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公开(公告)号：EP1687642B1
公开(公告)日：2009-01-14
申请号：EP04790957.7
申请日：2004-10-07
发明人： NESBIT, Mark , SPADA, Alfred, P. , HE, Wei , MYERS, Michael, R.
CPC分类号： A61K31/498 , G01N33/5011 , G01N2333/71
摘要： This invention is directed to potent inhibitors of protein tyrosine kinase alone or in synergistic combination with antiangiogenic or chemotherapeutic agents for the abrogation of mature vasculature within chemotherapeutic refractory tumors, pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cell proliferation, and particularly treatment of brain cancer, ovarian cancer, pancreatic cancer prostate cancer, and human leukemias, such as CML, AML or ALL.
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2.发明公开
公开(公告)号：EP1687642A2
公开(公告)日：2006-08-09
申请号：EP04790957.7
申请日：2004-10-07
发明人： NESBIT, Mark , SPADA, Alfred, P. , HE, Wei , MYERS, Michael, R.
IPC分类号： G01N33/74 , A61K31/498 , A61P9/00 , A61P35/00
CPC分类号： A61K31/498 , G01N33/5011 , G01N2333/71
摘要： This invention is directed to potent inhibitors of protein tyrosine kinase alone or in synergistic combination with antiangiogenic or chemotherapeutic agents for the abrogation of mature vasculature within chemotherapeutic refractory tumors, pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cell proliferation, and particularly treatment of brain cancer, ovarian cancer, pancreatic cancer prostate cancer, and human leukemias, such as CML, AML or ALL.
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公开(公告)号：EP1208097B1
公开(公告)日：2009-02-18
申请号：EP00951781.4
申请日：2000-07-26
发明人： EWING, William, R. , BECKER, Michael, R. , CHOI-SLEDESKI, Yong, Mi , PAULS, Heinz, W. , HE, Wei , CONDON, Stephen, M. , DAVIS, Roderick, S. , HANNEY, Barbara, A. , SPADA, Alfred, P. , BURNS, Christopher J. , JIANG, John, Z. , LI, Aiwen , MYERS, Michael, R. , LAU, Wan, F. , POLI, Gregory, B.
IPC分类号： C07D403/06 , C07D401/06 , C07D409/14 , C07D409/12 , C07D471/04 , C07D241/08 , C07D495/04 , C07D401/14 , C07D409/06 , C07D403/14 , C07D491/04 , C07D417/14 , A61K31/496 , A61P7/02
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D409/14 , C07D471/04 , Y02P20/582
摘要： This invention is directed to oxoazaheterocyclyl compounds which inhibit Factor Xa, to oxoazaheterocyclyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa.
摘要翻译： 本发明涉及抑制因子Xa的氧代氮杂环基化合物，抑制因子Xa和因子IIa的氧代氮杂环基化合物，包含这些化合物的药物组合物，用于制备这些化合物的中间体，涉及直接抑制因子Xa和 同时直接抑制因子Xa和因子IIa的方法。
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公开(公告)号：EP1208097A2
公开(公告)日：2002-05-29
申请号：EP00951781.4
申请日：2000-07-26
发明人： EWING, William, R. , BECKER, Michael, R. , CHOI-SLEDESKI, Yong, Mi , PAULS, Heinz, W. , HE, Wei , CONDON, Stephen, M. , DAVIS, Roderick, S. , HANNEY, Barbara, A. , SPADA, Alfred, P. , BURNS, Christopher J. , JIANG, John, Z. , LI, Aiwen , MYERS, Michael, R. , LAU, Wan, F. , POLI, Gregory, B.
IPC分类号： C07D403/06 , C07D401/06 , C07D409/14 , C07D409/12 , C07D471/04 , C07D241/08 , C07D495/04 , C07D401/14 , C07D409/06 , C07D403/14 , C07D491/04 , C07D417/14 , A61K31/496 , A61P7/02
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D409/14 , C07D471/04 , Y02P20/582
摘要： This invention is directed to oxoazaheterocyclyl compounds which inhibit Factor Xa, to oxoazaheterocyclyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa.
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5.发明授权QUINOXALINE COMPOUNDS WHICH INHIBIT PLATELET-DERIVED GROWTH FACTOR AND/OR p56lck TYROSINE KINASES 失效喹喔啉衍生物血小板衍生生长因子和/或P56酪氨酸激酶抑制其DEN
公开(公告)号：EP1001946B1
公开(公告)日：2010-12-29
申请号：EP98926129.2
申请日：1998-05-28
发明人： SPADA, Alfred, P. , HE, Wei , MYERS, Michael, R.
IPC分类号： C07D215/20 , C07D215/38 , A61K31/47 , A61K31/495 , C07D241/44 , C07D405/12
CPC分类号： C07D215/38 , C07D215/20 , C07D241/42 , C07D241/44 , C07D241/52 , C07D241/54 , C07D403/04 , C07D405/12 , C07D453/06
摘要： This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56 tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
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6.发明授权ARYL AND HETEROARYL QUINAZOLINE COMPOUNDS WHICH INHIBIT CSF-1R RECEPTOR TYROSINE KINASE 失效抑制CSF-1R受体酪氨酸激酶的芳基和杂芳基喹唑啉化合物
公开(公告)号：EP0871448B1
公开(公告)日：2005-03-02
申请号：EP95904308.4
申请日：1994-12-08
发明人： MYERS, Michael, R. , SPADA, Alfred, P. , MAGUIRE, Martin, P. , PERSONS, Paul, E. , ZILBERSTEIN, Asher , HSU, Chin-Yi, Jenny , JOHNSON, Susan, E.
IPC分类号： A61K31/505 , A61K31/535 , A61P35/04 , C07D239/72 , C07D239/74 , C07D239/88 , C07D239/93 , C07D239/94 , C07D241/04 , C07D265/28 , C07D319/18 , A61K31/00
CPC分类号： C07D213/30 , A61K31/517 , A61K31/5377 , C07C43/2055 , C07C43/225 , C07C43/23 , C07D213/64 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/233 , C07D215/50 , C07D239/74 , C07D239/88 , C07D239/91 , C07D239/93 , C07D239/94 , C07D241/42 , C07D241/52 , C07D265/22 , C07D277/64 , C07D401/04 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D471/04
摘要： This invention relates to the modulation and/or inhibition of cell signaling, cell proliferation, cell inflammatory response, the control of abnormal cell growth and cell reproduction. More specifically, this invention relates to the use of mono- and/or bicyclic aryl or heteroaryl quinazoline compounds in inhibiting cell proliferation, including compounds which are useful protein tyrosine kinase (PTK) inhibitors. The method of treating cell proliferation and/or differentiation or mediator release using said quinazoline compounds and their use in pharmaceutical compositions is described.
摘要翻译： 本发明涉及调节和/或抑制细胞信号传导，细胞增殖，细胞炎症反应，异常细胞生长和细胞繁殖的控制。 更具体地说，本发明涉及单和/或双环芳基或杂芳基喹唑啉化合物在抑制细胞增殖中的用途，包括可用于蛋白酪氨酸激酶（PTK）抑制剂的化合物。 描述了使用所述喹唑啉化合物处理细胞增殖和/或分化或介质释放的方法及其在药物组合物中的用途。
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公开(公告)号：EP1051176B1
公开(公告)日：2006-11-22
申请号：EP99906684.8
申请日：1999-01-27
发明人： EWING, William, R. , BECKER, Michael, R. , CHOI-SLEDESKI, Yong, Mi , PAULS, Heinz, W. , HE, Wei , CONDON, Stephen, M. , DAVIS, Roderick, S. , HANNEY, Barbara, A. , SPADA, Alfred, P. , BURNS, Christopher, J. , JIANG, John, Z. , LI, Aiwen , MYERS, Michael, R. , LAU, Wan, F. , POLI, Gregory, B.
IPC分类号： C07D241/08 , A61K31/495
CPC分类号： C07D471/04 , C07D241/08 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D495/04
摘要： This invention is directed to oxoazaheterocyclyl compounds which inhibit factor Xa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds and to a method of inhibiting factor Xa.
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8.发明授权QUINOLINE AND QUINOXALINE COMPOUNDS WHICH INHIBIT PLATELET-DERIVED GROWTH FACTOR AND/OR p56lck TYROSINE KINASES 失效喹啉和血小板源性系数和/或P56 LCK酪氨酸激酶抑制喹喔啉的DEN
公开(公告)号：EP1001945B1
公开(公告)日：2011-03-02
申请号：EP98925041.0
申请日：1998-05-28
IPC分类号： C07D241/52 , C07D401/04 , C07D405/04
CPC分类号： C07D215/38 , C07D215/20 , C07D241/42 , C07D241/44 , C07D241/52 , C07D241/54 , C07D403/04 , C07D405/12 , C07D453/06
摘要： This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56 tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
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9.发明授权PYRAZOLO 3,4-g]QUINOXALINE COMPOUNDS WHICH INHIBIT PDGF RECEPTOR PROTEIN TYROSINE KINASE 失效吡唑并（3,4-G）喹喔啉ALS PDGF受体蛋白酪氨酸激酶抑制剂
公开(公告)号：EP0779889B1
公开(公告)日：2004-06-23
申请号：EP95932446.8
申请日：1995-09-06
IPC分类号： C07D487/04 , A61K31/495
CPC分类号： C07D487/04
摘要： This invention relates to pyrazolo[3,4-g]quinoxaline compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, compounds of this invention are novel as selective inhibitors of the PDGF-R protein tyrosine kinase and can be applied as potential therapeutic agents for various disease states which are characterized by uncontrolled cellular proliferation. Further, the present invention provides pharmaceutical compositions and a method for treating such disorders comprising the administration to a patient of a PDGF receptor inhibiting effective amount of a pyrazolo[3,4-g]quinoxaline compound exhibiting protein tyrosine kinase inhibition activity. Processes for the preparation of pyrazolo[3,4-g]quinoxaline compounds.
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