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91. 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.

92. 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.

93. 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。

94. 发明授权

US07417030B2 Indazole peptidomimetics as thrombin receptor antagonists 有权
标题翻译：吲唑类似物作为凝血酶受体拮抗剂
公开(公告)号：US07417030B2
公开(公告)日：2008-08-26
申请号：US11393529
申请日：2006-03-30
申请人： Han-Cheng Zhang , Bruce E. Maryanoff , Anjali Pandey , Robert M. Scarborough
发明人： Han-Cheng Zhang , Bruce E. Maryanoff , Anjali Pandey , Robert M. Scarborough
IPC分类号： A61K38/00 , A61K31/416 , C07K5/00 , C07D277/04
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.
摘要翻译：本发明涉及可用作治疗与血栓形成，再狭窄，高血压，心力衰竭，心律失常，炎症，心绞痛，中风，动脉粥样硬化，缺血性疾病，血管发生相关疾病，癌症相关的疾病的凝血酶受体拮抗剂的新型吲唑拟肽化合物，和神经变性疾病。还公开了包含本发明的取代的吲唑肽模拟物的药物组合物和治疗由凝血酶受体介导的病症的方法。

95. 发明申请

US20070208045A1 SUBSTITUTED-(QUINAZOLINYL)PHENYL THIOPHENYL-SULFONYLUREAS, METHODS FOR MAKING AND INTERMEDIATES THEREOF 审中-公开
标题翻译：取代 - （喹喔啉基）苯基噻吩磺酰亚胺，其制备方法及其中间体
公开(公告)号：US20070208045A1
公开(公告)日：2007-09-06
申请号：US11556518
申请日：2006-11-03
申请人： Robert Scarborough , Carroll Scarborough , Anjali Pandey , Mukund Mehrotra , Michael Cruskie , David White , George Yiannikouros
发明人： Robert Scarborough , Carroll Scarborough , Anjali Pandey , Mukund Mehrotra , Michael Cruskie , David White , George Yiannikouros
IPC分类号： A61K31/517 , C07D409/02
CPC分类号： C07D409/12
摘要： The present invention provides sulfonylurea compounds of formula (VIII) and pharmaceutically acceptable derivatives thereof and a process for making 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 intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention also provides a method for inhibition platelet ADP receptor and preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (VIII) or a pharmaceutically acceptable salt or forms thereof.
摘要翻译：本发明提供式（VIII）的磺酰脲化合物及其药学上可接受的衍生物及其制备方法。各种形式的化合物是有效的血小板ADP受体抑制剂，可用于各种药物组合物中，并且特别有效预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病。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。本发明还提供了抑制血小板ADP受体并预防或治疗哺乳动物血栓形成和血栓形成相关病症的方法，包括施用治疗有效量的式（Ⅷ）化合物或其药学上可接受的盐或其形式的步骤。

96. 发明申请

US20060167011A1 Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof 失效
公开(公告)号：US20060167011A1
公开(公告)日：2006-07-27
申请号：US11313289
申请日：2005-12-19
申请人： James Kanter , Anjali Pandey , James Robinson , Robert Scarborough
发明人： James Kanter , Anjali Pandey , James Robinson , Robert Scarborough
IPC分类号： C07D241/04 , A61K31/495
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.

97. 发明申请

US20060166897A1 Novel indazole peptidomimetics as thrombin receptor antagonists 有权
公开(公告)号：US20060166897A1
公开(公告)日：2006-07-27
申请号：US11393529
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.

98. 发明授权

US06982266B2 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：US06982266B2
公开(公告)日：2006-01-03
申请号：US10344736
申请日：2001-08-17
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： A01K31/675 , A01K31/517 , C07D43/02 , C07D239/72
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 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，以及用于预防或治疗细胞增殖性疾病如动脉硬化的方法，血管重构，癌症和肾小球硬化症。

99. 发明授权

US06960580B2 Nitrogenous heterocyclic substituted quinoline compounds 有权
标题翻译：氮杂环取代喹啉化合物
公开(公告)号：US06960580B2
公开(公告)日：2005-11-01
申请号：US10094191
申请日：2002-03-08
申请人： Robert M. Scarborough , Anjali Pandey
发明人： Robert M. Scarborough , Anjali Pandey
IPC分类号： C07D215/46 , C07D215/54 , C07D401/12 , A61K31/496 , A61P35/00
CPC分类号： C07D401/12 , C07D215/46 , C07D215/54
摘要： The present invention relates to nitrogen-containing heterocyclic quinoline 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. More particularly, 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喹啉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。更具体地说，本发明提供了抑制PDGF受体的磷酸化阻碍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，血管重构的方法，癌症和肾小球硬化症。

100. 发明授权

US06956039B2 Nitrogenous heterocylic compounds 失效
标题翻译：含氮杂环化合物
公开(公告)号：US06956039B2
公开(公告)日：2005-10-18
申请号：US10344737
申请日：2001-08-17
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： A61P35/00 , C07D239/94 , C07D401/12 , C07D403/12 , C07D487/00
CPC分类号： C07D401/12 , C07D239/94 , 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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