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    Angiotensin II Receptor Antagonists
    3.
    发明申请
    Angiotensin II Receptor Antagonists 审中-公开
    血管紧张素II受体拮抗剂

    公开(公告)号：US20090123538A1

    公开(公告)日：2009-05-14

    申请号：US11886553

    申请日：2006-04-14

    申请人： Laman L. Alani ,  David C. Dubost ,  Bruce S. Foster ,  Soumojeet Ghosh ,  Hossain Jahansouz ,  Nazaneen Pourkavoos ,  Bhagwant Rege ,  Aditya Tatavarti

    发明人： Laman L. Alani ,  David C. Dubost ,  Bruce S. Foster ,  Soumojeet Ghosh ,  Hossain Jahansouz ,  Nazaneen Pourkavoos ,  Bhagwant Rege ,  Aditya Tatavarti

    IPC分类号： A61K9/20 ,  C07D257/04 ,  A61K31/41 ,  A61P9/12 ,  A61K9/16

    CPC分类号： C07D403/10

    摘要： The compounds of the present invention are polymorphic crystalline forms of the compound 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid, which has the structure (I). Specifically, the compounds of the invention are selected from the group consisting of 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid of Claim 3 selected from the group consisting of 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form I, 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form II, 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form III, and 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form IV, 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form V, 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VI, 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VII, and 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VIII.

    摘要翻译： 本发明的化合物是2-丁基-4-氯-1 - （（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-1-基的化合物的多晶型形式， 其具有结构（I）。 具体地说，本发明化合物选自2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑 -5-羧酸，其选自2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑 -5-甲酸盐酸盐形式I，2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸 盐酸盐形式II，2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸盐酸盐形式III和 2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式IV，2-丁基-4 - 氯 - 1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式V，2-丁基-4-氯-1- 甲基] - 咪唑-5-羧酸一水合物形式VI，2-丁基-4-氯-1 - [（2' - （1H-四唑-5-基）联苯-4-基） （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5- c 羧酸一水合物形式VII和2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式 八，

    Taste-Masked Tablets and Granules
    4.
    发明申请
    Taste-Masked Tablets and Granules 审中-公开
    味道掩蔽的片剂和颗粒

    公开(公告)号：US20090136570A1

    公开(公告)日：2009-05-28

    申请号：US12087827

    申请日：2007-01-16

    申请人： Bhagwant Rege ,  Kimberly Kaighn ,  Soumojeet Ghosh ,  Laman Alani

    发明人： Bhagwant Rege ,  Kimberly Kaighn ,  Soumojeet Ghosh ,  Laman Alani

    IPC分类号： A61K9/20 ,  A61K31/513 ,  A61K31/519 ,  A61P31/18 ,  A61K31/506

    CPC分类号： A61K9/2054 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2095 ,  A61K31/70

    摘要： Orally administered, taste-masked tablets and granules contain (a) a hydroxypyrimidinone carboxamide, a hydroxy-tetrahydropyridopyrimidinone carboxamide, or a related carboxamide compound, or a pharmaceutically acceptable salt thereof, (b) a taste-masking polymer, (c) a superdisintegrant, and optionally other excipients. The carboxamide compound is an HIV integrase inhibitor, and the tablets and granules are suitable for use in the inhibition of HIV integrase, the treatment or prophylaxis of HIV infection, and the treatment or prophylaxis or delay in the onset of AIDS.

    摘要翻译： 口服给药的掩味片和颗粒剂含有（a）羟基嘧啶酮羧酰胺，羟基四氢吡啶并嘧啶酮羧酰胺或相关的羧酰胺化合物或其药学上可接受的盐，（b）掩味聚合物，（c）超级崩解剂 ，和任选的其它赋形剂。 甲酰胺化合物是HIV整合酶抑制剂，片剂和颗粒剂适用于抑制HIV整合酶，治疗或预防HIV感染，以及治疗或预防或延迟艾滋病的发作。