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1. 发明申请

US20120201885A1 PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH PIOGLITAZONE 审中-公开
标题翻译： DIPEPTIDYL PEPTIDASE-4抑制剂与PIOGLITAZONE组合的药物组合物
公开(公告)号：US20120201885A1
公开(公告)日：2012-08-09
申请号：US13501252
申请日：2010-10-12
申请人： Nicholas Birringer , Christopher T. John , Zhen Liu , Adam Procopio , Bhagwant Rege
发明人： Nicholas Birringer , Christopher T. John , Zhen Liu , Adam Procopio , Bhagwant Rege
IPC分类号： A61K9/20 , A61K31/675 , A61P3/10 , A61K31/513 , A61K31/4439 , A61K9/28 , A61K31/4985
CPC分类号： A61K45/06 , A61K9/209
摘要： This invention relates to a bilayer pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and pioglitazone, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.
摘要翻译：本发明涉及包含二肽基肽酶-4抑制剂和吡格列酮的固定剂量组合的双层药物组合物，制备这种药物组合物的方法以及用这种药物组合物治疗2型糖尿病的方法。

2. 发明申请

US20120059011A1 PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH PIOGLITAZONE 审中-公开
标题翻译： DIPEPTIDYL PEPTIDASE-4抑制剂与PIOGLITAZONE的组合药物组合物
公开(公告)号：US20120059011A1
公开(公告)日：2012-03-08
申请号：US13319718
申请日：2010-06-04
申请人： Nicholas Birringer , Christopher T. John , Adam Procopio , Bhagwant Rege , Lawrence A. Rosen , Sutthilug Sotthivirat , Wei Xu
发明人： Nicholas Birringer , Christopher T. John , Adam Procopio , Bhagwant Rege , Lawrence A. Rosen , Sutthilug Sotthivirat , Wei Xu
IPC分类号： A61K31/4439 , A61K31/513 , A61P3/10 , A61K31/4985
CPC分类号： A61K45/06 , A61K31/44 , A61K31/4439 , A61K2300/00
摘要： This invention relates to pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and pioglitazone, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.
摘要翻译：本发明涉及包含二肽基肽酶-4抑制剂和吡格列酮的固定剂量组合的药物组合物，制备这种药物组合物的方法，以及用这种药物组合物治疗2型糖尿病的方法。

3. 发明授权

US08003672B2 CB-1 receptor modulator formulations 失效
标题翻译： CB-1受体调节剂制剂
公开(公告)号：US08003672B2
公开(公告)日：2011-08-23
申请号：US12386402
申请日：2009-04-17
申请人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
发明人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
IPC分类号： A61K31/44
CPC分类号： A61K31/44 , A61K9/1635 , A61K9/2027 , A61K31/4985 , A61K45/06 , A61K2300/00
摘要： Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabiniod inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.
摘要翻译：本文描述的是大麻素受体反向激动剂如塔拉班班特的固体，稳定的药物制剂，以及制备这些制剂的方法。另外，本文所述是大麻逆反向激动剂如塔拉班班特和另外的治疗剂的固体稳定药物制剂，以及制备这种药物制剂的方法。

4. 发明申请

US20090264436A1 CB-1 receptor modulator formulations 失效
标题翻译： CB-1受体调节剂制剂
公开(公告)号：US20090264436A1
公开(公告)日：2009-10-22
申请号：US12386402
申请日：2009-04-17
申请人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
发明人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
IPC分类号： A61K31/4985 , A61K31/44
CPC分类号： A61K31/44 , A61K9/1635 , A61K9/2027 , A61K31/4985 , A61K45/06 , A61K2300/00
摘要： Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabiniod inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.
摘要翻译：本文描述的是大麻素受体反向激动剂如塔拉班班特的固体，稳定的药物制剂，以及制备这些制剂的方法。另外，本文所述是大麻逆反向激动剂如塔拉班班特和另外的治疗剂的固体稳定药物制剂，以及制备这种药物制剂的方法。

5. 发明授权

US08486983B2 Self-emulsifying formulations of CETP inhibitors 有权
标题翻译： CETP抑制剂的自乳化制剂
公开(公告)号：US08486983B2
公开(公告)日：2013-07-16
申请号：US12085745
申请日：2006-12-05
申请人： Agam R. Sheth , Bhagwant Rege , Soumojeet Ghosh , Laman L. Alani , Maria T. Cruanes , Craig A. McKelvey
发明人： Agam R. Sheth , Bhagwant Rege , Soumojeet Ghosh , Laman L. Alani , Maria T. Cruanes , Craig A. McKelvey
IPC分类号： A61K31/421
CPC分类号： A61K9/08 , A61K9/4858 , A61K31/421 , A61K47/10 , A61K47/26 , A61K47/44
摘要： A liquid formulation for oral administration of the CETP inhibitor of formula (I) has improved bioavailability compared with conventional solid formulations. The formulation comprises the CETP inhibitor, or a pharmaceutically acceptable salt thereof; an oil; and one or more nonionic surfactants having a hydrophilic lipophilic balance (HLB)>10.
摘要翻译：用于口服给予式（I）的CETP抑制剂的液体制剂与常规固体制剂相比具有改善的生物利用度。该制剂包含CETP抑制剂或其药学上可接受的盐; 一油和一种或多种亲水亲油平衡（HLB）> 10的非离子表面活性剂。

6. 发明申请

US20110065800A1 FORMULATIONS FOR CATHEPSIN K INHIBITORS 审中-公开
标题翻译：卡贝汀K抑制剂的配方
公开(公告)号：US20110065800A1
公开(公告)日：2011-03-17
申请号：US12992124
申请日：2009-05-06
申请人： Haihong Fan , Majid Mahjour , Justin Moser , Bhagwant Rege
发明人： Haihong Fan , Majid Mahjour , Justin Moser , Bhagwant Rege
IPC分类号： A61K31/165 , A61P19/10 , A61P29/00 , A61P19/00 , A61P3/04 , A61P27/06 , A61P35/00
CPC分类号： A61K47/38 , A61K9/10 , A61K9/2018 , A61K9/2054 , A61K31/275 , A61K31/424 , A61K31/44 , A61K47/32 , Y10S514/96 , Y10S514/961
摘要： The instant invention relates to pharmaceutical compositions containing cathepsin K inhibitors. Also disclosed are processes for making said pharmaceutical compositions.
摘要翻译：本发明涉及含有组织蛋白酶K抑制剂的药物组合物。还公开了制备所述药物组合物的方法。

7. 发明申请

US20090186926A1 Self-Emulsifying Formulations of CETP Inhibitors 有权
标题翻译： CETP抑制剂的自乳化制剂
公开(公告)号：US20090186926A1
公开(公告)日：2009-07-23
申请号：US12085745
申请日：2006-12-05
申请人： Agam R. Sheth , Bhagwant Rege , Soumojeet Ghosh , Laman L. Alani , Maria T. Cruanes , Craig A. Mckelvey
发明人： Agam R. Sheth , Bhagwant Rege , Soumojeet Ghosh , Laman L. Alani , Maria T. Cruanes , Craig A. Mckelvey
IPC分类号： A61K31/421
CPC分类号： A61K9/08 , A61K9/4858 , A61K31/421 , A61K47/10 , A61K47/26 , A61K47/44
摘要： A liquid formulation for oral administration of the CETP inhibitor of formula (I) has improved bioavailability compared with conventional solid formulations. The formulation comprises the CETP inhibitor, or a pharmaceutically acceptable salt thereof; an oil; and one or more nonionic surfactants having a hydrophilic lipophilic balance (HLB)>10.
摘要翻译：用于口服给予式（I）的CETP抑制剂的液体制剂与常规固体制剂相比具有改善的生物利用度。该制剂包含CETP抑制剂或其药学上可接受的盐; 一油和一种或多种亲水亲油平衡（HLB）> 10的非离子表面活性剂。

8. 发明申请

US20090264476A1 CB-1 receptor modulator formulations 审中-公开
标题翻译： CB-1受体调节剂制剂
公开(公告)号：US20090264476A1
公开(公告)日：2009-10-22
申请号：US12386403
申请日：2009-04-17
申请人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
发明人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
IPC分类号： A61K31/44 , A61K31/4985 , A61P3/04
CPC分类号： A61K31/44 , A61K9/1635 , A61K9/1652 , A61K9/1694 , A61K9/2077 , A61K9/2095 , A61K31/4412 , A61K45/06 , A61K2300/00
摘要： Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabinoid inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.
摘要翻译：本文描述的是大麻素受体反向激动剂如塔拉班班特的固体，稳定的药物制剂，以及制备这些制剂的方法。另外，本文描述的是大麻素反向激动剂如塔拉班班特和另外的治疗剂的固体稳定药物制剂，以及制备这种药物制剂的方法。

9. 发明申请

US20090136570A1 Taste-Masked Tablets and Granules 审中-公开
标题翻译：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。

10. 发明申请

US20090123538A1 Angiotensin II Receptor Antagonists 审中-公开
标题翻译：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，

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