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公开(公告)号：EP2041139B1
公开(公告)日：2011-11-09
申请号：EP07755937.5
申请日：2007-04-24
发明人： FOLKES, Adrian , SHUTTLEWORTH, Stephen , CHUCKOWREE, Irina , OXENFORD, Sally , WAN, Nan Chi , CASTANEDO, Georgette , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , SUTHERLIN, Daniel, P. , ZHU, Bing-Yan , GOLDSMITH, Richard
IPC分类号： C07D491/04
CPC分类号： A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048 , C07D495/04
摘要： Compounds of Formulae la and Ib, and 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 la 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.
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公开(公告)号：EP2114949A1
公开(公告)日：2009-11-11
申请号：EP07854962.3
申请日：2007-12-05
发明人： BAYLISS, Tracy , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan, Chi , CASTANEDO, Georgette , GOLDSMITH, Richard , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , STABEN, Steven , SUTHERLIN, Daniel P. , ZHU, Bing-Yan
IPC分类号： C07D491/04 , C07D495/04 , A61K31/5377 , A61K31/519 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/519 , C07D413/14 , C07D491/04 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. [Insert Formula Ic and Id]
摘要翻译： 其中X是S或O，吗啉是吗啉基团，且R 3是单环杂芳基并包括其立体异构体，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的式Ia-d化合物可用于调节 包括PI3K的脂质激酶的活性，以及用于治疗诸如由脂质激酶介导的癌症的疾病。 公开了使用式Ia-d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。 [插入公式Ic和Id]
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公开(公告)号：EP2114950B1
公开(公告)日：2016-03-09
申请号：EP07865255.9
申请日：2007-12-05
发明人： CASTANEDO, Georgette , DOTSON, Jennafer , GOLDSMITH, Richard , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , STABEN, Steven , SUTHERLIN, Daniel P. , TSUI, Vickie , WANG, Shumei , ZHU, Bing-Yan , BAYLISS, Tracy , CHUCKOWREE, Irina , FOLKES, Adrian , WAN, Nan Chi
IPC分类号： C07D491/048 , C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D491/048 , C07D495/04
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公开(公告)号：EP2114950A2
公开(公告)日：2009-11-11
申请号：EP07865255.9
申请日：2007-12-05
发明人： CASTANEDO, Georgette , DOTSON, Jennafer , GOLDSMITH, Richard , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , STABEN, Steven , SUTHERLIN, Daniel P. , TSUI, Vickie , WANG, Shumei , ZHU, Bing-Yan , BAYLISS, Tracy , CHUCKOWREE, Irina , FOLKES, Adrian , WAN, Nan Chi
IPC分类号： C07D491/048 , C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D491/048 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. Formula (Ic) and (Id).
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公开(公告)号：EP2041139A2
公开(公告)日：2009-04-01
申请号：EP07755937.5
申请日：2007-04-24
发明人： FOLKES, Adrian , SHUTTLEWORTH, Stephen , CHUCKOWREE, Irina , OXENFORD, Sally , WAN, Nan Chi , CASTANEDO, Georgette , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , SUTHERLIN, Daniel, P. , ZHU, Bing-Yan , GOLDSMITH, Richard
IPC分类号： C07D491/04
CPC分类号： A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048 , C07D495/04
摘要： Compounds of Formulae la and Ib, and 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 la 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化合物及其立体异构体，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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6.发明公开
公开(公告)号：EP2024372A2
公开(公告)日：2009-02-18
申请号：EP07734376.2
申请日：2007-04-24
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： A61K31/5355 , C07D495/04
摘要： A thienopyrimidine of formula (I) and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K with selectivity for the P110α subtype, and may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour, particularly those associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
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公开(公告)号：EP2024372B1
公开(公告)日：2010-06-23
申请号：EP07734376.2
申请日：2007-04-24
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： A61K31/5355 , C07D495/04
摘要： A thienopyrimidine of formula (I) and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K with selectivity for the P110α subtype, and may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour, particularly those associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
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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：EP2279188A1
公开(公告)日：2011-02-02
申请号：EP09755767.2
申请日：2009-05-29
发明人： CASTANEDO, Georgette , CHUCKOWREE, Irina , FOLKES, Adrian , SUTHERLIN, Daniel, P. , WAN, Nan Chi
IPC分类号： C07D473/32 , A61P35/00 , A61K31/52
CPC分类号： C07D473/32
摘要： Purine compounds of Formula I, 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 Formula I for
in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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