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21. 发明申请

US20120009172A1 INTRAVENOUS AND ORAL DOSING OF A DIRECT-ACTING AND REVERSIBLE P2Y12 INHIBITOR 审中-公开
标题翻译：直接作用和可逆的P2Y12抑制剂的口服和口服剂量
公开(公告)号：US20120009172A1
公开(公告)日：2012-01-12
申请号：US13235305
申请日：2011-09-16
申请人： Daniel D. Gretler , Pamela B. Conley , Patrick Andre , Athiwat Hutchaleelaha , David R. Phillips , Anjali Pandey , Robert M. Scarborough , Carroll Anna Crew Scarborough , Wolin Huang
发明人： Daniel D. Gretler , Pamela B. Conley , Patrick Andre , Athiwat Hutchaleelaha , David R. Phillips , Anjali Pandey , Robert M. Scarborough , Carroll Anna Crew Scarborough , Wolin Huang
IPC分类号： A61K38/45 , A61K38/48 , A61P9/00 , A61K31/517 , C07D409/12 , A61P7/00 , A61K38/46 , A61K31/60
CPC分类号： A61K31/517 , A61K31/216 , A61K2300/00
摘要： The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula: alone or in combination with a second agent which can be aspirin or a thrombolytic agent.
摘要翻译：本发明提供了通过施用下式的化合物单独或与可以是阿司匹林或溶栓剂的第二药剂组合来快速和可逆地抑制有需要的人受试者血小板聚集的方法和组合物。

22. 发明申请

US20110212983A1 PLATELET ADP RECEPTOR INHIBITORS 审中-公开
标题翻译： PLATELET ADP受体抑制剂
公开(公告)号：US20110212983A1
公开(公告)日：2011-09-01
申请号：US12642379
申请日：2009-12-18
申请人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
发明人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
IPC分类号： A61K31/506 , C07D409/12 , C07D417/12 , A61K31/427 , A61K31/4436 , A61P9/10 , A61P9/00 , A61P9/04
CPC分类号： C07D239/22 , C07D239/48 , C07D239/50 , C07D333/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D495/04
摘要： Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）至（VI）的新型化合物，其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物，磺酰基硫脲衍生物，磺酰基胍衍生物，磺酰基氰胍基衍生物，硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。这些衍生物可用于各种药物组合物中，并且对于预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病特别有效。本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法，包括施用治疗有效量的式（I） - （VI）化合物或其药学上可接受的盐的步骤。

23. 发明授权

US07109332B2 2,4-dioxo-3-quinazolinylaryl sulfonylureas 失效
标题翻译： 2,4-二氧代-3-喹唑啉基芳基磺酰脲
公开(公告)号：US07109332B2
公开(公告)日：2006-09-19
申请号：US10956004
申请日：2004-09-29
申请人： Robert M. Scarborough , Wolin Huang , Anjali Pandey , Shawn M. Bauer , Xiaoming Zhang , Zhaozhong J. Jia
发明人： Robert M. Scarborough , Wolin Huang , Anjali Pandey , Shawn M. Bauer , Xiaoming Zhang , Zhaozhong J. Jia
IPC分类号： C07D409/12 , C07D409/14 , A61K31/517 , A61P7/02
CPC分类号： C07D409/12 , C07D409/14
摘要： 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C1-6 alkyl; R1 is a member selected from the group consisting of H, C1-6 alkyl, C1-6 haloalkyl, C3-5 cycloalkyl and C3-5 cycloalkyl-alkyl; R2 is a member selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, cyano and —C(O)R2a, wherein R2a is a member selected from the group consisting of C1-6 alkoxy and (C1-6 alkyl)0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of —CH2—, —CH(CH3)—, —CH2CH2—, —CH2CH(CH3)— and —CH2CH2CH2—; L1 is a linking group selected from the group consisting of a bond and —CH2—; L2 is a linking group selected from the group consisting of a bond, —NH— and —CH2—; and Ar1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided. The compounds are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.
摘要翻译： 2,4-二氧代-3-喹唑啉基芳基磺酰脲类化合物，其具有下式：其中R是选自H和C 1-6烷基的成员; R 1是选自H，C 1-6烷基，C 1-6卤代烷基，C 1 -C 6烷基，C 1 -C 6烷基， 3-5个环烷基和C 3-5环烷基 - 烷基; R 2是选自H，卤素，C 1-6 - 烷基，C 2-6 - 烯基，C 1 -C 6烷基， C 1-6烷基，C 1-6烷氧基，氰基和-C（O）R 2a，其中R 2a是选自C 1-6烷氧基和（C 1-6烷基）烷基的成员， 0-2氨基; L是选自-CH 2 - ， - CH（CH 3 CH 3） - ， - CH 2 - ， - CH 2 CH 2（CH 3 CH 3） - 和-CH 2 CH _{2 CH 2 - ; L 1是选自键和-CH 2 - 的连接基团。 L 2是从由-NH-和-CH 2 - 的键组成的组中的连接基团。和Ar 1是选自苯，吡啶和嘧啶的芳环; 被提供。该化合物可用于抑制ADP-血小板聚集，特别是在治疗血栓形成和血栓相关病症或病症中。}

24. 发明授权

US06689786B2 Platelet ADP receptor inhibitors 有权
标题翻译：血小板ADP受体抑制剂
公开(公告)号：US06689786B2
公开(公告)日：2004-02-10
申请号：US10350883
申请日：2003-01-23
申请人： Robert M. Scarborough , Wolin Huang
发明人： Robert M. Scarborough , Wolin Huang
IPC分类号： C07D41712
CPC分类号： C07D239/22 , C07D239/48 , C07D239/50 , C07D333/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D495/04
摘要： Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）至（VI）的新型化合物，其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物，磺酰基硫脲衍生物，磺酰基胍衍生物，磺酰基氰胍基衍生物，硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。这些衍生物可用于各种药物组合物中，并且对于预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病特别有效。本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法，包括施用治疗有效量的式（I） - （VI）化合物或其药学上可接受的盐的步骤。

25. 发明授权

US07678790B2 Platelet ADP receptor inhibitors 失效
标题翻译：血小板ADP受体抑制剂
公开(公告)号：US07678790B2
公开(公告)日：2010-03-16
申请号：US11286259
申请日：2005-11-23
申请人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
发明人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
IPC分类号： C07D417/12 , C07D411/12 , C07D417/14 , C07D401/04 , A61K31/40 , A61K31/38 , A61K31/44 , A61K31/425 , A61K31/495 , A61K31/55
CPC分类号： C07D239/22 , C07D239/48 , C07D239/50 , C07D333/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D495/04
摘要： Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）至（VI）的新型化合物，其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物，磺酰基硫脲衍生物，磺酰基胍衍生物，磺酰基氰胍基衍生物，硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。这些衍生物可用于各种药物组合物中，并且对于预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病特别有效。本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法，包括施用治疗有效量的式（I） - （VI）化合物或其药学上可接受的盐的步骤。

26. 发明申请

US20090048216A1 INTRAVENOUS AND ORAL DOSING OF A DIRECT-ACTING AND REVERSIBLE P2Y12 INHIBITOR 审中-公开
标题翻译：直接作用和可逆的P2Y12抑制剂的口服和口服剂量
公开(公告)号：US20090048216A1
公开(公告)日：2009-02-19
申请号：US12114630
申请日：2008-05-02
申请人： Daniel D. Gretler , Pamela B. Conley , Patrick Andre , Athiwat Hutchaleelaha , David R. Phillips , Anjali Pandey , Robert M. Scarborough , Caroll Scarborough , Wolin Huang
发明人： Daniel D. Gretler , Pamela B. Conley , Patrick Andre , Athiwat Hutchaleelaha , David R. Phillips , Anjali Pandey , Robert M. Scarborough , Caroll Scarborough , Wolin Huang
IPC分类号： A61K31/517 , A61K31/60 , A61P9/00
CPC分类号： A61K31/517 , A61K31/216 , A61K2300/00
摘要： The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula: alone or in combination with a second agent which can be aspirin or a thrombolytic agent.
摘要翻译：本发明提供了通过施用下式的化合物单独或与可以是阿司匹林或溶栓剂的第二药剂组合来快速和可逆地抑制有需要的人受试者血小板聚集的方法和组合物。

27. 发明授权

US07022731B2 Platelet ADP receptor inhibitors 失效
公开(公告)号：US07022731B2
公开(公告)日：2006-04-04
申请号：US10759396
申请日：2004-01-15
申请人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
发明人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
IPC分类号： C07D409/12 , A61K31/4025 , A61P7/02
CPC分类号： C07D239/22 , C07D239/48 , C07D239/50 , C07D333/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D495/04
摘要： Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)–(VI), or a pharmaceutically acceptable salt thereof.

28. 发明授权

US08268857B2 Compositions and methods for inhibiting TGF-β 失效
标题翻译：用于抑制TGF-β的组合物和方法
公开(公告)号：US08268857B2
公开(公告)日：2012-09-18
申请号：US11653679
申请日：2007-01-16
申请人： Robert M. Scarborough , Anjali Pandey , Meenakshi S. Venkatraman
发明人： Robert M. Scarborough , Anjali Pandey , Meenakshi S. Venkatraman
IPC分类号： A61K31/4745 , C07D471/04 , A61P25/28 , A61P9/10 , A61P13/12 , A61P19/02
CPC分类号： C07D471/04
摘要： This invention provides compounds that are useful for treating patients having a TGF-β-mediated disease, particularly an ALK5-mediated disease. The compounds are represented by formula I: wherein: a-b is CH2CH2, CH2CH2CH2, CH═CH, CH═N, or N═CH; Z is N or C—F; and G is C1-6 aliphatic or a phenyl, naphthyl, or 5-6 membered heteroaryl ring.
摘要翻译：本发明提供可用于治疗患有TGF-和bgr介导的疾病，特别是ALK5介导的疾病的患者的化合物。化合物由式I表示：其中：a-b为CH 2 CH 2，CH 2 CH 2 CH 2，CH = CH，CH = N或N = CH; Z是N或C-F; 和G是C 1-6脂族基或苯基，萘基或5-6元杂芳基环。

29. 再颁专利

USRE43098E1 Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof 失效
标题翻译：含氮杂环化合物及其制备含氮杂环化合物的方法及其中间体
公开(公告)号：USRE43098E1
公开(公告)日：2012-01-10
申请号：US11866275
申请日：2007-10-02
申请人： James Kanter , Anjali Pandey , James Robinson , Robert M. Scarborough , Carroll Scarborough, legal representative
发明人： James Kanter , Anjali Pandey , James Robinson , Robert M. Scarborough
IPC分类号： A61K31/495 , C07D487/00 , C07D487/04 , C07D239/94
摘要： The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.
摘要翻译：本发明提供了含氮杂环化合物及其药学上可接受的盐及其制备方法。这些化合物对抑制这种激酶活性的激酶的磷酸化具有抑制活性。本发明还提供了可用于该方法的中间体化合物，以及通过该方法生产的最终产物及其盐或前药。本发明进一步提供了通过抑制激酶的磷酸化来抑制哺乳动物激酶和治疗疾病状态的方法，包括向有需要的患者施用有效量的本发明化合物。

30. 发明授权

US07943640B2 Compositions and methods for inhibiting TGF-β 失效
标题翻译：用于抑制TGF-β的组合物和方法
公开(公告)号：US07943640B2
公开(公告)日：2011-05-17
申请号：US11941284
申请日：2007-11-16
申请人： Anjali Pandey , Robert M. Scarborough , Meenakshi S. Venkatraman
发明人： Anjali Pandey , Robert M. Scarborough , Meenakshi S. Venkatraman
IPC分类号： A61K31/04
CPC分类号： C07D401/12 , C07D405/14
摘要： The present invention provides compounds of the formula: and pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives thereof, wherein R1, R6, R7, R8, Pg, and n are those defined herein. The present invention also provides pharmaceutical compositions comprising the same and methods for using the same. In particular, compounds of Formula I are useful in modulating TGF-β activity.
摘要翻译：本发明提供下式的化合物及其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物，其中R1，R6，R7，R8，Pg和n是本文定义的那些。本发明还提供了包含该组合物的药物组合物及其使用方法。特别地，式I化合物可用于调节TGF- 活动。

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