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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：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：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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4.发明公开PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权磷酸三磷酸激酶HEMMENDE VERBINDUNGEN UND SIE ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN
公开(公告)号：EP2046799A1
公开(公告)日：2009-04-15
申请号：EP07776052.8
申请日：2007-04-24
发明人： CASTANEDO, Georgette , GOLDSMITH, Richard , GUNZNER, Janet , HEFFRON, Tim , MALESKY, Kimberly , MATHIEU, Simon , OLIVERO, Alan , SUTHERLIN, Daniel, P. , TSUI, Vickie , WANG, Shumei , WEISMANN, Christian , ZHU, Bing-Yan , DOTSON, Jennafer , FOLKES, Adrian , SHUTTLEWORTH, Stephen , OXENFORD, Sally , HANCOX, Tim , BAYLISS, Tracy
IPC分类号： C07D491/04 , C07D495/04 , C07D519/00 , A61K31/519 , A61P35/00
CPC分类号： C07D491/04 , C07D495/04
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的化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐，可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式Ia和Ib的化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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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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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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7.发明公开BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE 审中-公开台达P110选择性双环嘧啶，其PI3K抑制化合物及使用方法
公开(公告)号：EP2435438A1
公开(公告)日：2012-04-04
申请号：EP10720979.3
申请日：2010-05-26
发明人： CASTANEDO, Georgette , CHAN, Bryan , GOLDSTEIN, David Michael , KONDRU, Rama K. , LUCAS, Matthew C. , PALMER, Wylie Solang , PRICE, Stephen , SAFINA, Brian , SAVY, Pascal Pierre Alexandre , SEWARD, Eileen Mary , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
IPC分类号： C07D487/04 , C07D491/04 , C07D513/04 , A61K31/519 , A61P35/00 , A61P9/00 , A61P29/00 , A61P25/00
CPC分类号： C07D513/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Formula (I) ((Ia) and (Ib)) compounds wherein (i) X
1 is N and X
2 is S, (ii) X
1 is CR
7 and X
2 is S, (iii) X
1 is N and X
2 is NR
2 , or (iv) X
1 is CR
7 and X
2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. 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.-
公开(公告)号：EP3036230A1
公开(公告)日：2016-06-29
申请号：EP14755806.8
申请日：2014-08-22
发明人： BLAQUIERE, Nicole , BURCH, Jason , CASTANEDO, Georgette , FENG, Jianwen A. , HU, Baihua , STABEN, Steven , WU, Guosheng , YUEN, Po-wai
IPC分类号： C07D401/14 , C07D413/14 , C07D401/10 , C07D403/10 , C07D403/14 , C07D413/10 , C07D471/04 , C07D487/04 , C07D495/04 , C07D417/10 , C07D491/048 , C07D491/052 , C07D513/04 , A61K31/416 , A61K31/4155
CPC分类号： C07D513/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D403/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/052 , C07D495/04
摘要： The invention relates to compounds of Formula (0): wherein Q, A
1 -A
8 , R
4 and R
5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over- activation of NF-kB signaling is observed.摘要翻译： 本发明涉及式（O）的化合物：其中Q，A1-A8，R4和R5各自具有如本文所述的含义。 式（0）的化合物及其药物组合物可用于治疗其中观察到NF-kB信号传导的不期望或过度活化的疾病和病症。
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公开(公告)号：EP3036229A1
公开(公告)日：2016-06-29
申请号：EP14755363.0
申请日：2014-08-22
发明人： BLAQUIERE, Nicole , BURCH, Jason , CASTANEDO, Georgette , FENG, Jianwen A. , HU, Baihua , LIN, Xingyu , STABEN, Steven , WU, Guosheng , YUEN, Po-wai
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D401/10 , C07D403/10 , C07D403/14 , C07D409/14 , C07D413/10 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/107 , C07D495/04 , A61K31/439 , A61P29/00
CPC分类号： C07D401/10 , A61K31/395 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/107 , C07D495/04 , C07D495/06
摘要： wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
摘要翻译： 本发明涉及式（O）的化合物：其中A1-A8，R4和R5各自具有如本文所述的含义。 式（0）的化合物及其药物组合物可用于治疗其中观察到NF-kB信号传导的不期望或过度活化的疾病和病症。
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10.发明公开PYRIDO[3,2-D]PYRIMIDINE PI3K DELTA INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开吡啶并[3,2-d]嘧啶的PI3Kδ抑制剂的化合物及其使用方法
公开(公告)号：EP2539337A1
公开(公告)日：2013-01-02
申请号：EP11704604.5
申请日：2011-02-18
发明人： CASTANEDO, Georgette , CHAN, Bryan , LUCAS, Matthew C. , SAFINA, Brian , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , C07D491/107
摘要： Formula (I) compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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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