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1.发明授权公开(公告)号：US08816072B2
公开(公告)日：2014-08-26
申请号：US13375548
申请日：2010-06-02
申请人： Deepak Mohanlal Jain , Maneck Khurana , Hiten Sharadchandra Mehta , Abhay Tatiya , Asok Nath , Sanjay Mahadeo Gade , Mohan Prasad , Subhash Dhar
发明人： Deepak Mohanlal Jain , Maneck Khurana , Hiten Sharadchandra Mehta , Abhay Tatiya , Asok Nath , Sanjay Mahadeo Gade , Mohan Prasad , Subhash Dhar
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： The present invention provides a process for preparation of crystalline aprepitant having not more than 15% by weight of Form I content which comprises, a) dissolving aprepitant in a suitable solvent to obtain a solution, b) cooling the solution to 10-15° C., c) optionally seeding the solution with aprepitant Form I crystals, d) adding an anti-solvent to the solution, and e) isolating crystalline aprepitant having not more than 15% by weight of Form I content.
摘要翻译： 本发明提供一种制备具有不超过15重量％的形式I含量的结晶阿拉曲百特的方法，其包括：a）将阿瑞消制剂溶解在合适的溶剂中以获得溶液，b）将溶液冷却至10-15℃ c）任选地用溶液形式I晶体接种该溶液，d）向该溶液中加入抗溶剂，和e）分离不超过15重量％的形式I含量的结晶阿拉米特。
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2.发明申请公开(公告)号：US20120277426A1
公开(公告)日：2012-11-01
申请号：US13375548
申请日：2010-06-02
申请人： Deepak Mohanlal Jain , Maneck Khurana , Hiten Sharadchandra Mehta , Abhay Tatiya , Asok Nath , Sanjay Mahadeo Gade , Mohan Prasad , Subhash Dhar
发明人： Deepak Mohanlal Jain , Maneck Khurana , Hiten Sharadchandra Mehta , Abhay Tatiya , Asok Nath , Sanjay Mahadeo Gade , Mohan Prasad , Subhash Dhar
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： The present invention provides a process for preparation of crystalline aprepitant having not more than 15% by weight of Form I content which comprises, a) dissolving aprepitant in a suitable solvent to obtain a solution, b) cooling the solution to 10-15° C., c) optionally seeding the solution with aprepitant Form I crystals, d) adding an anti-solvent to the solution, and e) isolating crystalline aprepitant having not more than 15% by weight of Form I content.
摘要翻译： 本发明提供一种制备具有不超过15重量％的形式I含量的结晶阿拉曲百特的方法，其包括：a）将阿瑞消制剂溶解在合适的溶剂中以获得溶液，b）将溶液冷却至10-15℃ c）任选地用溶液形式I晶体接种该溶液，d）向该溶液中加入抗溶剂，和e）分离不超过15重量％的形式I含量的结晶阿拉米特。
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公开(公告)号：US20120184750A1
公开(公告)日：2012-07-19
申请号：US13321231
申请日：2010-05-20
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： The present invention provides an improved process for the preparation of olmesartan medoxomil, which is free of OLM-acid and has lower amount of eliminate and acetic acid impurity.
摘要翻译： 本发明提供了一种制备奥美沙坦酯的改进方法，其不含OLM-酸并具有较少量的消除和乙酸杂质。
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公开(公告)号：US20120184751A1
公开(公告)日：2012-07-19
申请号：US13388091
申请日：2010-07-29
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： The present invention relates to a polymorphic form of olmesartan medoxomil and a process for the preparation of crystalline olmesartan medoxomil.
摘要翻译： 本发明涉及奥美沙坦酯的多晶型物及其制备结晶奥美沙坦酯的方法。
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公开(公告)号：US20100004242A1
公开(公告)日：2010-01-07
申请号：US12089297
申请日：2006-10-05
IPC分类号： A61K31/5377 , C07D265/32 , C07D413/06
CPC分类号： C07D265/32 , C07D413/06
摘要： The present invention relates to a highly pure (2R,3S)-4-benzyl-3-(4-fluorophenyl)morpholin-2-yl 3,5-bis(trifluoromethyl)benzoate of Formula II, and a process for its preparation. The present invention further provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof, using the highly pure compound of Formula II. The present invention also provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof which comprises of cyclising the compound of Formula VII at elevated temperature, in the absence of solvent.
摘要翻译： 本发明涉及式II的高纯度（2R，3S）-4-苄基-3-（4-氟苯基）吗啉-2-基3,5-双（三氟甲基）苯甲酸酯及其制备方法。 本发明还提供使用高度纯的式II化合物制备式I的阿维地丁或其药学上可接受的盐的方法。 本发明还提供了制备式I的阿维地敏剂或其药学上可接受的盐的方法，其包括在不存在溶剂的情况下在高温下使式VII的化合物环化。
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公开(公告)号：US08080656B2
公开(公告)日：2011-12-20
申请号：US12089297
申请日：2006-10-05
IPC分类号： C07D413/02 , C07D295/00
CPC分类号： C07D265/32 , C07D413/06
摘要： The present invention relates to a highly pure (2R,3S)-4-benzyl-3-(4-fluorophenyl)morpholin-2-yl 3,5-bis(trifluoromethyl)benzoate of Formula II, and a process for its preparation. The present invention further provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof, using the highly pure compound of Formula II. The present invention also provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof which comprises of cyclising the compound of Formula VII at elevated temperature, in the absence of solvent.
摘要翻译： 本发明涉及式II的高纯度（2R，3S）-4-苄基-3-（4-氟苯基）吗啉-2-基3,5-双（三氟甲基）苯甲酸酯及其制备方法。 本发明还提供使用高度纯的式II化合物制备式I的阿维地丁或其药学上可接受的盐的方法。 本发明还提供了制备式I的阿维地敏剂或其药学上可接受的盐的方法，其包括在不存在溶剂的情况下在高温下使式VII的化合物环化。
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公开(公告)号：US07943794B2
公开(公告)日：2011-05-17
申请号：US12370249
申请日：2009-02-12
申请人： Ira Saxena , Asok Nath , Mohan Prasad
发明人： Ira Saxena , Asok Nath , Mohan Prasad
IPC分类号： C07C255/50
CPC分类号： C07C255/58 , C07C255/60 , C07D257/04
摘要： The present invention relates to processes for the preparation of intermediates of valsartan.
摘要翻译： 本发明涉及制备缬沙坦中间体的方法。
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8.发明申请Stable lamotrigine pharmaceutical compositions and processes for their preparation 审中-公开稳定的拉莫三嗪药物组合物及其制备方法公开(公告)号：US20070129549A1
公开(公告)日：2007-06-07
申请号：US10550173
申请日：2004-03-22
申请人： Yatendra Kumar , Mohan Prasad , Asok Nath , Nitin Maheshwari
发明人： Yatendra Kumar , Mohan Prasad , Asok Nath , Nitin Maheshwari
IPC分类号： C07D211/06
CPC分类号： C07D211/32 , A61K31/4465 , C07D213/50
摘要： The invention relates to processes for the preparation of piperidylmethyl-indanones, and to the use of these compounds as intermediates for the preparation of benzyl-piperidylmethyl-indanones which are active compounds for the treatment of CNS disorders. The invention also relates to a process for the preparation of donepezil or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions that include the donepezil or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明涉及制备哌啶甲基 - 茚满酮的方法，以及这些化合物作为制备作为用于治疗CNS障碍的活性化合物的苄基 - 哌啶基甲基 - 茚满酮的中间体的用途。 本发明还涉及制备多奈哌齐或其药学上可接受的盐的方法，以及包含多奈哌齐或其药学上可接受的盐的药物组合物。
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公开(公告)号：US08916713B2
公开(公告)日：2014-12-23
申请号：US13812066
申请日：2011-07-15
IPC分类号： C07D277/56
CPC分类号： C07D277/56
摘要： An improved and efficient process for the preparation of 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methylthiazole-5-carboxylic acid (febuxostat) that is substantially free from amide by-product is provided.
摘要翻译： 提供了一种改进和有效的制备基本上不含酰胺副产物的2- [3-氰基-4-（2-甲基丙氧基）苯基] -4-甲基噻唑-5-羧酸（febustostat）的方法。
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10.发明申请公开(公告)号：US20120178821A1
公开(公告)日：2012-07-12
申请号：US13388134
申请日：2010-07-30
申请人： Pranab Chatterjee , Asok Nath , Mohan Prasad
发明人： Pranab Chatterjee , Asok Nath , Mohan Prasad
IPC分类号： A61K31/138 , C07C59/265
CPC分类号： C07C217/18 , C07C59/265 , C07C213/08 , C07C213/10
摘要： The present invention provides a polymorphic form of toremifene citrate and processes for its preparation. It also relates to an improved process for the preparation of the Z isomer of the toremifene base, free of E isomer, and its pharmaceutically acceptable salts.
摘要翻译： 本发明提供了一种多晶型托伐米芬柠檬酸盐及其制备方法。 本发明还涉及制备不含E异构体的托瑞米芬碱的Z异构体及其药学上可接受的盐的改进方法。
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