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31. 发明授权

US08048452B2 Pharmaceutical compositions of cholesteryl ester transfer protein inhibitor 有权
标题翻译：胆固醇酯转运蛋白抑制剂的药物组合物
公开(公告)号：US08048452B2
公开(公告)日：2011-11-01
申请号：US11421888
申请日：2006-06-02
申请人： William J. Curatolo , Dwayne T. Friesen , Michael J. Gumkowski , Douglas A. Lorenz , James A. S. Nightingale , Roger B. Ruggeri , Ravi M. Shanker
发明人： William J. Curatolo , Dwayne T. Friesen , Michael J. Gumkowski , Douglas A. Lorenz , James A. S. Nightingale , Roger B. Ruggeri , Ravi M. Shanker
IPC分类号： A01N25/34 , A61K9/14 , A61K9/22 , A61K9/48 , A61K47/32 , A61K31/21 , A61K31/19 , A61K31/715
CPC分类号： A61K9/1652 , A61K9/146 , A61K9/1635 , A61K31/4196 , A61K31/47
摘要： A pharmaceutical composition comprises a solid amorphous dispersion of a cholesteryl ester transfer protein inhibitor and a concentration-enhancing polymer.
摘要翻译：药物组合物包含胆固醇酯转移蛋白抑制剂和浓度增强聚合物的固体无定形分散体。

32. 发明申请

US20080293801A1 Solid Amorphous Dispersions of An Mtp Inhibitor For Treatment of Obesity 审中-公开
标题翻译：用于治疗肥胖的Mtp抑制剂的固体无定形分散体
公开(公告)号：US20080293801A1
公开(公告)日：2008-11-27
申请号：US10595732
申请日：2004-11-01
申请人： Dwayne T. Friesen , Ravi M. Shanker
发明人： Dwayne T. Friesen , Ravi M. Shanker
IPC分类号： A61K31/404 , A61P3/04
CPC分类号： A61K9/1652 , A61K9/1688 , A61K31/404
摘要： A composition comprises a solid amorphous dispersion comprising (S)—N-{2-[benzyl(methyl)amino]-2-oxo-1-phenylethyl}-methyl-5-[4′-(trifluoromethyl)[1,1′-biphenyl]-2-carboxamido]-1H-indole-2-carboxamide and a polymer.
摘要翻译：组合物包含固体无定形分散体，其包含（S）-N- {2- [苄基（甲基）氨基] -2-氧代-1-苯基乙基} - 甲基-5- [4' - （三氟甲基） - 联苯] -2-甲酰氨基] -1H-吲哚-2-甲酰胺和聚合物。

33. 发明授权

US09486410B2 Pharmaceutical compositions of amorphous dispersions of drugs and lipophilic microphase-forming materials 有权
公开(公告)号：US09486410B2
公开(公告)日：2016-11-08
申请号：US11924988
申请日：2007-10-26
申请人： Michael E. Perlman , Ravi M. Shanker , Walter C. Babcock , Dwayne Thomas Friesen , Mark D. Rabenstein , Dan Tod Smithey
发明人： Michael E. Perlman , Ravi M. Shanker , Walter C. Babcock , Dwayne Thomas Friesen , Mark D. Rabenstein , Dan Tod Smithey
IPC分类号： A61K9/20 , A61K47/38 , A61K9/14 , A61K9/16
CPC分类号： A61K9/10 , A61K9/145 , A61K9/146 , A61K9/1617 , A61K9/1652 , A61K9/2013 , A61K9/2031 , A61K9/2054 , A61K9/4858 , A61K9/4866 , A61K31/40 , A61K31/44 , A61K31/4706 , A61K31/496
摘要： A pharmaceutical composition comprises a solid amorphous dispersion comprising a low-solubility drug and a concentration-enhancing polymer and a lipophilic microphase-forming material. Alternatively, a solid amorphous dispersion comprising a low-solubility drug and a concentration-enhancing polymer is co-administered with a lipophilic microphase-forming material to an in vivo use environment.

34. 发明授权

US6124457A Process and intermediates for a .beta..sub.3 -adrenergic receptor agonist 失效
公开(公告)号：US6124457A
公开(公告)日：2000-09-26
申请号：US488245
申请日：2000-01-20
申请人： Keith M. DeVries , Jeffrey W. Raggon , Ravi M. Shanker , Frank J. Urban , Brian C. Vanderplas
发明人： Keith M. DeVries , Jeffrey W. Raggon , Ravi M. Shanker , Frank J. Urban , Brian C. Vanderplas
IPC分类号： C07D213/74 , A61K31/44 , A61P43/00 , C07D213/16 , C07D213/73 , C07D213/75 , C07F7/02 , C07D211/74 , C07D213/53 , C07D405/02
CPC分类号： C07D213/75
摘要： The instant invention relates to intermediates of Formula II, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, and to processes for preparing such intermediates. This invention also relates to processes for preparing compounds of Formula III, ##STR2## and enantiomers thereof, wherein R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification. Compounds of Formula II and Formula III are intermediates in the preparation of a potent .beta..sub.3 adrenergic receptor agonist. The instant invention also relates to processes for preparing the .beta..sub.3 adrenergic receptor agonist using the compounds of Formula II and Formula III.

35. 发明授权

US09034913B2 Process for annealing amorphous atorvastatin 有权
标题翻译：无定形阿托伐他汀退火方法
公开(公告)号：US09034913B2
公开(公告)日：2015-05-19
申请号：US12067056
申请日：2006-09-11
申请人： Renuka D. Reddy , Evgenyi Shalaev , Ravi M. Shanker , Carl B. Ziegler
发明人： Renuka D. Reddy , Evgenyi Shalaev , Ravi M. Shanker , Carl B. Ziegler
IPC分类号： C07D207/34 , A61K31/40
CPC分类号： C07D207/34 , A61K31/40
摘要： Processes for annealing amorphous atorvastatin is described. Pharmaceutical compositions and formulations containing annealed amorphous atorvastatin are also described.
摘要翻译：描述了退火无定形阿托伐他汀的方法。还描述了含有退火的无定形阿托伐他汀的药物组合物和制剂。

36. 发明授权

US06548555B1 Basic drug compositions with enhanced bioavailability 有权
标题翻译：具有增强的生物利用度的基本药物组合物
公开(公告)号：US06548555B1
公开(公告)日：2003-04-15
申请号：US09495438
申请日：2000-01-31
申请人： William J. Curatolo , James A. S. Nightingale , Ravi M. Shanker , Steven C. Sutton
发明人： William J. Curatolo , James A. S. Nightingale , Ravi M. Shanker , Steven C. Sutton
IPC分类号： A61K4732
CPC分类号： A61K47/38 , A61K9/146 , A61K9/1652 , A61K9/2054 , A61K9/4866 , Y10S977/915
摘要： A composition comprising a basic drug, a drug which forms a zwitterion, or a salt of either entity, admixed with a polymer selected from hydroxypropylmethylcellulose acetate succinate (HPMCAS), cellulose acetate trimellitate (CAT), cellulose acetate phthalate (CAP), hydroxypropylcellulose acetate phthalate (HPCAP), hydroxypropylmethylcellulose acetate phthalate (HPMCAP), and methylcellulose acetate phthalate (MCAP). The compositions having improved solubility, hence bioavailability, in the small intestine; Processes for testing such compositions, and methods of using such compositions. The compositions comprise the basic drug, zwitterion, or salt and one or more of the aforementioned polymers. The invention further relates to a method for increasing the bioavailability of a basic or a zwitterionic drug comprising co-administering the basic drug, the zwitterionic drug, or the salt, with one or more of the aforementioned polymers.
摘要翻译：包含碱性药物，形成两性离子的药物或任一实体的盐，与选自羟丙基甲基纤维素乙酸酯琥珀酸酯（HPMCAS），醋酸偏苯三酸纤维素（CAT），乙酸邻苯二甲酸纤维素（CAP），羟丙基纤维素乙酸酯邻苯二甲酸酯（HPCAP），羟丙基甲基纤维素乙酸邻苯二甲酸酯（HPMCAP）和甲基纤维素乙酸邻苯二甲酸酯（MCAP）。所述组合物在小肠中具有改善的溶解度，因此具有生物利用度; 用于测试这些组合物的方法，以及使用这些组合物的方法。组合物包含碱性药物，两性离子或盐和一种或多种上述聚合物。本发明还涉及增加碱性或两性离子药物的生物利用度的方法，包括将一种或多种上述聚合物共同给予碱性药物，两性离子药物或盐。

37. 发明授权

US6090942A Process and intermediates for a .beta..sub.3 -adrenergic receptor agonist 失效
标题翻译： β-肾上腺素能受体激动剂的方法和中间体
公开(公告)号：US6090942A
公开(公告)日：2000-07-18
申请号：US408998
申请日：1999-09-29
申请人： Keith M. DeVries , Jeffrey W. Raggon , Ravi M. Shanker , Frank J. Urban , Brian C. Vanderplas
发明人： Keith M. DeVries , Jeffrey W. Raggon , Ravi M. Shanker , Frank J. Urban , Brian C. Vanderplas
IPC分类号： C07D213/74 , A61K31/44 , A61P43/00 , C07D213/16 , C07D213/73 , C07D213/75 , C07F7/02 , C07D403/12 , C07D405/12
CPC分类号： C07D213/75
摘要： The instant invention relates to intermediates of Formula II, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, and to processes for preparing such intermediates. This invention also relates to processes for preparing compounds of Formula III, ##STR2## and enantiomers thereof, wherein R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification. Compounds of Formula II and Formula III are intermediates in the preparation of a potent .beta..sub.3 adrenergic receptor agonist. The instant invention also relates to processes for preparing the .beta..sub.3 adrenergic receptor agonist using the compounds of Formula II and Formula III.
摘要翻译：本发明涉及式II的中间体，其中R1，R2和R3如说明书中所定义，以及制备这种中间体的方法。本发明还涉及制备式III化合物及其对映异构体的方法，其中R2，R3和R4如说明书中所定义。式II和式III的化合物是制备有效β3肾上腺素能受体激动剂的中间体。本发明还涉及使用式II和式III化合物制备β3肾上腺素能受体激动剂的方法。

38. 发明授权

US06399777B2 Inclusion complexes of aryl-heterocyclic salts 有权
标题翻译：芳基杂环盐的包合物
公开(公告)号：US06399777B2
公开(公告)日：2002-06-04
申请号：US09850658
申请日：2001-05-07
申请人： Yesook Kim , Kevin C. Johnson , Ravi M. Shanker
发明人： Yesook Kim , Kevin C. Johnson , Ravi M. Shanker
IPC分类号： C07D41714
CPC分类号： B82Y5/00 , A61K31/496 , A61K31/724 , A61K47/6951 , A61K2300/00
摘要： The esylate, mesylate, and tartrate salts of ziprasidone exhibit excellent solubilities in cyclodextrins.
摘要翻译：齐拉西酮的甲磺酸盐，甲磺酸盐和酒石酸盐在环糊精中表现出优异的溶解度。

39. 发明申请

US20090221667A1 Process for Annealing Amorphous Atorvastatin 审中-公开
标题翻译：退火无定形阿托伐他汀的方法
公开(公告)号：US20090221667A1
公开(公告)日：2009-09-03
申请号：US12067056
申请日：2006-09-11
申请人： Renuka D. Reddy , Evgenyi Shalaev , Ravi M. Shanker , Carl B. Ziegler
发明人： Renuka D. Reddy , Evgenyi Shalaev , Ravi M. Shanker , Carl B. Ziegler
IPC分类号： A61K31/40 , C07D207/34
CPC分类号： C07D207/34 , A61K31/40
摘要： Processes for annealing amorphous atorvastatin is described. Pharmaceutical compositions and formulations containing annealed amorphous atorvastatin are also described.
摘要翻译：描述了退火无定形阿托伐他汀的方法。还描述了含有退火的无定形阿托伐他汀的药物组合物和制剂。

40. 发明授权

US06232304B1 Inclusion complexes of aryl-heterocyclic salts 有权
标题翻译：芳基杂环盐的包合物
公开(公告)号：US06232304B1
公开(公告)日：2001-05-15
申请号：US09147239
申请日：1998-11-05
申请人： Yesook Kim , Kevin C. Johnson , Ravi M. Shanker
发明人： Yesook Kim , Kevin C. Johnson , Ravi M. Shanker
IPC分类号： A61K4748
CPC分类号： B82Y5/00 , A61K31/496 , A61K31/724 , A61K47/6951 , A61K2300/00
摘要： Compositions of matter comprising a pharmaceutically acceptable salt of an aryl-heterocyclic compound, such as ziprasidone, in a cyclodextrin. Preferred cyclodextrins are SBECD and HPBCD. The composition can comprise a dry mixture, a dry inclusion complex or an aqueous solution. The salt/cyclodextrin inclusion complex preferably provides an amount of ziprasidone of at least 2.5 mgA/ml when the complex is dissolved in water at 40% w/v. A variety of ziprasidone salts are preferred, including the mesylate, esylate, besylate, tartrate, napsylate, and tosylate.
摘要翻译：包含芳环杂环化合物如齐拉西酮的药学上可接受的盐在环糊精中的组合物。优选的环糊精是SBECD和HPBCD。该组合物可以包含干燥混合物，干燥包合络合物或水溶液。当络合物溶于40％w / v的水中时，盐/环糊精包合配合物优选提供至少2.5mgA / ml的量的齐拉西酮。各种齐拉西酮盐是优选的，包括甲磺酸盐，乙磺酸盐，苯磺酸盐，酒石酸盐，萘磺酸盐和甲苯磺酸盐。

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