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1. 发明授权

US07897613B2 Crystalline polymorphs of clopidogrel 有权
标题翻译：氯吡格雷的结晶多晶型物
公开(公告)号：US07897613B2
公开(公告)日：2011-03-01
申请号：US10571419
申请日：2004-09-09
申请人： Ramakrishnan Arul , Ajay Singh Rawat , Maheshkumar Gadakar , Rajesh Rao , Abhinay Pise , Jason Gray
发明人： Ramakrishnan Arul , Ajay Singh Rawat , Maheshkumar Gadakar , Rajesh Rao , Abhinay Pise , Jason Gray
IPC分类号： C07D495/04 , A61K31/4365 , A61P7/02
CPC分类号： C07D495/04
摘要： The present invention relates to novel crystalline forms of the platelet aggregation inhibitor (+)-(S)-methyl-2-(2-chlorophenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetate, clopidogrel (1), in the form of hydrogen bromide salts, identified as polymorph forms 1, 2 and 3. The present invention further relates to processes for preparing such forms, pharmaceutical compositions comprising such forms, and uses for such forms and compositions. The pharmaceutical compositions may be used, in particular, for inhibiting platelet aggregation or for treating, preventing or managing thrombosis, atherothrombosis, an atherothrombotic event, ischaemic stroke, myocardial infarction, non-Q-wave myocardial infarction, atherosclerosis, peripheral arterial disease, or unstable angina. The present invention also relates to methods of treating said disorders. Formula (1).
摘要翻译：本发明涉及血小板聚集抑制剂（+） - （S） - 甲基-2-（2-氯苯基） - （6,7-二氢-4H-噻吩并[3,2-c]吡啶-3-基）（1），以溴化氢的形式，被鉴定为多晶型形式1,2和3.本发明还涉及制备这些形式的方法，包含这些形式的药物组合物和用于这种形式和组成。药物组合物可特别用于抑制血小板聚集或治疗，预防或控制血栓形成，动脉粥样硬化血栓形成，动脉粥样硬化血栓形成事件，缺血性中风，心肌梗塞，非Q波心肌梗塞，动脉粥样硬化，外周动脉疾病或不稳定型心绞痛本发明还涉及治疗所述疾病的方法。公式1）。

2. 发明申请

US20070281964A1 Novel Crystalline Polymorphs of Clopidogrel 有权
标题翻译：氯吡格雷的新型结晶多晶型物
公开(公告)号：US20070281964A1
公开(公告)日：2007-12-06
申请号：US10571419
申请日：2004-09-09
申请人： Ramakrishnan Arul , Ajay Rawat , Maheshkumar Gadakar , Rajesh Rao , Abhinay Pise , Jason Gray
发明人： Ramakrishnan Arul , Ajay Rawat , Maheshkumar Gadakar , Rajesh Rao , Abhinay Pise , Jason Gray
IPC分类号： A61K31/4365 , A61P7/02 , C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to novel crystalline forms of the platelet aggregation inhibitor (+)-(S)-methyl-2-(2-chlorophenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetate, clopidogrel (1), in the form of hydrogen bromide salts, identified as polymorph forms 1, 2 and 3. The present invention further relates to processes for preparing such forms, pharmaceutical compositions comprising such forms, and uses for such forms and compositions. The pharmaceutical compositions may be used, in particular, for inhibiting platelet aggregation or for treating, preventing or managing thrombosis, atherothrombosis, an atherothrombotic event, ischaemic stroke, myocardial infarction, non-Q-wave myocardial infarction, atherosclerosis, peripheral arterial disease, or unstable angina. The present invention also relates to methods of treating said disorders. Formula (1).
摘要翻译：本发明涉及血小板聚集抑制剂（+） - （S） - 甲基-2-（2-氯苯基） - （6,7-二氢-4H-噻吩并[3,2-c]吡啶-3-基）（1），以溴化氢的形式，被鉴定为多晶型形式1,2和3.本发明还涉及制备这些形式的方法，包含这些形式的药物组合物和用于这种形式和组成。药物组合物可特别用于抑制血小板聚集或治疗，预防或控制血栓形成，动脉粥样硬化血栓形成，动脉粥样硬化血栓形成事件，缺血性卒中，心肌梗死，非Q波心肌梗塞，动脉粥样硬化，外周动脉疾病或不稳定型心绞痛本发明还涉及治疗所述疾病的方法。公式1）。

3. 发明申请

US20050049415A1 Process for preparing enantiomerically pure alpha phenyl-alpha (6,7-dihydro-4h-thieno[3,2-c]pyridin-5-yl)-acetic acid derivatives 审中-公开
标题翻译：制备对映体纯的α-苯基-α（6,7-二氢-4H-噻吩并[3,2-c]吡啶-5-基） - 乙酸衍生物的方法
公开(公告)号：US20050049415A1
公开(公告)日：2005-03-03
申请号：US10493994
申请日：2002-10-28
申请人： Ramakrishna Arul , Rawat Ajaysingh , Mahesh Gadakar , Abhinay Pise , Rajesh Rao , Jayaraman Raman
发明人： Ramakrishna Arul , Rawat Ajaysingh , Mahesh Gadakar , Abhinay Pise , Rajesh Rao , Jayaraman Raman
IPC分类号： C07D495/04 , C07D498/02
CPC分类号： C07D495/04 , C07B2200/07
摘要： A process for preparing a substantially enantiomerically pure compound of formula (IV), or a pharmaceutically acceptable salt thereof wherein: R is hydrogen or a Cl alkyl group and X, Y and Z are any atom or group, comprising a step of isolating a substantially enantiomerically pure compound of formula (V) wherein: R3 is CN or C(O)NR1R2 and R1 and R2 are each independently hydrogen or a C1-C4 alkyl group, or, together with the nitrogen in the C(O)NR1R2 group, form a ring that includes 2-6 carbon atoms, from a racemate of formula (V) and converting the substantially enantiomerically pure compound of formula (V) into a substantially enantiomerically pure compound of formula (IV).
摘要翻译：制备基本上对映体纯的式（IV）化合物或其药学上可接受的盐的方法，其中：R是氢或C1烷基，X，Y和Z是任何原子或基团，包括基本上分离对映体纯的式（Ⅴ）化合物，其中：R 3为CN或C（O）NR 1 R 2，R 1和R 2各自独立地为氢或C 1 -C 4烷基，或者与C（O）NR 1 R 2基团中的氮一起，由式（V）的外消旋物形成包含2-6个碳原子的环，并将基本上对映体纯的式（V）化合物转化为基本上对映体纯的式（IV）化合物。

4. 发明授权

US08471039B2 Process for the preparation of indoline derivatives and their intermediates thereof 有权
标题翻译：二氢吲哚衍生物及其中间体的制备方法
公开(公告)号：US08471039B2
公开(公告)日：2013-06-25
申请号：US13392564
申请日：2010-09-13
申请人： Shreerang Joshi , Sachin Bhuta , Sanjay Talukdar , Sudhir Sawant , Deepak Venkataraman , Abhinay Pise , Shashikant Metkar , Dattatraya Chavan , Parven Kumar Luthra
发明人： Shreerang Joshi , Sachin Bhuta , Sanjay Talukdar , Sudhir Sawant , Deepak Venkataraman , Abhinay Pise , Shashikant Metkar , Dattatraya Chavan , Parven Kumar Luthra
IPC分类号： C07D209/08
CPC分类号： C07D209/08 , C07D317/22
摘要： Processes for the preparation of Silodosin and its intermediates comprising reductive amination of compound of Formula (VIII) with a compound of Formula (VII) or a compound of Formula (XV) in a suitable solvent using a reducing agent.
摘要翻译：制备Silodosin及其中间体的方法包括使用还原剂在合适的溶剂中将式（Ⅷ）化合物与式（Ⅶ）化合物或式（ⅩⅤ）化合物还原胺化。

5. 发明申请

US20120165548A1 PROCESS FOR THE PREPARATION OF INDOLINE DERIVATIVES AND THEIR INTERMEDIATES THEREOF 有权
标题翻译：制备吲哚衍生物的方法及其中间体
公开(公告)号：US20120165548A1
公开(公告)日：2012-06-28
申请号：US13392564
申请日：2010-09-13
申请人： Shreerang Joshi , Sachin Bhuta , Sanjay Talukdar , Sudhir Sawant , Deepak Venkataraman , Abhinay Pise , Shashikant Metkar , Dattatraya Chavan , Parven Kumar Luthra
发明人： Shreerang Joshi , Sachin Bhuta , Sanjay Talukdar , Sudhir Sawant , Deepak Venkataraman , Abhinay Pise , Shashikant Metkar , Dattatraya Chavan , Parven Kumar Luthra
IPC分类号： C07D209/08 , C07D317/22 , C07C45/81 , C07C47/277 , C07C45/80
CPC分类号： C07D209/08 , C07D317/22
摘要： Processes for the preparation of Silodosin and its intermediates comprising reductive amination of compound of Formula (VIII) with a compound of Formula (VII) or a compound of Formula (XV) in a suitable solvent using a reducing agent.
摘要翻译：制备Silodosin及其中间体的方法包括使用还原剂在合适的溶剂中将式（Ⅷ）化合物与式（Ⅶ）化合物或式（ⅩⅤ）化合物还原胺化。

6. 发明申请

US20070276012A1 Process for Preparing Thiazolidinediones 失效
标题翻译：噻唑烷二酮的制备方法
公开(公告)号：US20070276012A1
公开(公告)日：2007-11-29
申请号：US10577121
申请日：2004-10-27
申请人： Sudhir Nambiar , Abhinay Pise
发明人： Sudhir Nambiar , Abhinay Pise
IPC分类号： A61K31/44 , A61P3/00 , C07D417/00
CPC分类号： C07D405/12 , C07D417/12
摘要： This invention provides a process for reducing an exocyclic double bond at the 5-position of a thiazolidinedione moiety of a thiazolidinedione precursor comprising the steps of: a) preparing a solution or suspension of the thiazolidinedione precursor in a non-ether solvent medium with a base, and b) combining the solution or suspension with a dithionite source. Preferred solvent media include aqueous N,N-dimethylformamide. Sodium dithionite is a preferred dithionite source.
摘要翻译：本发明提供了一种减少噻唑烷二酮前体的噻唑烷二酮部分5-位上的环外双键的方法，包括以下步骤：a）在非醚溶剂介质中制备噻唑烷二酮前体与碱的溶液或悬浮液，和b）将溶液或悬浮液与连二亚硫酸盐源组合。优选的溶剂介质包括N，N-二甲基甲酰胺水溶液。连二亚硫酸钠是优选的连二亚硫酸盐源。

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