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公开(公告)号：EP1144373A2
公开(公告)日：2001-10-17
申请号：EP00911572.6
申请日：2000-01-11
申请人： Genentech, Inc.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C317/00
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having structure (A) are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
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2.发明公开BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权苯并吡喃和BENZOXEPINVERBINDUNGEN AS PI3K抑制剂及其使用方法
公开(公告)号：EP2276767A1
公开(公告)日：2011-01-26
申请号：EP09726963.3
申请日：2009-03-30
发明人： ZHU, Bing-yan , GOLDSMITH, Paul , BAYLISS, Tracy , FOLKES, Adrian , PEGG, Neil , DO, Steven , GOLDSMITH, Richard , HEFFRON, Tim , KOLESNIKOV, Aleksandr , STABEN, Steven , OLIVERO, Alan, G. , SIU, Michael , SUTHERLIN, Daniel, P.
IPC分类号： C07D495/04 , C07D513/04 , A61K31/38 , A61K31/429 , A61P35/00
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for
in vitro, in situ, and
in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.-
3.发明授权BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权苯并吡喃和BENZOXEPINVERBINDUNGEN AS PI3K抑制剂及其使用方法
公开(公告)号：EP2276767B1
公开(公告)日：2014-05-07
申请号：EP09726963.3
申请日：2009-03-30
发明人： ZHU, Bing-yan , GOLDSMITH, Paul , BAYLISS, Tracy , FOLKES, Adrian , PEGG, Neil , DO, Steven , GOLDSMITH, Richard , HEFFRON, Tim , KOLESNIKOV, Aleksandr , STABEN, Steven , OLIVERO, Alan, G. , SIU, Michael , SUTHERLIN, Daniel, P.
IPC分类号： C07D495/04 , C07D513/04 , A61K31/38 , A61K31/429 , A61P35/00
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
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公开(公告)号：EP1144373B1
公开(公告)日：2005-10-19
申请号：EP00911572.6
申请日：2000-01-11
申请人： GENENTECH, INC.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C311/51
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having structure (A) are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
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公开(公告)号：EP1144373A3
公开(公告)日：2002-01-02
申请号：EP00911572.6
申请日：2000-01-11
申请人： Genentech, Inc.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C311/51
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
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公开(公告)号：EP0975608A2
公开(公告)日：2000-02-02
申请号：EP98913417.6
申请日：1998-04-08
申请人： Genentech, Inc.
IPC分类号： C07D243/24 , A61K31/55
CPC分类号： C07D243/14
摘要： Halo-alkoxycarbonyl derivatives of formula (I) are provided as prodrug moieties for pharmaceutical agents containing a basic or polar nitrogen containing fucntionality. The prodrugs are provided as pharmaceutical compositions as well as in methods of treatment. A compound of said formula wherein [(H)0-2(X)1-3] is selected from the group consisting of X3, HX2, and H2X and X2 is a halogen selected from the group consisting of F, Cl, Br, I or a combination thereof; R?2 and R3¿ are the same or different and are selected from the group consisting of H, C¿1?-C4alkyl, C1-C4alkoxy, cyano, halo(F, Cl, Br, I) C1-C4alkyl and aryl, AG-Q is a biologically active pharmaceutical agent wherein Q is a basic N-containing functionality selected from the group consisting of an amino, amidino, aminoalkyleneamino, iminoalkyleneamino, and guanidino group.
摘要翻译： 式（I）的卤代 - 烷氧基羰基衍生物作为含有碱性或极性含氮官能团的药剂的前药部分提供。 前药作为药物组合物以及治疗方法提供。 上式的化合物，其中[（H）0-2（X）1-3]选自X3，HX2和H2X，X2是选自F，Cl，Br， 我或其组合; R 2和R 3'相同或不同，选自H，C 1 -C 4烷基，C 1 -C 4烷氧基，氰基，卤代（F，Cl，Br，I）C 1 -C 4烷基和芳基， AG-Q是生物活性药剂，其中Q是选自氨基，脒基，氨基亚烷基氨基，亚氨基亚烷基氨基和胍基的基本的含N官能团。
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公开(公告)号：EP2207781B1
公开(公告)日：2012-11-28
申请号：EP08832932.1
申请日：2008-09-23
发明人： CASTANEDO, Georgette, M. , GUNZNER, Janet, L. , MALESKY, Kimberly , MATHIEU, Simon , OLIVERO, Alan, G. , SUTHERLIN, Daniel, P. , WANG, Shumei , ZHU, Bing-yan , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan Chi
IPC分类号： C07D513/04 , A61K31/519 , A61P35/00
CPC分类号： C07D513/04
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公开(公告)号：EP2207781A1
公开(公告)日：2010-07-21
申请号：EP08832932.1
申请日：2008-09-23
发明人： CASTANEDO, Georgette, M. , GUNZNER, Janet, L. , MALESKY, Kimberly , MATHIEU, Simon , OLIVERO, Alan, G. , SUTHERLIN, Daniel, P. , WANG, Shumei , ZHU, Bing-yan , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan Chi
IPC分类号： C07D513/04 , A61K31/519 , A61P35/00
CPC分类号： C07D513/04
摘要： Compounds of Formulas (Ia and Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式（Ia和Ib）化合物，包括其立体异构体，几何异构体，互变异构体，溶剂化物，代谢物和药学上可接受的盐可用于抑制包括PI3K在内的脂质激酶，以及用于治疗诸如由脂质激酶介导的癌症等疾病。 公开了使用式Ia和Ib化合物体外，原位和体内诊断，预防或治疗哺乳动物细胞中的此类病症或相关病理学病症的方法。
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公开(公告)号：EP0975608B1
公开(公告)日：2005-06-15
申请号：EP98913417.6
申请日：1998-04-08
申请人： Genentech, Inc.
IPC分类号： C07D243/24 , A61K31/55
CPC分类号： C07D243/14
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