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1.发明申请SUBSTANTIALLY PURE SALTS OF FEBUXOSTAT AND PROCESSES FOR PREPARATION THEREOF 审中-公开FEBUXOSTAT的主要纯盐及其制备方法公开(公告)号：US20130190366A1
公开(公告)日：2013-07-25
申请号：US13579418
申请日：2011-02-18
IPC分类号： C07D277/56
CPC分类号： C07D277/56
摘要： Substantially pure salts of febuxostat of Formula (IA): wherein Y is Na+, K+, Li+, Mg2+, Ca2+, Zn2+, Ba2+, Sr2+, choline, epolamine and N+(R)4 and processes for preparation thereof are disclosed.
摘要翻译： 公开了式（IA）的Febostostat的基本纯盐：其中Y是Na +，K +，Li +，Mg 2+，Ca 2+，Zn 2+，Ba 2+，Sr 2+，胆碱，亚胺胺和N +（R）4及其制备方法。
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公开(公告)号：US08933123B2
公开(公告)日：2015-01-13
申请号：US13252387
申请日：2011-10-04
IPC分类号： A61K31/205 , C07C215/64 , A61K31/137 , C07C55/10
CPC分类号： C07C215/64 , A61K31/137 , C07B2200/13 , C07C55/10 , C07C2601/14
摘要： The present invention discloses polymorphic forms of O-desmethyl-venlafaxine succinate and processes for the preparation thereof.
摘要翻译： 本发明公开了O-去甲基 - 文拉法辛琥珀酸酯的多晶型物及其制备方法。
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公开(公告)号：US20140378682A1
公开(公告)日：2014-12-25
申请号：US14343785
申请日：2012-09-10
申请人： Shriprakash Dhar Dwivedi , Ashok Prasad , Daya Ram Pal , Mukul Hari Prasad Sharma , Kuldeep Natwarlal Jain , Naitik Bharatbhai Patel
发明人： Shriprakash Dhar Dwivedi , Ashok Prasad , Daya Ram Pal , Mukul Hari Prasad Sharma , Kuldeep Natwarlal Jain , Naitik Bharatbhai Patel
IPC分类号： C07D413/14 , C07D413/10 , C07D265/32
CPC分类号： C07D413/14 , C07D265/32 , C07D413/10
摘要： The invention discloses processes for the preparation of rivaroxaban and its pharmaceutically acceptable salts, solvates, and hydrates thereof. The invention also relates to novel intermediates for the preparation of rivaroxaban.
摘要翻译： 本发明公开了制备利伐沙班及其药学上可接受的盐，溶剂化物和水合物的方法。 本发明还涉及用于制备利伐沙班的新型中间体。
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公开(公告)号：US20130197260A1
公开(公告)日：2013-08-01
申请号：US13818791
申请日：2011-08-25
IPC分类号： C07C219/28 , C07C213/00 , C07C213/10 , C07C303/28 , C07C309/67 , C07C213/06 , C07C213/08
CPC分类号： C07C219/28 , C07B2200/07 , C07B2200/13 , C07C41/26 , C07C51/43 , C07C59/56 , C07C67/03 , C07C213/00 , C07C213/06 , C07C213/08 , C07C213/10 , C07C217/62 , C07C303/28 , C07C309/66 , C07C309/67 , C07C215/54 , C07C43/23 , C07C69/734
摘要： The invention relates to improved process for the preparation of fesoterodine and its pharmaceutically acceptable salt, specifically fesoterodine fumarate of formula (1). The invention relates to solid state forms of a novel salt of fesoterodine and process for the preparation thereof. The invention also relates to highly pure fesoterodine fumarate substantially free of impurity X at RRT 1.37. The invention also provides solid particles of pure fesoterodine fumarate wherein 90 volume-percent of the particles (D90) have a size of higher than 200 microns.
摘要翻译： 本发明涉及制备非索特罗及其药学上可接受的盐，特别是式（1）的富马酸弗索塔罗汀的改进方法。 本发明涉及非索罗定新型盐的固态形式及其制备方法。 本发明还涉及在RRT 1.37基本上不含杂质X的高纯度富马酸菲索特罗。 本发明还提供富马酸纯的富特罗定的固体颗粒，其中90体积％的颗粒（D90）具有高于200微米的尺寸。
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公开(公告)号：US09012678B2
公开(公告)日：2015-04-21
申请号：US13818791
申请日：2011-08-25
IPC分类号： C07C69/76 , C07C219/28 , C07C41/26 , C07C51/43 , C07C59/56 , C07C67/03 , C07C213/10 , C07C217/62 , C07C309/66 , C07C213/00 , C07C213/06 , C07C213/08 , C07C303/28 , C07C309/67
CPC分类号： C07C219/28 , C07B2200/07 , C07B2200/13 , C07C41/26 , C07C51/43 , C07C59/56 , C07C67/03 , C07C213/00 , C07C213/06 , C07C213/08 , C07C213/10 , C07C217/62 , C07C303/28 , C07C309/66 , C07C309/67 , C07C215/54 , C07C43/23 , C07C69/734
摘要： The invention relates to improved process for the preparation of fesoterodine and its pharmaceutically acceptable salt, specifically fesoterodine fumarate of formula (1). The invention relates to solid state forms of a novel salt of fesoterodine and process for the preparation thereof. The invention also relates to highly pure fesoterodine fumarate substantially free of impurity X at RRT 1.37. The invention also provides solid particles of pure fesoterodine fumarate wherein 90 volume-percent of the particles (D90) have a size of higher than 200 microns.
摘要翻译： 本发明涉及制备非索特罗及其药学上可接受的盐，特别是式（1）的富马酸弗索塔罗汀的改进方法。 本发明涉及非索罗定新型盐的固态形式及其制备方法。 本发明还涉及在RRT 1.37基本上不含杂质X的高纯度富马酸菲索特罗。 本发明还提供富马酸纯的富特罗定的固体颗粒，其中90体积％的颗粒（D90）具有高于200微米的尺寸。
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6.发明授权Intermediates for the preparation of HMG CoA reductase inhibitors and processes for the preparation thereof 失效用于制备HMG CoA还原酶抑制剂的中间体及其制备方法公开(公告)号：US08759518B2
公开(公告)日：2014-06-24
申请号：US13576296
申请日：2011-02-23
IPC分类号： C07D239/02 , C07D405/12 , C07D239/42 , C07D405/06 , C07D257/04
CPC分类号： C07D405/12 , C07D239/42 , C07D257/04 , C07D405/06 , Y02P20/55
摘要： A compound of Formula (1), is disclosed wherein P1 and P2 are alcohol protecting groups or 1,3-diol protecting group, R is selected from: wherein R4a is selected from alkyl, aryl, arylalkyl and cycloalkyl, Rc is selected from H, alkyl, aryl, alkaoxy, haloalkyl, monohaloalkyloxy, and dihaloalkyloxy, Rd is selected from alkyl, aryl, arylalkyl, CF3, halo and NO2 and X is selected from O, N—H, N-alkyl and S, Ra and Rb are same or different and each represents hydrogen, an alkyl group of 1 to 12 carbon atoms, an aryl group of 6 to 12 carbon atoms, or an aralkyl group of 7 to 12 carbon atoms.
摘要翻译： 公开了式（1）的化合物，其中P1和P2是醇保护基或1,3-二醇保护基，R选自：其中R 4a选自烷基，芳基，芳烷基和环烷基，R c选自H 烷基，芳基，烷氧基，卤代烷基，单卤代烷氧基和二卤烷氧基，Rd选自烷基，芳基，芳基烷基，CF 3，卤素和NO 2，X选自O，N-H，N-烷基和S， 相同或不同，各自表示氢，1至12个碳原子的烷基，6至12个碳原子的芳基或7至12个碳原子的芳烷基。
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7.发明申请INTERMEDIATES FOR THE PREPARATION OF HMG COA REDUCTASE INHIBITORS AND PROCESSES FOR THE PREPARATION THEREOF 失效制备HMG COA还原酶抑制剂的中间体及其制备方法公开(公告)号：US20130158263A1
公开(公告)日：2013-06-20
申请号：US13576296
申请日：2011-02-23
IPC分类号： C07D405/12 , C07D405/06 , C07D239/42 , C07D257/04
CPC分类号： C07D405/12 , C07D239/42 , C07D257/04 , C07D405/06 , Y02P20/55
摘要： A compound of Formula (1), is disclosed wherein P1 and P2 are alcohol protecting groups or 1,3-diol protecting group, R is selected from: wherein R4a is selected from alkyl, aryl, arylalkyl and cycloalkyl, Rc is selected from H, alkyl, aryl, alkaoxy, haloalkyl, monohaloalkyloxy, and dihaloalkyloxy, Rd is selected from alkyl, aryl, arylalkyl, CF3, halo and NO2 and X is selected from O, N—H, N-alkyl and S, Ra and Rb are same or different and each represents hydrogen, an alkyl group of 1 to 12 carbon atoms, an aryl group of 6 to 12 carbon atoms, or an aralkyl group of 7 to 12 carbon atoms.
摘要翻译： 公开了式（1）的化合物，其中P1和P2是醇保护基或1,3-二醇保护基，R选自：其中R 4a选自烷基，芳基，芳烷基和环烷基，R c选自H 烷基，芳基，烷氧基，卤代烷基，单卤代烷氧基和二卤烷氧基，Rd选自烷基，芳基，芳基烷基，CF 3，卤素和NO 2，X选自O，NH，N-烷基和S，R a和R b相同或 各自表示氢，1〜12个碳原子的烷基，6〜12个碳原子的芳基或7〜12个碳原子的芳烷基。
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公开(公告)号：US09034901B2
公开(公告)日：2015-05-19
申请号：US13818681
申请日：2011-08-24
IPC分类号： C07D215/14
CPC分类号： C07D215/14
摘要： The invention provides the process for the preparation of pitavastatin and its pharmaceutically acceptable salts thereof. In particular, the invention provides a process for the preparation of stable pitavastatin calcium in crystalline form having water content less than 5% wt/wt. The present invention also provides stable crystalline form of pitavastatin calcium substantially free from crystal Form-A and use thereof for pharmaceutical compositions.
摘要翻译： 本发明提供了匹伐他汀及其药学上可接受的盐的制备方法。 特别地，本发明提供了制备水含量小于5％wt / wt的结晶形式的稳定匹伐他汀钙的方法。 本发明还提供基本上不含晶形A的匹伐他汀钙的稳定结晶形式及其用于药物组合物的用途。
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公开(公告)号：US20100113784A1
公开(公告)日：2010-05-06
申请号：US12443299
申请日：2007-09-24
申请人： Niraj Shyamlal Shah , Shriprakash Dhar Dwivedi , Kishorkumar Maneklal Vinchhi , Sathya Varahala Raju Nadimpally
发明人： Niraj Shyamlal Shah , Shriprakash Dhar Dwivedi , Kishorkumar Maneklal Vinchhi , Sathya Varahala Raju Nadimpally
IPC分类号： C07D401/12
CPC分类号： C07D215/22
摘要： The present invention relates the process for preparation of stable polymorph of aripiprazole and in particular the present invention is related to an improved process for the preparation of crystalline anhydrous aripiprazole and its hydrochloride salt.
摘要翻译： 本发明涉及制备阿立哌唑稳定多晶型物的方法，特别是本发明涉及制备结晶无水阿立哌唑及其盐酸盐的改进方法。
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公开(公告)号：US20140148481A1
公开(公告)日：2014-05-29
申请号：US13818681
申请日：2011-08-24
IPC分类号： C07D215/14
CPC分类号： C07D215/14
摘要： The invention provides the process for the preparation of pitavastatin and its pharmaceutically acceptable salts thereof. In particular, the invention provides a process for the preparation of stable pitavastatin calcium in crystalline form having water content less than 5% wt/wt. The present invention also provides stable crystalline form of pitavastatin calcium substantially free from crystal Form-A and use thereof for pharmaceutical compositions.
摘要翻译： 本发明提供了匹伐他汀及其药学上可接受的盐的制备方法。 特别地，本发明提供了制备水含量小于5％wt / wt的结晶形式的稳定匹伐他汀钙的方法。 本发明还提供基本上不含晶形A的匹伐他汀钙的稳定结晶形式及其用于药物组合物的用途。
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