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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
Applicant: Irina Chuckowree , Adrian Folkes , Tim Hancox , Stephen Shuttleworth
Inventor： Irina Chuckowree , Adrian Folkes , Tim Hancox , Stephen Shuttleworth
CPC classification number: A61K31/5355 , C07D495/04
Abstract: 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.
Abstract translation: 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：US20090318411A1
公开(公告)日：2009-12-24
申请号：US12474613
申请日：2009-05-29
Applicant: Georgette Castanedo , Irina Chuckowree , Adrian Folkes , Daniel P. Sutherlin , Nan Chi Wan
Inventor： Georgette Castanedo , Irina Chuckowree , Adrian Folkes , Daniel P. Sutherlin , Nan Chi Wan
IPC: A61K31/5377 , C07D473/00
CPC classification number: C07D473/32
Abstract: 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.
Abstract translation: 式I的嘌呤化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗诸如由脂质激酶介导的癌症 。 公开了使用式I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：US09487533B2
公开(公告)日：2016-11-08
申请号：US11951189
申请日：2007-12-05
Applicant: Georgette Castanedo , Jennafer Dotson , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Shumei Wang , Bing-Yan Zhu , Steven Staben , Vickie Tsui , Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Nan Chi Wan
Inventor： Georgette Castanedo , Jennafer Dotson , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Shumei Wang , Bing-Yan Zhu , Steven Staben , Vickie Tsui , Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Nan Chi Wan
IPC: C07D491/048 , C07D495/04
CPC classification number: C07D491/048 , C07D495/04
Abstract: 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.
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公开(公告)号：US08802670B2
公开(公告)日：2014-08-12
申请号：US11789468
申请日：2007-04-24
Applicant: Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Bing-Yan Zhu
Inventor： Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Bing-Yan Zhu
IPC: A61K31/535 , C07D413/14
CPC classification number: A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048 , C07D495/04
Abstract: Compounds of Formulae Ia 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 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.
Abstract translation: 式Ia和Ib的化合物及其立体异构体，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：US20130230585A1
公开(公告)日：2013-09-05
申请号：US13669174
申请日：2012-11-05
Applicant: Irina Chuckowree , Adrian Folkes , Tim Hancox , Stephen Shuttleworth
Inventor： Irina Chuckowree , Adrian Folkes , Tim Hancox , Stephen Shuttleworth
IPC: A61K31/5355
CPC classification number: A61K31/5355 , C07D495/04
Abstract: 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.
Abstract translation: 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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Patent Agency Ranking
公开(公告)号：US20080242665A1
公开(公告)日：2008-10-02
申请号：US11951203
申请日：2007-12-05
Applicant: Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Steven Staben , Daniel P. Sutherlin , Bing-Yan Zhu
Inventor： Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Steven Staben , Daniel P. Sutherlin , Bing-Yan Zhu
IPC: A61K31/5377 , C07D495/04 , A61P35/04
CPC classification number: A61K31/5377 , A61K31/519 , C07D413/14 , C07D491/04 , C07D495/04
Abstract: 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.
Abstract translation: 式Ia-d的化合物，其中X是S或O，mor是吗啉基团，R 3是单环杂芳基，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 其盐可用于调节脂质激酶（包括PI3K）的活性，以及用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式Ia-d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：US20080076768A1
公开(公告)日：2008-03-27
申请号：US11789423
申请日：2007-04-24
Applicant: Irina Chuckowree , Adrian Folkes , Tim Hancox , Stephen Shuttleworth
Inventor： Irina Chuckowree , Adrian Folkes , Tim Hancox , Stephen Shuttleworth
IPC: A61K31/5355 , A61P29/00 , A61P3/00 , A61P31/12 , A61P35/00 , A61P37/00 , A61P5/00 , A61P9/00 , C07D413/14
CPC classification number: A61K31/5355 , C07D495/04
Abstract: 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.
Abstract translation: 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：US20080076758A1
公开(公告)日：2008-03-27
申请号：US11789468
申请日：2007-04-24
Applicant: Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel Sutherlin , Bing-Yan Zhu
Inventor： Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel Sutherlin , Bing-Yan Zhu
IPC: A61K31/5377 , A61K31/551 , A61P25/00 , A61P29/00 , A61P3/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P9/00 , C07D491/048 , C07D495/04
CPC classification number: A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048 , C07D495/04
Abstract: Compounds of Formulae Ia 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 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.
Abstract translation: 式Ia和Ib的化合物及其立体异构体，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：US08445487B2
公开(公告)日：2013-05-21
申请号：US13369941
申请日：2012-02-09
Applicant: Georgette Castanedo , Irina Chuckowree , Adrian Folkes , Daniel P. Sutherlin , Nan Chi Wan
Inventor： Georgette Castanedo , Irina Chuckowree , Adrian Folkes , Daniel P. Sutherlin , Nan Chi Wan
IPC: A61K31/535 , C07D413/00 , C07D473/00
CPC classification number: C07D473/32
Abstract: 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.
Abstract translation: 式I的嘌呤化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗诸如由脂质激酶介导的癌症 。 公开了使用式I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：US20120135988A1
公开(公告)日：2012-05-31
申请号：US13369941
申请日：2012-02-09
Applicant: Georgette Castanedo , Irina Chuckowree , Adrian Folkes , Daniel P. Sutherlin , Nan Chi Wan
Inventor： Georgette Castanedo , Irina Chuckowree , Adrian Folkes , Daniel P. Sutherlin , Nan Chi Wan
IPC: A61K31/5377 , A61P35/02 , A61P35/00
CPC classification number: C07D473/32
Abstract: 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.
Abstract translation: 式I的嘌呤化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗诸如由脂质激酶介导的癌症 。 公开了使用式I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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