Patent application number | Description | Published |
20080200684 | Process for Preparing Ethyl (s)-2-Ethoxy-4-[N-[1-(2-Piperidinophenyl)-3-Methyl-1-Butyl]Aminocarbonyl Methyl]Benzoate and Use Thereof for the Preparation of Repaglinide - Described herein is an improved, commercially viable and industrially advantageous process for the preparation of Repaglinide intermediate, ethyl (S)-2-ethoxy-4-[N-(1-(2-piperidino-phenyl)-3-methyl-1-butyl)-aminocarbonylmethyl]-benzoate. The process provides the Repaglinide intermediate in higher yield and purity compared to the previously disclosed processes, thereby providing for production of Repaglinide and its pharmaceutically acceptable salts in high purity and in high yield. | 08-21-2008 |
20090181977 | Anhydrous Amorphous Imatinib Mesylate - Described is a highly stable amorphous form of imatinib mesylate having a water content of less than 0.5 percent by weight, based on the total weight of the amorphous imatinib mesylate, (anhydrous amorphous imatinib mesylate), a process for preparation thereof, and pharmaceutical compositions. | 07-16-2009 |
20090202647 | SOLID FORM OF RACEMIC ROTIGOTINE - Disclosed herein are solid state forms, amorphous and crystalline forms, of racemic rotigotine having high purity, adequate stability, good flowability and good dissolution properties, a process for preparation, and pharmaceutical compositions comprising amorphous racemic rotigotine. | 08-13-2009 |
20100063299 | Process for Preparing Irbesartan - Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of Irbesartan, or a pharmaceutically acceptable salt thereof, in high yield and purity. | 03-11-2010 |
20100104649 | Lercanidipine Hydrochloride Polymorphs and an Improved Process for Preparation of 1,1,N-Trimethyl-N-(3,3-Diphenylpropyl)-2-Aminoethyl Acetoacetate - Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of substantially pure Lercanidipine intermediate, 1,1,N-trimethyl-N-(3,3-diphenylpropyl)-2-aminoethyl acetoacetate. The intermediate is useful for preparing Lercanidipine, or a pharmaceutically acceptable salt thereof, in high yield and purity. The present invention further provides a novel crystalline form of Lercanidipine hydrochloride and a process for its preparation. The present invention also provides a process for the preparation of amorphous form of Lercanidipine hydrochloride. | 04-29-2010 |
20100197732 | Repaglinide Substantially Free of Dimer Impurity - The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D | 08-05-2010 |
20100204296 | Novel Polymorphs of Darifenacin Free Base and its Hydrobromide Salt - The present invention provides a novel and stable amorphous form of darifenacin free base, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention further provides a novel and stable polymorphic form of darifenacin hydrobromide, process for preparation, pharmaceutical compositions, and method of treating thereof. | 08-12-2010 |
20100217034 | Process for the Preparation of Fesoterodine - Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of Fesoterodine or a pharmaceutically acceptable salt thereof in high yield and purity. Disclosed also herein is an improved and industrially advantageous optical resolution method of racemic (±)-N,N-Diisopropyl-3-(2-benzyloxy-5-bromophenyl)-3-phenylpropylamine and use thereof for the preparation of Fesoterodine. | 08-26-2010 |
20100272815 | AMORPHOUS FORM OF TAPENTADOL HYDROCHLORIDE - Disclosed herein is a novel and stable amorphous form of tapentadol hydrochloride, a process for the preparation, pharmaceutical compositions, and a method of treating thereof. Disclosed also herein is a stable amorphous co-precipitate of tapentadol hydrochloride with pharmaceutically acceptable excipients, a method for the preparation, pharmaceutical compositions, and a method of treating thereof. Advantageously, the amorphous co-precipitates of tapentadol hydrochloride have improved physiochemical characteristics that assist in the effective bioavailability. | 10-28-2010 |
20100278878 | QUETIAPINE SALTS AND THEIR POLYMORPHS - The present invention relates to novel and stable salt forms of quetiapine, processes for preparation, pharmaceutical compositions, and method of treating thereof. More particularly, the present invention provides novel acid addition salts of quetiapine wherein the acid counter ion is provided by an acid selected from the group consisting of benzene sulfonic acid, dibenzoyl-L-(+)-tartaric acid and di-p-toluoyl-L-(+)-tartaric acid. The present invention also provides novel polymorphic forms of quetiapine salts selected from the group consisting of quetiapine hydrobromide, quetiapine sulfate, quetiapine nitrate and quetiapine citrate. | 11-04-2010 |
20100285075 | Novel Hemioxalate Salt of Eletriptan - The present invention relates to novel hemioxalate salt of eletriptan, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention relates to solid forms of eletriptan hemioxalate, processes for preparation, pharmaceutical compositions, and method of treating thereof. The solid form of eletriptan hemioxalate is useful for preparing eletriptan free base or a pharmaceutically acceptable salt thereof, particularly eletriptan hydrobromide, in high purity. The present invention also provides a process for preparing substantially pure eletriptan hydrobromide using eletriptan hemioxalate. | 11-11-2010 |
20100297241 | Amorphous Fesoterodine Fumarate - The present invention provides a novel amorphous form of fesoterodine fumarate, process for preparation, pharmaceutical compositions, and method of treating thereof. | 11-25-2010 |
20100317859 | Process for the Preparation of Risedronate Sodium - Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of risedronic acid or a pharmaceutically acceptable salt thereof, in high yield and purity. | 12-16-2010 |
20100330130 | SUBSTANTIALLY PURE IMATINIB OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Provided herein are impurities of imatinib, N-(2-Methyl-5-methylamino-phenyl)-N-(4-pyridin-3-yl-pyrimidin-2-yl)-formamide (formamide impurity) and 4-[4-(Imidazole-1-carbonyl)-piperazin-1-ylmethyl]-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide (carbonylimidazole impurity), and processes for the preparation and isolation thereof. Provided further herein is a highly pure imatinib or a pharmaceutically acceptable salt thereof substantially free of formamide and carbonylimidazole impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure imatinib or a pharmaceutically acceptable salt thereof substantially free of impurities. Disclosed also herein is a process for preparing substantially pure α-form of imatinib mesylate. | 12-30-2010 |
20110014246 | AMORPHOUS ARFORMOTEROL L-(+)-TARTRATE - Disclosed herein is a novel and stable amorphous form of arformoterol L-(+)-tartrate, a process for its preparation, pharmaceutical compositions comprising amorphous arformoterol L-(+)-tartrate, and methods of treating with amorphous arformoterol L-(+)-tartrade. | 01-20-2011 |
20110014291 | Novel Polymorphs of Bosentan - Disclosed herein are novel polymorphic forms of bosentan, processes for preparation, pharmaceutical compositions, and method of treating thereof. | 01-20-2011 |
20110021547 | Substantially Pure and a Stable Crystalline Form of Bosentan - Described is a highly stable crystalline form of bosentan having a water content in the range of about 3-4% by weight, based on the total weight of the bosentan, (bosentan crystalline form A5), a process for preparation thereof, and pharmaceutical compositions comprising the bosentan crystalline form A | 01-27-2011 |
20110046231 | SOLID FORMS OF (.+-.)-O-DESMETHYLVENLAFAXINE SALTS - The present invention relates to solid forms of (±)-O-desmethylvenlafaxine salts, processes for preparation, pharmaceutical compositions, and method of treating thereof. More particularly, the present invention provides solid forms of acid addition salts of (±)-O-desmethylvenlafaxine wherein the acid counter ion is provided by an acid selected from the group consisting of oxalic acid, benzoic acid and lactic acid. | 02-24-2011 |
20110071120 | SOLID STATE FORMS OF TAPENTADOL SALTS - Provided herein are novel solid state forms of tapentadol salts, process for their preparation, pharmaceutical compositions, and method of treating thereof. The tapentadol salts include an L-(−)-camphorsulfonate salt, a dibenzoyl-(L)-tartrate salt, a dibenzoyl-(D)-tartrate salt, a malate salt, a maleate salt, or a salicylate salt. | 03-24-2011 |
20110086103 | NOVEL MANDELATE SALT OF FESOTERODINE - Provided herein is a novel raantlelate sail of fesoterodine, process for the preparation, pharmaceutics!! compositions, and method of treating thereof. Provided also herein are solid state forms of fesoterodine mandelate, process for the preparation, pharmaceutical compositions, and method of treating thereof. The raandelate salt of fesoterodine is useful for preparing fesoterodine free base or a pharmaceutically acceptable salt thereof; particularly fesoterodine fumaraie, in high purity. | 04-14-2011 |
20110097413 | SOLID STATE FORMS OF DEFERASIROX SALTS AND PROCESS FOR THE PREPARATION THEREOF - Provided herein are novel solid state forms of deferasirox salts, process for the preparation, pharmaceutical compositions, and method of treating thereof. The solid state forms of deferasirox salts are useful for preparing deferasirox (I) in high purity. | 04-28-2011 |
20110105756 | Process for Preparing Quinoline-3-Carboxamide Derivatives - Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of quinoline-3-carboxamide derivatives such as laquinimod, or a pharmaceutically acceptable salt thereof, in high yield and purity. | 05-05-2011 |
20110117200 | RASAGILINE MESYLATE PARTICLES AND PROCESS FOR THE PREPARATION THEREOF - Provided herein is rasagiline mesylate having a 90 volume-percent of the particles (D | 05-19-2011 |
20110124903 | SOLID STATE FORMS OF FESOTERODINE INTERMEDIATES - Provided herein are novel solid state forms of fesoterodine intermediates, (R)-4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-benzoic acid and (R)-[4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-phenyl]-methanol, and processes for their preparation thereof. The solid state intermediates are useful for preparing fesoterodine or a pharmaceutically acceptable salt thereof in high purity. | 05-26-2011 |
20110171138 | SUBSTANTIALLY PURE DEFERASIROX AND PROCESSES FOR THE PREPARATION THEREOF - Provided herein is a highly pure deferasirox or a pharmaceutically acceptable salt thereof substantially free of hydrazine impurity, 4-hydrazinobenzoic acid, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure deferasirox or a pharmaceutically acceptable salt thereof substantially free of hydrazine impurity. | 07-14-2011 |
20110171270 | NOVEL SOLID STATE FORMS OF LAQUINIMOD AND ITS SODIUM SALT - Provided herein is a novel crystalline form of laquinimod, process for the preparation, pharmaceutical compositions, and method of treating thereof. Provided also herein are novel amorphous and polymorphic forms of laquinimod sodium, process for the preparation, pharmaceutical compositions, and method of treating thereof. | 07-14-2011 |
20110171274 | Fesoterodine Substantially Free of Dehydroxy Impurity - Provided herein is an impurity of fesoterodine, fesoterodine dehydroxy impurity, 2-[(1R)-3-[bis(1-methylethy)amino]-1-phenylpropyl]-4-methylphenyl isobutyrate, and a process for preparing and isolating thereof. Provided further herein is a highly pure fesoterodine or a pharmaceutically acceptable salt thereof substantially free of fesoterodine dehydroxy impurity, process for the preparation thereof, and pharmaceutical compositions comprising highly pure fesoterodine or a pharmaceutically acceptable salt thereof substantially free of dehydroxy impurity. Provided also herein is a pharmaceutical composition comprising solid particles of pure fesoterodine fumarate substantially free of dehydroxy impurity, wherein 90 volume-percent of the particles (D90) have a size of less than about 200 microns. | 07-14-2011 |
20110178326 | UNSATURATED CINACALCET SALTS AND PROCESSES FOR PREPARING CINACALCET HYDROCHLORIDE - Disclosed herein are convenient, industrially advantageous and environmentally friendly processes for the preparation of cinacalcet hydrochloride. Disclosed also herein are novel hydrochloride, oxalate and di-p-toluoyl-L-(+)-tartrate salts of (R)-α-methyl-N-[3-[3-(trifluoromethyl)phenyl]propylene]-1-naphthalenemethaneamine (unsaturated cinacalcet), solid state forms of the salts, and a process for their preparation thereof. | 07-21-2011 |
20110223213 | HIGHLY PURE RANOLAZINE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Provided herein is an impurity of ranolazine, 1-[4-[2-hydroxy-3-(2-methoxy-phenoxy)-propyl]-piperazin-1-yl]-3-(2-methoxy-phenoxy)-propan-2-ol (dimer impurity-3), and process for preparing and isolating thereof. Provided further herein is a highly pure ranolazine or a pharmaceutically acceptable salt thereof substantially free of dimer impurity-3, process for the preparation, and pharmaceutical compositions comprising highly pure ranolazine or a pharmaceutically acceptable salt thereof substantially free of dimer impurity-3. | 09-15-2011 |
20110224437 | PROCESS FOR PREPARING VARENICLINE, VARENICLINE INTERMEDIATES, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4,5-diamino-10-aza-tricyclo[6.3.1.0 | 09-15-2011 |
20110245536 | PROCESS FOR PREPARING PREGABALIN - Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of pregabalin in high yield and purity. The present invention also provides a process for the purification of (S)-pregabalin. | 10-06-2011 |
20110313176 | PROCESSES FOR PREPARING HIGHLY PURE ROTIGOTINE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Provided herein are convenient, industrially advantageous and environmentally friendly processes for the preparation of (−)-(S)-5-hydroxy-2-[N-n-propyl-N-2-(2-thienyl)ethylamino]tetralin (rotigotine) or a pharmaceutically acceptable salt thereof. Provided further herein is a highly pure rotigotine or a pharmaceutically acceptable salt thereof substantially free of impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure rotigotine or a pharmaceutically acceptable salt thereof substantially free of impurities. | 12-22-2011 |
20110313199 | PROCESSES FOR PREPARING SUBSTANTIALLY PURE ARFORMOTEROL AND ITS INTERMEDIATES - Provided herein are improved, convenient and industrially advantageous processes for the preparation of N-[2-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]phenyl]formamide (Arformoterol) or a pharmaceutically acceptable salt thereof, in high yield and purity. Provided further herein is an improved and industrially advantageous process for the preparation of a substantially enantiomerically pure arformoterol intermediate, (R)-4-methoxy-α-methyl-N-(phenylmethyl)benzeneethanamine. | 12-22-2011 |
20110318417 | HIGHLY PURE CINACALCET OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Provided herein are impurities of cinacalcet, (R)-α-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-(5,6,7,8-tetrahydronaphthalene)methaneamine (tetrahydro cinacalcet impurity), (R)-α-Methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethaneamine-N-oxide (cinacalcet N-oxide impurity) and (R)-α-methyl-N-[3-[3-(trifluoromethyl)phenyl]methyl]-1-naphthalenemethaneamine (benzylamine impurity); and processes for preparation and isolation thereof. Provided further herein is a highly pure cinacalcet or a pharmaceutically acceptable salt thereof substantially free of impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure cinacalcet or a pharmaceutically acceptable salt thereof substantially free of impurities. | 12-29-2011 |
20120009226 | HIGHLY PURE LAQUINIMOD OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Provided herein is an impurity of laquinimod, N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxoquinoline-3-carboxamide (deschloro laquinimod impurity), and process for preparation and isolation thereof. Provided further herein is a highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity. | 01-12-2012 |
20120027816 | HIGHLY PURE ELETRIPTAN OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF ELETRIPTAN N-OXIDE IMPURITY - Provided herein is an impurity of eletriptan, eletriptan N-oxide, (R)-5-[2- (phenylsulfonypethyl]-3-[(1-methyl-2-pyrrolidinyl-N-oxide)methyl]-1H-indole, and a process for the preparation and isolation thereof. Provided further herein is a highly pure eletriptan or a pharmaceutically acceptable salt thereof substantially free of eletriptan N-oxide impurity, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure eletriptan or a pharmaceutically acceptable salt thereof substantially free of eletriptan N-oxide impurity. | 02-02-2012 |
20120065404 | Process for Preparing Ethyl (s)-2-Ethoxy-4-[N-[1-(2-Piperidinophenyl)-3-Methyl-1-Butyl]Aminocarbonyl Methyl]Benzoate and Use Thereof for the Preparation of Repaglinide - Described herein is an improved, commercially viable and industrially advantageous process for the preparation of Repaglinide intermediate, ethyl (S)-2-ethoxy-4-[N-(1-(2-piperidino-phenyl)-3-methyl-1-butyl)-aminocarbonylmethyl]-benzoate. The process provides the Repaglinide intermediate in higher yield and purity compared to the previously disclosed processes, thereby providing for production of Repaglinide and its pharmaceutically acceptable salts in high purity and in high yield. | 03-15-2012 |
20120093887 | AMORPHOUS VARENICLINE TARTRATE CO-PRECIPITATES - Disclosed herein is a stable amorphous coprecipitate comprising varenicline tartrate and a pharmaceutically acceptable excipient selected from the group consisting of maltodextrin, lactose monohydrate and 2-hydroxypropyl-β-cyclodextrin, method for the preparation, pharmaceutical compositions, and method of treating thereof. Advantageously, the amorphous coprecipitates of varenicline tartrate disclosed herein have improved physiochemical characteristics that assist in the effective bioavailability. | 04-19-2012 |
20120164188 | PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF IMPURITIES - Provided herein are impurities of paliperidone, 3-[2-[4-[1-(4-fluoro-2-hydroxyphenyl)methanoyl]piperidinyl-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one (methanoyl impurity), 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one (dehydroxy impurity) and 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-7,8-dihydro-6H-pyrido[1,2-a]pyrimidin-4,9-dione (9-keto impurity), and processes for preparing and isolating thereof. Provided further herein is a highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9-keto impurities, process for the preparation thereof, and pharmaceutical compositions comprising highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9-keto impurities. Provided also herein are improved and efficient processes for preparing paliperidone intermediates. | 06-28-2012 |
20120269871 | SOLID STATE FORMS OF RASAGILINE SALTS - Provided herein are novel crystalline forms of rasagiline salts, processes for their preparation, pharmaceutical compositions, and method of treating thereof. The rasagiline salts include a maleate salt, a mandelate salt, or a salicylate salt. | 10-25-2012 |
20130072682 | PROCESS FOR PREPARING VARENICLINE, VARENICLINE INTERMEDIATES, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4 ,5-diamino-10-aza-tricyclo[6.3.1.0 | 03-21-2013 |
20130090314 | SOLID STATE FORMS OF TAPENTADOL SALTS - Provided herein are novel solid state forms of tapentadol salts, process for their preparation, pharmaceutical compositions, and method of treating thereof. The tapentadol salts include an L-(−)-camphorsulfonate salt, a dibenzoyl-(L)-tartrate salt, a dibenzoyl-(D)-tartrate salt, a malate salt, a maleate salt, or a salicylate salt. | 04-11-2013 |
20130096346 | RESOLUTION METHODS FOR ISOLATING DESIRED ENANTIOMERS OF TAPENTADOL INTERMEDIATES AND USE THEREOF FOR THE PREPARATION OF TAPENTADOL - Provided herein is an improved and industrially advantageous optical resolution method for resolving (2R,3R)/(2S,3S)-1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol, and use thereof for the preparation of tapentadol or a pharmaceutically acceptable salt thereof. Provided further herein is an improved and industrially advantageous optical resolution method for resolving (2R,3R)/(2S,3S)-[3-(3-methoxyphenyl)-2-methylpentyl]-dimethylamine, and use thereof for the preparation of tapentadol or a pharmaceutically acceptable salt thereof. Disclosed also herein is an improved, commercially viable and industrially advantageous process for the preparation of tapentadol or a pharmaceutically acceptable salt thereof in high yield and purity. | 04-18-2013 |
20130096347 | NOVEL PROCESS FOR PREPARING HIGHLY PURE TAPENTADOL OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Provided herein is a novel, commercially viable and industrially advantageous process for the preparation of 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol (Tapentadol), or a pharmaceutically acceptable salt thereof, and its intermediates, in high yield and purity. Provided also herein are novel solid state forms of tapentadol intermediates and processes for their preparation thereof. Provided further herein is a purification process for preparing highly pure tapentadol hydrochloride. | 04-18-2013 |
20130101630 | HIGHLY PURE VARENICLINE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF METHYLVARENICLINE IMPURITY - Provided herein is an impurity of varenicline, methylvarenicline, 6-methyl-5,8,14-triazatetracyclo[10.3.1.0 | 04-25-2013 |
20130150577 | NOVEL PROCESS FOR PREPARING PHENYLCYCLOPROPYLAMINE DERIVATIVES USING NOVEL INTERMEDIATES - Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity. | 06-13-2013 |
20130165696 | NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR - Provided herein are novel processes for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. Provided further herein are novel acid addition salts of trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine, and process for their preparation. The intermediate and its acid addition salts are useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity. | 06-27-2013 |
20130317220 | NOVEL PROCESSES FOR PREPARING TRIAZOLO[4, 5-d]PYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF - Provided herein is a novel process for the preparation of triazolo[4,5-d]pyrimidine derivatives. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of highly pure ticagrelor or a pharmaceutically acceptable salt thereof. Provided further herein is a novel process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]-dioxol-4-yl]oxy]-1-ethanol. | 11-28-2013 |
20140005401 | Process for Preparing Quinoline-3-Carboxamide Derivatives | 01-02-2014 |
20140206867 | Process for Preparing Cyclopentylamine Derivatives and Intermediates Thereof - Disclosed herein is an improved process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Particularly described is an improved, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, [3aR-(3aα,4α,6α,6aα]-2-[[6-amino-2,2-dimethyltetrahydro-4H-cyclopenta-1,3-dioxol-4-yl]oxy]-ethanol, alternatively named, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]-dioxol-4-yl]oxy]-1-ethanol. | 07-24-2014 |
20140323727 | NOVEL PROCESS FOR PREPARING PHENYLCYCLOPROPYLAMINE DERIVATIVES USING NOVEL INTERMEDIATES - Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity. | 10-30-2014 |
20140350301 | NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR - Provided herein are novel processes for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. Provided further herein are novel acid addition salts of trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine, and process for their preparation. The intermediate and its acid addition salts are useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity. | 11-27-2014 |