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81. 发明申请

US20090156620A1 [4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENYL]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO 审中-公开
公开(公告)号：US20090156620A1
公开(公告)日：2009-06-18
申请号：US12265699
申请日：2008-11-05
申请人： Emma Sharp , Louisa Jane Quegan , Anjali Pandey , Juan Wang , Matthew Nieder , Wolin Huang
发明人： Emma Sharp , Louisa Jane Quegan , Anjali Pandey , Juan Wang , Matthew Nieder , Wolin Huang
IPC分类号： C07D409/12 , A61K31/517 , C12N5/06 , A61P9/00 , A61P7/00
CPC分类号： C07D409/12
摘要： The present invention provides novel sulfonylurea salts of a salt of formula (I) and polymorph forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and 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 provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a salt of formula (I) or a pharmaceutically acceptable form thereof.

82. 发明申请

US20090054425A1 PROTEIN KINASE INHIBITORS 有权
标题翻译：蛋白激酶抑制剂
公开(公告)号：US20090054425A1
公开(公告)日：2009-02-26
申请号：US12192034
申请日：2008-08-14
申请人： Yonghong Song , Qing Xu , Anjali Pandey
发明人： Yonghong Song , Qing Xu , Anjali Pandey
IPC分类号： A61K31/496 , C07D487/04 , A61K31/538 , A61P7/00 , A61P9/00 , A61P29/00 , A61P35/02 , C07D413/14
CPC分类号： C07D487/04
摘要： Compounds, particularly compounds having spleen tyrosine kinase (Syk) inhibition activity, having the following structure: or a pharmaceutically acceptable salt thereof, wherein R1 is structure (a), (b), (c) or (d): and Ra, Rb, Rc, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed, as well as uses of the same to treat a condition or disorder mediated by a Syk and/or JAK kinase.
摘要翻译：具有以下结构的化合物，特别是具有脾酪氨酸激酶（Syk）抑制活性的化合物或其药学上可接受的盐，其中R 1是结构（a），（b），（c）或（d）：和Ra，Rb ，Rc，R2，R3，R4，R5，R6和R7如本文所定义。还公开了与其制备和使用相关的方法以及含有该组合物的药物组合物，以及其用于治疗由Syk和/或JAK激酶介导的病症或病症的用途。

83. 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。

84. 发明申请

US20070142408A1 Compositions and methods for inhibiting TGF-Beta 失效
标题翻译：用于抑制TGF-β的组合物和方法
公开(公告)号：US20070142408A1
公开(公告)日：2007-06-21
申请号：US11653679
申请日：2007-01-16
申请人： Robert Scarborough , Anjali Pandey , Meenakshi Venkatraman
发明人： Robert Scarborough , Anjali Pandey , Meenakshi Venkatraman
IPC分类号： A61K31/517 , A61K31/4745 , C07D471/02
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-β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：ab是CH 2 CH 2 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为C 1-6脂族基或苯基，萘基或5-6元杂芳基环。

85. 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。}

86. 发明申请

US20060166896A1 Novel indazole peptidomimetics as thrombin receptor antagonists 审中-公开
公开(公告)号：US20060166896A1
公开(公告)日：2006-07-27
申请号：US11393350
申请日：2006-03-30
申请人： Han-Cheng Zhang , Bruce Maryanoff , Anjali Pandey , Robert Scarborough
发明人： Han-Cheng Zhang , Bruce Maryanoff , Anjali Pandey , Robert Scarborough
IPC分类号： A61K38/04
CPC分类号： C07K5/06078 , A61K31/416 , A61K38/00
摘要： The invention is directed to novel indazole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indazole peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.

87. 发明授权

US08536184B2 Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof 失效
公开(公告)号：US08536184B2
公开(公告)日：2013-09-17
申请号：US12622411
申请日：2009-11-19
申请人： James Kanter , James Robinson , Anjali Pandey , Robert M. Scarborough
发明人： James Kanter , James Robinson , Anjali Pandey , Robert M. Scarborough
IPC分类号： A61K31/4965 , C07D241/04
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.

88. 发明授权

US08394964B2 Methods of synthesizing factor Xa inhibitors 有权
公开(公告)号：US08394964B2
公开(公告)日：2013-03-12
申请号：US12969371
申请日：2010-12-15
申请人： Anjali Pandey , Emilia P. T. Leitao , Jose Rato , Zhiguo Jake Song
发明人： Anjali Pandey , Emilia P. T. Leitao , Jose Rato , Zhiguo Jake Song
IPC分类号： C07D213/75
CPC分类号： C07D213/75
摘要： Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof.

89. 发明申请

US20130029944A1 INHIBITORS OF PROTEIN KINASES 有权
标题翻译：蛋白激酶抑制剂
公开(公告)号：US20130029944A1
公开(公告)日：2013-01-31
申请号：US13528709
申请日：2012-06-20
申请人： Yonghong Song , Qing Xu , Shawn M. Bauer , Zhaozhong J. Jia , Mukund Mehrotra , Anjali Pandey
发明人： Yonghong Song , Qing Xu , Shawn M. Bauer , Zhaozhong J. Jia , Mukund Mehrotra , Anjali Pandey
IPC分类号： C07D471/04 , C07D401/04 , A61K31/506 , C07D403/04 , C07D473/16 , A61K31/52 , A61K31/496 , C07D401/14 , A61K31/635 , C07D487/04 , A61K31/5377 , C07D403/14 , A61K31/551 , A61K31/538 , A61K31/541 , A61P43/00 , A61P9/00 , A61P29/00 , A61P37/00 , A61P35/00 , C07D498/04 , A61K31/519
CPC分类号： C07D471/04 , C07D239/48 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D473/16
摘要： The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
摘要翻译：本发明涉及式I-II化合物及其药学上可接受的盐，酯和前体药物，它们是syk和/或JAK激酶的抑制剂。本发明还涉及用于制备这种化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制性syk和/或JAK激酶活性的方法，抑制血小板聚集的方法以及预防方法或治疗至少部分通过syk和/或JAK激酶活性介导的许多病症，例如不期望的血栓形成和非霍奇金淋巴瘤。

90. 发明授权

US08324205B2 Quinazoline derivatives as kinase inhibitors 失效
标题翻译：喹唑啉衍生物作为激酶抑制剂
公开(公告)号：US08324205B2
公开(公告)日：2012-12-04
申请号：US12471280
申请日：2009-05-22
申请人： Anjali Pandey , Robert M. Scarborough , Kenji Matsuno , Michio Ichimura , Yuji Nomoto , Shinichi Ide , Eiji Tsukuda , Junko Sasaki , Shoji Oda
发明人： Anjali Pandey , Robert M. Scarborough , Kenji Matsuno , Michio Ichimura , Yuji Nomoto , Shinichi Ide , Eiji Tsukuda , Junko Sasaki , Shoji Oda
IPC分类号： A61K31/535 , A61K31/497
CPC分类号： C07D239/94 , A61K31/517 , C07D401/12 , C07D403/12
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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