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公开(公告)号:US09556166B2
公开(公告)日:2017-01-31
申请号:US13468757
申请日:2012-05-10
申请人: Megan Foley , Bradley Tait , Matthew Cullen
发明人: Megan Foley , Bradley Tait , Matthew Cullen
IPC分类号: C07D401/06 , C07D403/06 , C07D405/06 , C07D471/04 , C07D207/333 , C07D207/337 , C07D231/12 , C07D249/06 , C07D263/32 , C07D275/02 , C07D295/185 , C07D333/20
CPC分类号: C07D403/06 , C07D207/333 , C07D207/337 , C07D231/12 , C07D249/06 , C07D263/32 , C07D275/02 , C07D295/185 , C07D333/20 , C07D333/22 , C07D401/06 , C07D405/06 , C07D471/04
摘要: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.
摘要翻译: 本发明涉及具有式(Ia-Ie),(II),(IIIa-IIId),(IVa-IVc),(Va-Vb),(VIa-VIe),(VII) -VIIIc)和(IX),其药学上可接受的盐,前药和溶剂化物,其任何组合物以及用于治疗与蛋白酶抑制功能障碍相关的病症的方法,其包含有效量的这些化合物。
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公开(公告)号:US20120316193A1
公开(公告)日:2012-12-13
申请号:US13468757
申请日:2012-05-10
申请人: Megan Foley , Bradley Tait , Matthew Cullen
发明人: Megan Foley , Bradley Tait , Matthew Cullen
IPC分类号: C07D207/333 , C07D401/06 , C07D403/06 , C07D471/04 , C07D405/06 , C07D231/12 , C07D413/06 , C07D417/06 , C07D409/06 , C07D207/34 , A61K31/402 , A61K31/454 , A61K31/4025 , A61K31/4178 , A61K31/4745 , A61K31/404 , A61K31/4155 , A61K31/415 , A61K31/4535 , A61K31/4192 , A61P25/28 , A61P25/16 , A61P25/00 , A61P3/10 , A61P35/00 , C07D207/337
CPC分类号: C07D403/06 , C07D207/333 , C07D207/337 , C07D231/12 , C07D249/06 , C07D263/32 , C07D275/02 , C07D295/185 , C07D333/20 , C07D333/22 , C07D401/06 , C07D405/06 , C07D471/04
摘要: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.
摘要翻译: 本发明涉及具有式(Ia-Ie),(II),(IIIa-IIId),(IVa-IVc),(Va-Vb),(VIa-VIe),(VII) -VIIIc)和(IX),其药学上可接受的盐,前药和溶剂化物,其任何组合物以及用于治疗与蛋白酶抑制功能障碍相关的病症的方法,其包含有效量的这些化合物。
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公开(公告)号:US20120214824A1
公开(公告)日:2012-08-23
申请号:US13315057
申请日:2011-12-08
IPC分类号: A61K31/519 , A61K31/47 , A61K31/4709 , A61K31/4162 , A61P3/10 , C07D491/052 , C07D409/08 , A61P35/00 , A61P25/28 , A61P25/16 , A61K31/436 , C07D471/04
CPC分类号: C07D409/04 , A61K31/519 , C07D215/54 , C07D487/04 , C07D491/04
摘要: The present invention is directed to compounds of Formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.
摘要翻译: 本发明涉及式(I),(II),(III),(IV),(V),(VI),(VII)和(VIII))的药物组合物及其使用方法 在治疗与蛋白酶抑制功能障碍有关的病症。
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公开(公告)号:US20130072473A1
公开(公告)日:2013-03-21
申请号:US13467949
申请日:2012-05-09
申请人: Bradley Tait , Noel A. Powell , Matthew Cullen
发明人: Bradley Tait , Noel A. Powell , Matthew Cullen
IPC分类号: A61K31/55 , C07D495/04 , C07D333/68 , C07D417/04 , C07D307/85 , A61K31/4743 , A61K31/4745
CPC分类号: C07D495/04 , A61K31/40 , C07D307/85 , C07D333/68 , C07D417/04
摘要: The present invention is directed to compounds of Formulae (I), (IIa-IIh), (IIIa-IIIe), (IVa-IVc), (Va-V1), (VIa-VII), (VII), (VIII) and (IX), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.
摘要翻译: 本发明涉及式(I),(IIa-IIh),(IIIa-IIIe),(IVa-IVc),(Va-V1),(VIa-VII),(VII) 和(IX),其药物组合物及其在治疗与蛋白质降解功能障碍相关的病症中的用途。
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公开(公告)号:US5326762A
公开(公告)日:1994-07-05
申请号:US885420
申请日:1992-05-19
申请人: John Clader , Sundeep Dugar , Timothy Kogan , Bradley Tait , Wayne Vaccaro
发明人: John Clader , Sundeep Dugar , Timothy Kogan , Bradley Tait , Wayne Vaccaro
IPC分类号: C07C233/18 , C07C233/20 , C07C233/22 , C07C233/36 , C07C233/38 , C07C233/40 , C07C233/49 , C07C233/51 , C07C235/50 , C07C237/22 , C07C271/22 , C07C311/08 , H01N43/40 , C07D211/70
CPC分类号: C07C233/20 , C07C233/18 , C07C233/22 , C07C233/36 , C07C233/38 , C07C233/40 , C07C233/49 , C07C233/51 , C07C235/50 , C07C237/22 , C07C271/22 , C07C311/08 , Y10S514/824
摘要: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected form the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.4 is hydrogen, lower alkyl, phenyl, X-substituted phenyl, heteroaryl or X-substituted heteroaryl; or a pharmaceutically acceptable salt thereof, useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.
摘要翻译: 其中R 1和R 2独立地是杂芳基,X取代的杂芳基,X取代的苯基,N-取代的三嗪基或N-取代的咪唑基; 此外,R 1和R 2中的一个可以如上所定义,另一个可以是苯基; R3是2至25个碳原子的饱和或不饱和的烷基链; 由一个或多个选自苯基,X取代的苯基,杂芳基和X取代的杂芳基的取代基取代的烷基链; 由一个或多个独立地选自-O - , - S - , - SO - , - SO 2 - , - NH - , - N(低级烷基) - , - C ) - ,亚苯基,X取代亚苯基,亚杂芳基和X取代亚杂芳基; 或被一个或多个选自苯基,X取代的苯基,杂芳基和X取代的杂芳基的取代基取代的中断的烷基链; R4是氢,低级烷基,苯基,X取代的苯基,杂芳基或X取代的杂芳基; 或其药学上可接受的盐,其可用作酰基辅酶A的抑制剂:胆固醇酰基转移酶,因此用于治疗动脉粥样硬化。
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公开(公告)号:US20050075390A1
公开(公告)日:2005-04-07
申请号:US10938442
申请日:2004-09-09
申请人: Frederick Boyer , John Domagala , Edmund Ellsworth , Christopher Gajda , Susan Hagen , Michael Lovdahl , Elizabeth Lunney , Larry Markoski , Josyula Venkata Prasad , Bradley Tait
发明人: Frederick Boyer , John Domagala , Edmund Ellsworth , Christopher Gajda , Susan Hagen , Michael Lovdahl , Elizabeth Lunney , Larry Markoski , Josyula Venkata Prasad , Bradley Tait
IPC分类号: C07D233/64 , A61K31/351 , A61K31/381 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61P31/14 , A61P31/18 , C07D207/333 , C07D209/12 , C07D209/30 , C07D213/30 , C07D213/71 , C07D231/12 , C07D235/06 , C07D235/26 , C07D239/26 , C07D239/42 , C07D241/44 , C07D277/20 , C07D277/24 , C07D277/46 , C07D277/82 , C07D307/12 , C07D307/42 , C07D309/32 , C07D333/16 , C07D333/32 , C07D333/62 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/06 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/12 , C07D417/14 , C07D309/30 , A61K31/366
CPC分类号: C07D405/06 , C07D309/32 , C07D405/12 , C07D405/14 , C07D407/06 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/12 , C07D417/14
摘要: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
摘要翻译: 本发明涉及具有改善的药理学性质的具有栓系杂环的新型二氢吡喃酮,其有效抑制HIV天冬氨酰蛋白酶阻断HIV感染性。 二氢吡喃可用于开发用于治疗病毒感染和疾病(包括AIDS)的治疗。 本发明还涉及合成二氢吡喃的方法和可用于制备最终化合物的中间体。
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公开(公告)号:US5149709A
公开(公告)日:1992-09-22
申请号:US547644
申请日:1990-07-03
申请人: John Clader , Sundeep Dugar , Timothy Kogan , Bradley Tait , Wayne Vaccaro
发明人: John Clader , Sundeep Dugar , Timothy Kogan , Bradley Tait , Wayne Vaccaro
IPC分类号: C07C233/18 , C07C233/20 , C07C233/22 , C07C233/36 , C07C233/38 , C07C233/40 , C07C233/49 , C07C233/51 , C07C235/50 , C07C237/22 , C07C271/22 , C07C311/08
CPC分类号: C07C233/20 , C07C233/18 , C07C233/22 , C07C233/36 , C07C233/38 , C07C233/40 , C07C233/49 , C07C233/51 , C07C235/50 , C07C237/22 , C07C271/22 , C07C311/08 , Y10S514/824
摘要: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.4 is hydrogen, lower alkyl, phenyl, X-substituted phenyl, heteroaryl or X-substituted heteroaryl; or a pharmaceutically acceptable salt thereof, useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.
摘要翻译: 其中R 1和R 2独立地是杂芳基,X取代的杂芳基,X取代的苯基,N-取代的三嗪基或N-取代的咪唑基; 此外,R 1和R 2中的一个可以如上所定义,另一个可以是苯基; R3是2至25个碳原子的饱和或不饱和的烷基链; 由一个或多个选自苯基,X取代的苯基,杂芳基和X取代的杂芳基的取代基取代的烷基链; 由一个或多个独立地选自-O - , - S - , - SO - , - SO 2 - , - NH - , - N(低级烷基) - , - C ) - ,亚苯基,X取代亚苯基,亚杂芳基和X取代亚杂芳基; 或被一个或多个选自苯基,X取代的苯基,杂芳基和X取代的杂芳基的取代基取代的间断的烷基链; R4是氢,低级烷基,苯基,X取代的苯基,杂芳基或X取代的杂芳基; 或其药学上可接受的盐,其可用作酰基辅酶A的抑制剂:胆固醇酰基转移酶,因此用于治疗动脉粥样硬化。
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