the preparation of the salt and polymorphic forms. The invention also relates to pharmaceutical compositions comprising the salt, optionally in a polymorphic form, and to uses of said compositions for treating patients suffering from gastrointestinal disorders.
The present invention relates to a novel salt of tegaserod, tegaserod malate,and also to polymorphic forms of this salt. The invention further relates to processes for the preparation of the salt and polymorphic forms. The invention also relates to pharmaceutical compositions comprising the salt, optionally in a polymorphic form, and to uses of said compositions for treating patients suffering from gastrointestinal disorders.
The present invention relates to a novel process for the preparation of rizatriptan and its pharmaceutically acceptable salts. It provides a novel process for the preparation of highly pure rizatriptan, which can be easily adopted for commercial production with a high degree of consistency in purity and yield. Subsequently the rizatriptan base preparedcan be converted into any suitable pharmaceutically acceptable salt, such as the oxalate, succinate or benzoate salt,for dosage form preparation. The present invention also provides a composition comprising rizatriptan useful for the manufacture of a medicament for the treatment or prevention of migraine.
C07D 403/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
The present invention is directed towards a novel crystalline form of olmesartan medoxomil, to methods for preparing the compound, to compositionscomprising the compound, and to the use of said compound and compositions for the treatment or prevention of an angiotensin II receptor mediated disorder, in particular hypertension.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
The present invention is directed towards amorphous olmesartan medoxomil, to methods for preparing the compound, to compositions comprising the compound, and to the use of said compound and compositions for the treatment or prevention of an angiotensin II receptor mediated disorder, in particular hypertension.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
The present invention relates to novel polymorphic forms of the fumarate salt of tegaserod, and to processes for the preparation of these novel polymorphic forms. The invention also relates to pharmaceutical compositions comprising these novel polymorphs, and to uses of said compositions for treating patients suffering from gastrointestinal disorders.
The present invention relates to novel polymorphic forms of the oxalate salt of tegaserod,and to processes for the preparation of these novel polymorphic forms. The invention also relates to pharmaceutical compositions comprising these novel polymorphs,and to uses of said compositions for treating patients suffering from gastrointestinal disorders.
The present invention relates to a process for the preparation of polymorphic forms of the R- and S-enantiomers of modafinil, R-(-)-2-benzhydrylsulfinylacetamide and S-(+)-2- benzhydrylsulfinylacetamide respectively.
C07C 315/02 - Preparation of sulfonesPreparation of sulfoxides by formation of sulfone or sulfoxide groups by oxidation of sulfides, or by formation of sulfone groups by oxidation of sulfoxides
C07C 317/44 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
The present invention relates to various novel salts of tegaserod and to novel polymorphic forms of various salts of tegaserod, including polymorphic forms of tegaserod succinate, tartrate, malonate, camphor sulphonate, mandelate, oxalate and fumarate. The invention further relates to processes for the preparation of these novel salts and novel polymorphic forms. The invention also relates to pharmaceutical compositions comprising these novel salts or novel polymorphs, and to uses of said compositions for treating patients suffering from gastrointestinal disorders.
The present invention relates to a process for preparing polymorphic form A of 2-[(5-5 methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide maleate (tegaserod maleate). The invention further relates to tegaserod maleate form A substantially free of other polymorphic forms and chemicalimpurities, to compositions comprising tegaserod maleate form A and to the use of said compositions in the treatment of gastrointestinal disorders such as irritable bowel syndrome and heartburn.
The present invention relates to a novel process for the preparation of pharmaceutically pure olanzapine. The invention is also related to impurities obtained during the preparation of pharmaceutically pure olanzapine and methods for the detection of the impurities.
Novel polymorphic forms of bosentan and processes for their preparation are disclosed. Further, pharmaceutical compositions comprising said polymorphicforms and the use of said compositions in the treatment of patientssuffering from endothelin receptor mediated disorders, for example,cardiovascular disorders such as hypertension, pulmonary hypertension, ischemia, vasospasm and angina pectoris are disclosed.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 9/00 - Drugs for disorders of the cardiovascular system
96.
PROCESS FOR THE PREPARATION OF O-DESMETHYL VENLAFAXINE
C07C 215/56 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups
C07C 217/64 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 235/34 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A pharmaceutical composition comprising eplerenone having a D90 particle size of between 15-25 microns and further comprising one or more pharmaceutically acceptable excipients.
A61K 31/569 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone substituted in position 17 alpha, e.g. ethisterone
The present invention is related to a device attachable to a pill container to alert a person when a pill or a medication has to be taken, the device comprising a case having a top case (1), a bottom case (2) suitable to engage with the pill container (3), said case comprising a clock and timer electronic circuit (4) to provide current time in hours and minutes and to provide an alarm signal, power source means (5), alarm means responsive to said alarm signal, sensing means (7) for detecting an access to the pill container (3), memory means (8) to store alarm time and to record access to the pill container, a LCD unit (10) to display current time, alarm time and information relating to the compliance of pills, a LCD lens (11), selector means (12) comprising means (13) to set the time clock, means (14) to set the alarm, means (15) to adjust clock time or adjust clock alarm time.
The present invention relates to a novel process for the synthesis of 1-((5-methoxy- 1H-indol-3-yl)methyleneamino)-3-pentyl-guanidine, commonly known as tegaserod, which is used as a gastroprokinetic, and salts thereof. The present invention also relates to tegaserod and salts thereof having an HPLC purity of about 95% or more. The present invention further relates to pharmaceutical compositions comprising tegaserod or a salt thereof, second medical uses of tegaserod or a salt thereof, and methods of treating or preventing irritable bowel syndrome using tegaserod or a salt thereof.
