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1. 发明申请

US20110098247A1 Substituted Dihydroquinazolines as Platelet ADP Receptor Inhibitors 审中-公开
标题翻译：取代的二氢喹唑啉作为血小板ADP受体抑制剂
公开(公告)号：US20110098247A1
公开(公告)日：2011-04-28
申请号：US12912367
申请日：2010-10-26
申请人： Robert M. Scarborough , Shawn M. Bauer , Anjali Pandey , Carrol Anna Crew Scarborough
发明人： Robert M. Scarborough , Shawn M. Bauer , Anjali Pandey , Carrol Anna Crew Scarborough
IPC分类号： A61K31/727 , A61K31/517 , A61K31/5355 , A61K31/4725 , A61P7/02
CPC分类号： C07D409/12 , C07D239/96 , C07D265/22 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Compounds of formula I are provided: wherein Ar1 and Ar2 are substituted aromatic rings and L1 and L2 are independent divalent linking groups. The compounds are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.
摘要翻译：提供式I化合物：其中Ar 1和Ar 2是取代的芳环，且L 1和L 2是独立的二价连接基团。该化合物可用作血小板ADP受体抑制剂，用于治疗血栓形成和降低患者中二次缺血事件的可能性和/或严重性。

2. 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。}

3. 发明授权

US07834023B2 Substituted dihydroquinazolines as platelet ADP receptor inhibitors 有权
标题翻译：取代的二氢喹唑啉作为血小板ADP受体抑制剂
公开(公告)号：US07834023B2
公开(公告)日：2010-11-16
申请号：US11856616
申请日：2007-09-17
申请人： Robert M. Scarborough , Carroll Anna Crew, legal representative , Shawn M. Bauer , Anjali Pandey
发明人： Robert M. Scarborough , Shawn M. Bauer , Anjali Pandey
IPC分类号： A61K31/517
CPC分类号： C07D409/12 , C07D239/96 , C07D265/22 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Compounds of formula I are provided: wherein Ar1 and Ar2 are substituted aromatic rings and L1 and L2 are independent divalent linking groups. The compounds are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.
摘要翻译：提供式I化合物：其中Ar 1和Ar 2是取代的芳环，且L 1和L 2是独立的二价连接基团。该化合物可用作血小板ADP受体抑制剂，用于治疗血栓形成和降低患者中二次缺血事件的可能性和/或严重性。

4. 发明申请

US20080132499A1 PLATELET ADP RECEPTOR INHIBITORS 有权
标题翻译： PLATELET ADP受体抑制剂
公开(公告)号：US20080132499A1
公开(公告)日：2008-06-05
申请号：US11856616
申请日：2007-09-17
申请人： Robert M. Scarborough , Carroll Anna Crew Scarborough , Shawn M. Bauer , Anjali Pandey
发明人： Robert M. Scarborough , Carroll Anna Crew Scarborough , Shawn M. Bauer , Anjali Pandey
IPC分类号： A61K31/536 , C07D237/30 , C07D403/02 , C07D239/88 , A61K31/517 , A61P7/02 , A61K31/4725 , A61K31/502 , C07D265/22 , C07D217/24
CPC分类号： C07D409/12 , C07D239/96 , C07D265/22 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Compounds are provided which are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.
摘要翻译：提供了可用作血小板ADP受体抑制剂，用于治疗血栓形成和降低患者二次缺血事件的可能性和/或严重性的化合物。

5. 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。

6. 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。

7. 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。

8. 发明申请

US20070259924A1 FACTOR XA INHIBITORS 有权
标题翻译：因子XA抑制剂
公开(公告)号：US20070259924A1
公开(公告)日：2007-11-08
申请号：US11744735
申请日：2007-05-04
申请人： Yonghong Song , Zhaozhong J. Jia , Anjali Pandey , Robert M. Scarborough , Carroll Scarborough
发明人： Yonghong Song , Zhaozhong J. Jia , Anjali Pandey , Robert M. Scarborough , Carroll Scarborough
IPC分类号： A61K31/4439 , A61K31/4178 , A61K31/4172 , C07D403/02 , C07D409/02 , C07D405/02
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译：本发明涉及作为因子Xa抑制剂的式（I）化合物及其药学上可接受的盐，酯和前药。本发明还涉及用于制备这种化合物的中间体，含有这种化合物的药物组合物，预防或治疗许多不希望的血栓形成特征的病症的方法以及抑制血液样品凝固的方法。

9. 发明授权

US07709640B2 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：US07709640B2
公开(公告)日：2010-05-04
申请号：US11313289
申请日：2005-12-19
申请人： James Kanter , Anjali Pandey , James Robinson , Robert M. Scarborough
发明人： James Kanter , Anjali Pandey , James Robinson , Robert M. Scarborough
IPC分类号： C07D295/182
CPC分类号： 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。

10. 发明申请

US20090176780A1 NITROGENOUS HETEROCYCLIC COMPOUNDS 失效
标题翻译：硝基杂环化合物
公开(公告)号：US20090176780A1
公开(公告)日：2009-07-09
申请号：US11959341
申请日：2007-12-18
申请人： Anjali Pandey , Robert M. Scarborough , Kenji Matsuno , Michio Ichimura , Yuji Nomoto , Shinichi Ide , Eiji Tsukuda , Nee Junko Irie Junko Sasaki , Shoji Oda
发明人： Anjali Pandey , Robert M. Scarborough , Kenji Matsuno , Michio Ichimura , Yuji Nomoto , Shinichi Ide , Eiji Tsukuda , Nee Junko Irie Junko Sasaki , Shoji Oda
IPC分类号： A61K31/5377 , A61K31/517
CPC分类号： C07D401/12 , C07D239/94 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.
摘要翻译：本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。在一个特定方面，本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐，以及预防或治疗细胞增殖性疾病如动脉硬化，血管重建，癌症和肾小球硬化症。

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