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1. 发明申请

WO2012123958A1 HIGHLY PURE SALTS OF CLOPIDOGREL FREE OF GENOTOXIC IMPURITIES 审中-公开
标题翻译：高纯度无菌的纯天然食物
公开(公告)号：WO2012123958A1
公开(公告)日：2012-09-20
申请号：PCT/IN2012/000098
申请日：2012-02-14
申请人： CADILA HEALTHCARE LIMITED , PANDEY, Bipin , DAVE, Mayank Ghanshyambhai , DAVADRA, Prakash
发明人： PANDEY, Bipin , DAVE, Mayank Ghanshyambhai , DAVADRA, Prakash
IPC分类号： C07D495/04 , A61K31/4365 , A61P9/10
CPC分类号： C07D495/04 , A61K31/4365
摘要： The present invention relates to substantially pure salts of clopidogrel of Formula (I) substantially free from genotoxic impurities. (I) wherein (S) represents a suitable organic or inorganic acid, which forms a salt with clopidogrel having less acidity.
摘要翻译：本发明涉及基本上不含基因毒性杂质的基本上纯的式（I）氯吡格雷盐。（I）其中（S）表示与酸度较小的氯吡格雷形成盐的合适的有机或无机酸。

2. 发明申请

WO2012046254A3 PROCESS FOR PREPARING AN INTERMEDIATE OF SITAGLIPTIN VIA ENZYMATIC CONVERSION 审中-公开
标题翻译：通过酶转化制备西他汀的中间体的方法
公开(公告)号：WO2012046254A3
公开(公告)日：2012-06-07
申请号：PCT/IN2011000702
申请日：2011-10-10
申请人： CADILA HEALTHCARE LTD , MENDIRATTA SANJEEV KUMAR , PANDEY BIPIN , JOSHI RUPAL , TRIVEDI UMANG , DAVE MAYANK G , KOTHARI HIMANSHU M , SHUKLA BHAVIN
发明人： MENDIRATTA SANJEEV KUMAR , PANDEY BIPIN , JOSHI RUPAL , TRIVEDI UMANG , DAVE MAYANK G , KOTHARI HIMANSHU M , SHUKLA BHAVIN
IPC分类号： C07D487/04 , C12N9/02 , C12P17/18
CPC分类号： C07D487/04 , C12N9/0004 , C12P17/182 , C12P41/002 , C12R1/19
摘要： The invention provides a process for preparing 3 -hydroxy-1-(3- (trifluoromethyl)-5,6-dihydro-[l,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl) butan-1-one (Formula I), into its racemic (R/S) form or any of its optically active (S) or (R) forms or enantiomeric excess mixture of any of the forms comprising: a) reacting 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1- (2,4,5-trifluorophenyl)butan-2-one of formula (III) with a suitable oxidoreductase enzymes or its suitable variants in the presence of suitable conditions and co-factor b) isolating 3-hydroxy-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl)-4-(2,4,5-trifluorophenyl) butan-1-one, into its racemic (R/S) form or any of its optically active (S) or (R) forms or enantiomeric excess mixture of any of the forms
摘要翻译：本发明提供了制备3-羟基-1-（3-（三氟甲基）-5,6-二氢 - [1,2,4]三唑并[4,3-a]吡嗪-7（8H） - 基） -4-（2,4,5-三氟苯基）丁-1-酮（式I）转化成其外消旋（R / S）形式或其任何光学活性（S）或（R）形式或对映体过量混合物任何形式包括：a）使4-氧代-4- [3-（三氟甲基）-5,6-二氢[1,2,4]三唑并[4,3-a]吡嗪-7（8H） - 基 ] - （2,4,5-三氟苯基）丁-2-酮与合适的氧化还原酶或其合适的变体在合适的条件和辅因子存在下b）分离3-羟基-1 - （3-（三氟甲基）-5,6-二氢 - [1,2,4]三唑并[4,3-a]吡嗪-7（8H） - 基）-4-（2,4,5-三氟苯基）（R / S）形式或其任何形式的任何光学活性（S）或（R）形式或对映异构体过量混合物

3. 发明申请

WO2010097802A3 A PROCESS FOR THE PREPARATION OF ETORICOXIB 审中-公开
标题翻译：一种制备ETORICOXIB的方法
公开(公告)号：WO2010097802A3
公开(公告)日：2010-12-23
申请号：PCT/IN2010000045
申请日：2010-01-25
申请人： CADILA HEALTHCARE LTD , PANDEY BIPIN , DAVE MAYANK GHANSHYAMBHAI , SHAH MITESH
发明人： PANDEY BIPIN , DAVE MAYANK GHANSHYAMBHAI , SHAH MITESH
IPC分类号： C07D207/20 , C07D211/70 , C07D213/61
CPC分类号： C07D213/61 , C07D207/20 , C07D211/70
摘要： The present invention provides a improved process for preparing Etoricoxib using substituted ß-chlorovinaniidinium salts containing a cyclic group, optionally containing a heteroatom. The present invention also provides a process for the preparation of the intermediate ß-chlorovinamidinium salts. In one of the embodiments is provided a process for the purification of Etoricoxib as well as the intermediates.
摘要翻译：本发明提供了使用含有环状基团的任选含有杂原子的取代的β-氯乙烯基鎓盐制备Etoricoxib的改进方法。本发明还提供了制备中间体β-氯乙脒盐的方法。在其中一个实施方案中提供了用于纯化Etoricoxib以及中间体的方法。

4. 发明申请

WO2010097802A2 A PROCESS FOR THE PREPARATION OF ETORICOXIB 审中-公开
标题翻译：一种制备ETORICOXIB的方法
公开(公告)号：WO2010097802A2
公开(公告)日：2010-09-02
申请号：PCT/IN2010/000045
申请日：2010-01-25
申请人： CADILA HEALTHCARE LIMITED , PANDEY, Bipin , DAVE, Mayank, Ghanshyambhai , SHAH, Mitesh
发明人： PANDEY, Bipin , DAVE, Mayank, Ghanshyambhai , SHAH, Mitesh
IPC分类号： C07D207/20 , C07D211/70 , C07D213/61
CPC分类号： C07D213/61 , C07D207/20 , C07D211/70
摘要： The present invention provides a improved process for preparing Etoricoxib using substituted β-chlorovinaniidinium salts containing a cyclic group, optionally containing a heteroatom. The present invention also provides a process for the preparation of the intermediate β-chlorovinamidinium salts. In one of the embodiments is provided a process for the purification of Etoricoxib as well as the intermediates.
摘要翻译：本发明提供了使用含有环状基团的取代的β-氯代乙酰id盐来制备依托考昔的改进方法，所述环状基团任选地含有杂原子。本发明还提供了制备中间体β-氯乙酰胺脒盐的方法。在一个实施方案中提供了用于Etoricoxib以及中间体纯化的方法。

5. 发明申请

WO2010032264A3 IMPROVED PROCESS FOR PREPARATION OF (2R)-4-OXO-4-[3- (TRIFLUOROMETHYL)-5,6-DIHYDRO [1,2,4]-TRIAZOLO[4,3-A]PYRAZIN- 7(8H)-YL]-L-(2,4,5-TRIFLUOROPHENYL)BUTAN-2-AMINE & NEW IMPURITIES IN PREPARATION THEREOF 审中-公开
公开(公告)号：WO2010032264A3
公开(公告)日：2010-03-25
申请号：PCT/IN2009/000470
申请日：2009-08-26
申请人： CADILA HEALTHCARE LIMITED , KOTHARI, Himanshu, Madhusudan , DAVE, Mayank, Ghanshyambhai , PANDEY, Bipin , SHUKLA, Bhavin, Shriprasad
发明人： KOTHARI, Himanshu, Madhusudan , DAVE, Mayank, Ghanshyambhai , PANDEY, Bipin , SHUKLA, Bhavin, Shriprasad
IPC分类号： C07D487/04
摘要： The present invention relates to synthesis of β-amino acid derivatives of formula (I) and its salts of formula (Ia) by a novel process. The process comprises the reduction of a protected or unprotected prochiral β-amino acrylic acid or derivative there of, by using borane containing reducing agents at atmospheric pressure. The resulting racemic β-amino compound is resolved to a pure stereoisomer of formula (I), specifically to (2R)-4-oxo-4- [3-Ctrifluoromethyl)-5, 6-dihydrol [1,2,4]triazolo [4,3-alpyrazin-7(8H)-yl]-1-(2,4,4-trifluorophenyl)butan-2-amine. In an embodiment the invention disclosed polymorphic forms of formula (I), phosphate salt of formula (I) and also a Dibenzoyl-L-tartaric acid salt of formula (I).

6. 发明申请

WO2008056377A3 POLYMORPHIC FORMS OF RIMONABANT 审中-公开
标题翻译：多形态的多形态
公开(公告)号：WO2008056377A3
公开(公告)日：2008-10-30
申请号：PCT/IN2007000522
申请日：2007-11-05
申请人： CADILA HEALTHCARE LTD , DHOLAKIA PARIND NARENDRA , DAVE MAYANK GHANSHYAMBHAI , PANDEY BIPIN , PATEL PANKAJ RAMANBHAI
发明人： DHOLAKIA PARIND NARENDRA , DAVE MAYANK GHANSHYAMBHAI , PANDEY BIPIN , PATEL PANKAJ RAMANBHAI
IPC分类号： C07D231/14 , A61K31/4523 , A61P3/00 , A61P25/00
CPC分类号： C07D231/14
摘要： Disclosed herein are the novel amorphous hydratcd and crystalline forms of Rimonabant, process(s) for their preparation and pharmaceutical compositions containing it.
摘要翻译：本文公开了Rimonabant的新型无定形水合物和结晶形式，其制备方法和含有它的药物组合物。

7. 发明申请

WO2007144895A1 PROCESS FOR THE PREPARATION OF (S) - (+)-CLOPIDOGREL 审中-公开
标题翻译：制备（S） - （+） - 氯化碳的方法
公开(公告)号：WO2007144895A1
公开(公告)日：2007-12-21
申请号：PCT/IN2006/000465
申请日：2006-11-20
申请人： CADILA HEALTHCARE LIMITED , DHOLAKIA, Parind, Narendra , DAVE, Mayank, Ghanshyambhai , PANDEY, Bipin , LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , PATEL, Pankaj, Ramanbhai
发明人： DHOLAKIA, Parind, Narendra , DAVE, Mayank, Ghanshyambhai , PANDEY, Bipin , LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , PATEL, Pankaj, Ramanbhai
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： A process for the preparation of Methyl (+)-(S)-(2-chlorophenyl)-(6,7dihydro- 4H-thieno[3,2-c]pyridin-5-yl)acetate represented by formula (I) is disclosed. The process comprises a) contacting an amide of formula (III) with optionally substituted aryl sulfonic acid(s) and methanol; b) refluxing or heating the reaction mixture to elevated temperature for 2-40 hours; c) basifying the salt using suitable base (s) and evaporating the solvent.
摘要翻译：由式（I）表示的（+） - （S） - （2-氯苯基） - （6,7-二氢-4H-噻吩并[3,2-c]吡啶-5-基）乙酸甲酯的制备方法为披露。该方法包括a）使式（III）的酰胺与任选取代的芳基磺酸和甲醇接触; b）将反应混合物回流或加热至升高的温度2-40小时; c）使用合适的碱使盐碱化并蒸发溶剂。

8. 发明申请

WO2005063708A2 PROCESSES FOR PREPARING DIFFERENT FORMS OF (S)-(+)- CLOPIDOGREL BISULFATE 审中-公开
标题翻译：制备不同形式的（S） - （+） - 氯吡格雷二硫酸酯的方法
公开(公告)号：WO2005063708A2
公开(公告)日：2005-07-14
申请号：PCT/IN2004/000341
申请日：2004-11-02
申请人： CADILA HEALTHCARE LIMITED , LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , PANDEY, Bipin , DAVE, Mayank, Ghanshyambhai , DHOLAKIA, Parind, Narendra
发明人： LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , PANDEY, Bipin , DAVE, Mayank, Ghanshyambhai , DHOLAKIA, Parind, Narendra
IPC分类号： C07D213/00
CPC分类号： C07D495/04
摘要： The invention provides improved processes for the preparation of hydrated form of (S)-(+)-Clopidogrel bisulfate as well as improved processes for the preparation of form-I and form-II of (S)-(+)-Clopidogrel bisulfate.
摘要翻译：（S） - （+） - 氯吡格雷硫酸氢盐的水合形式的制备方法以及用于制备（S） - （+） - 氯吡格雷硫酸氢盐的形式-I和形式-II的改进方法， - （+） - 硫酸氢氯吡格雷。

9. 发明申请

WO2002059128A2 PROCESS FOR PREPARING CLOPIDOGREL 审中-公开
标题翻译：制备CLOPIDOGREL的方法
公开(公告)号：WO2002059128A2
公开(公告)日：2002-08-01
申请号：PCT/IN2002/000012
申请日：2002-01-21
申请人： CADILA HEALTHCARE LTD. , PANDEY, Bipin , LOHRAY, Vidya, Bhushan , LOHRAY, Braj, Bhushan
发明人： PANDEY, Bipin , LOHRAY, Vidya, Bhushan , LOHRAY, Braj, Bhushan
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention discloses a process for the preparation of thieno[3,2-c]pyridine derivatives of general formula (I), in either racemic or optically active (+) or (-) forms and their salts, wherein X, the substituent on benzene ring represents either a hydrogen or halogen atom such as fluorine, chlorine, bromine or iodine. The present invention also describes a process for preparing the compounds of general formula (II), in either racemic or optically active (+) or (-) forms and their salts, where X, the substituent on benzene ring represents either a hydrogen or halogen atom such as fluorine, chlorine, bromine or iodine. The compounds represented by formulae (I) and (II) have one asymmetric carbon and hence, the optically active compounds of formula (I) or of formula (ii), may be obtained either by resolving the racemic intermediate/final product or using an optically active intermediate. The compounds of the invention are pharmacologically active and have significant anti-aggregating and anti-thrombotic properties.
摘要翻译：本发明公开了制备通式（I）的噻吩并[3,2-c]吡啶衍生物的方法，其为外消旋形式或旋光形式（+）或（ - ）形式，和它们的盐，其中X是苯环上的取代基代表氢或卤原子如氟，氯，溴或碘。本发明还描述了制备外消旋或光学活性（+）或（ - ）形式及其盐的通式（II）化合物的方法，其中X为苯环上的取代基表示氢或卤素原子如氟，氯，溴或碘。由式（I）和（II）表示的化合物具有一个不对称碳，因此式（I）或式（ii）的旋光化合物可以通过拆分外消旋中间体/最终产物或使用光学活性中间体。本发明的化合物具有药理学活性并具有显着的抗聚集和抗血栓形成性质。

10. 发明申请

WO2012104869A1 TREATMENT FOR LIPODYSTROPHY 审中-公开
标题翻译： LIPODYSTROPHY的治疗
公开(公告)号：WO2012104869A1
公开(公告)日：2012-08-09
申请号：PCT/IN2012/000069
申请日：2012-01-30
申请人： CADILA HEALTHCARE LIMITED , GAMBHIRE, Dhiraj , JANI, Rajendrakumar Hariprasad , PANDEY, Bipin , SATA, Kaushik , KOTHARI, Himanshu , PATEL, Pankaj Ramanbhai
发明人： GAMBHIRE, Dhiraj , JANI, Rajendrakumar Hariprasad , PANDEY, Bipin , SATA, Kaushik , KOTHARI, Himanshu , PATEL, Pankaj Ramanbhai
IPC分类号： A61P3/00 , A61K31/40
CPC分类号： C07D207/333 , A61K9/2009 , A61K9/2013 , A61K31/40 , A61K45/06 , C07D207/33
摘要： The present invention provides a therapeutic compound of formula (I) and their pharmaceutically acceptable salts for the prevention and treatment of lipodystrophy caused because of HIV infection or combination therapy of HIV-1 protease inhibitors (Pis) and/or reverse transcriptase inhibitors (nRTIs) by neutralizing lipohypertrophy, lipoatrophy and metabolic abnormalities in HIV patient.
摘要翻译：本发明提供了用于预防和治疗HIV感染或HIV-1蛋白酶抑制剂（Pis）和/或逆转录酶抑制剂（nRTI）的联合治疗引起的脂肪营养不良的式（I）的治疗化合物及其药学上可接受的盐，通过中和艾滋病毒患者的脂肪营养不良，脂肪萎缩和代谢异常。

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