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公开(公告)号：US20080039459A1
公开(公告)日：2008-02-14
申请号：US11789427
申请日：2007-04-24
申请人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
发明人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
IPC分类号： C07D413/14 , A61K31/5377 , A61P17/00 , A61P25/00 , A61P3/00 , A61P3/10 , C12N9/99 , A61P31/00 , A61P35/00 , A61P41/00 , A61P9/00
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，并且包括立体异构体，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。 公开了将式Ia和Ib化合物用于体外，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：US07846929B2
公开(公告)日：2010-12-07
申请号：US11789427
申请日：2007-04-24
申请人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
发明人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
IPC分类号： A61K31/5377 , C07D413/14
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，并且包括立体异构体，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。 公开了将式Ia和Ib化合物用于体外，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：US20110105464A1
公开(公告)日：2011-05-05
申请号：US12916125
申请日：2010-10-29
申请人： Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson , Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss
发明人： Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson , Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss
CPC分类号： C07D491/04 , C07D495/04
摘要： 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： 公开了将式Ia和Ib化合物用于体外，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：US08450315B2
公开(公告)日：2013-05-28
申请号：US12916125
申请日：2010-10-29
申请人： Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson , Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss
发明人： Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson , Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss
IPC分类号： A61K31/5377
CPC分类号： C07D491/04 , C07D495/04
摘要： 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： 公开了将式Ia和Ib化合物用于体外，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：US20110065701A1
公开(公告)日：2011-03-17
申请号：US12840070
申请日：2010-07-20
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.
摘要翻译： 式（I）的噻吩并嘧啶及其药学上可接受的盐具有作为P110α亚型选择性的PI3K抑制剂的活性，并且可用于治疗由异常细胞生长，功能或行为引起的疾病和障碍，特别是与 PI3激酶如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌障碍和神经障碍。 还描述了合成化合物的方法。
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公开(公告)号：US20130230585A1
公开(公告)日：2013-09-05
申请号：US13669174
申请日：2012-11-05
IPC分类号： A61K31/5355
CPC分类号： A61K31/5355 , C07D495/04
摘要： Provided herein is a pharmaceutical composition that comprises a pharmaceutically acceptable carrier or diluent and, as an active ingredient, the compound 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine bismesylate.
摘要翻译： 本文提供了包含药学上可接受的载体或稀释剂，作为活性成分的化合物2-（1H-吲唑-4-基）-6-（4-甲磺酰基 - 哌嗪-1-基甲基）-4 - 吗啉-4-基 - 噻吩并[3,2-d]嘧啶二甲酸苯酯。
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公开(公告)号：US20080076768A1
公开(公告)日：2008-03-27
申请号：US11789423
申请日：2007-04-24
IPC分类号： A61K31/5355 , A61P29/00 , A61P3/00 , A61P31/12 , A61P35/00 , A61P37/00 , A61P5/00 , A61P9/00 , C07D413/14
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.
摘要翻译： 式（I）的噻吩并嘧啶及其药学上可接受的盐具有作为P110α亚型选择性的PI3K抑制剂的活性，并且可用于治疗由异常细胞生长，功能或行为引起的疾病和障碍，特别是与 PI3激酶如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌障碍和神经障碍。 还描述了合成化合物的方法。
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公开(公告)号：US08324206B2
公开(公告)日：2012-12-04
申请号：US12840070
申请日：2010-07-20
IPC分类号： A61K31/535
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.
摘要翻译： 式（I）的噻吩并嘧啶及其药学上可接受的盐具有作为P110α亚型选择性的PI3K抑制剂的活性，并且可用于治疗由异常细胞生长，功能或行为引起的疾病和障碍，特别是与 PI3激酶如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌障碍和神经障碍。 还描述了合成化合物的方法。
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公开(公告)号：US07781433B2
公开(公告)日：2010-08-24
申请号：US11789423
申请日：2007-04-24
IPC分类号： A61K31/535 , C07D413/14
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.
摘要翻译： 式（I）的噻吩并嘧啶及其药学上可接受的盐具有作为P110α亚型选择性的PI3K抑制剂的活性，并且可用于治疗由异常细胞生长，功能或行为引起的疾病和障碍，特别是与 PI3激酶如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌障碍和神经障碍。 还描述了合成化合物的方法。
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