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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。
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公开(公告)号:US06960580B2
公开(公告)日:2005-11-01
申请号:US10094191
申请日:2002-03-08
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。
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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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公开(公告)号:US20120130073A1
公开(公告)日:2012-05-24
申请号:US13269523
申请日:2011-10-07
申请人: Zhaozhong Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrotra , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
发明人: Zhaozhong Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrotra , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
IPC分类号: C07D403/12
CPC分类号: A61K31/506 , C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk 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 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 kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
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公开(公告)号:US20110005947A1
公开(公告)日:2011-01-13
申请号:US12775358
申请日:2010-05-06
申请人: Shawn M. Bauer , Jack W. Rose , Yonghong Song , Qing Xu , Mukund Mehrotra , Wolin Huang , Anjali Pandey
发明人: Shawn M. Bauer , Jack W. Rose , Yonghong Song , Qing Xu , Mukund Mehrotra , Wolin Huang , Anjali Pandey
IPC分类号: B65D85/00 , C07D239/48 , A61K31/505 , C07D403/12 , A61K31/506 , C07D405/12 , C07D413/12 , A61K31/5377 , C07D403/14 , C07D401/12 , C07D417/12 , C07D401/14 , A61K31/444 , A61K31/4427 , A61K31/4439 , A61P29/00 , A61P3/10 , A61P25/00 , A61P37/06 , A61P9/00 , A61P11/06
CPC分类号: C07D417/14 , C07D213/82 , C07D239/48 , C07D401/12 , C07D403/12 , C07D403/14 , C07D417/12
摘要: The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. 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 JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity.
摘要翻译: 本发明涉及作为JAK的选择性抑制剂的式I化合物及其互变异构体及其药学上可接受的盐。 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JAK活性的方法,以及预防或治疗至少部分地由 JAK活动。
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公开(公告)号:US20100048567A1
公开(公告)日:2010-02-25
申请号:US12386525
申请日:2009-04-16
申请人: Zhaozhong Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrota , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
发明人: Zhaozhong Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrota , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
IPC分类号: A61K31/5377 , C07D239/02 , C07D413/02 , C07D403/02 , A61K31/497 , A61K31/505 , A61K31/506 , C12N5/02
CPC分类号: A61K31/506 , C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk 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 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 kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
摘要翻译: 本发明涉及作为syk激酶抑制剂的式I-V化合物及其互变异构体或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,这种化合物的制备,含有这种化合物的药物组合物,抑制syk激酶活性的方法,抑制血小板聚集的方法,以及预防或治疗数字的方法 至少部分通过syk激酶活性介导的病症,例如不期望的血栓形成和非霍奇金淋巴瘤。
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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。
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公开(公告)号:US08367689B2
公开(公告)日:2013-02-05
申请号:US12775358
申请日:2010-05-06
申请人: Shawn M. Bauer , Jack W. Rose , Yonghong Song , Qing Xu , Mukund Mehrotra , Wolin Huang , Anjali Pandey
发明人: Shawn M. Bauer , Jack W. Rose , Yonghong Song , Qing Xu , Mukund Mehrotra , Wolin Huang , Anjali Pandey
IPC分类号: A01N43/54 , A61K31/505
CPC分类号: C07D417/14 , C07D213/82 , C07D239/48 , C07D401/12 , C07D403/12 , C07D403/14 , C07D417/12
摘要: The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. 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 JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity.
摘要翻译: 本发明涉及作为JAK的选择性抑制剂的式I化合物及其互变异构体及其药学上可接受的盐。 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JAK活性的方法,以及预防或治疗至少部分地由 JAK活动。
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公开(公告)号:US20120101275A1
公开(公告)日:2012-04-26
申请号:US13275253
申请日:2011-10-17
申请人: Zhaozhong Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrotra , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
发明人: Zhaozhong Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrotra , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
IPC分类号: C07D403/12
CPC分类号: A61K31/506 , C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk 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 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 kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
摘要翻译: 本发明涉及作为syk激酶抑制剂的式I-V化合物及其互变异构体或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,这种化合物的制备,含有这种化合物的药物组合物,抑制syk激酶活性的方法,抑制血小板聚集的方法,以及预防或治疗数字的方法 至少部分通过syk激酶活性介导的病症,例如不期望的血栓形成和非霍奇金淋巴瘤。
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公开(公告)号:US07705004B2
公开(公告)日:2010-04-27
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: C07D487/04 , A61K31/519
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。
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