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公开(公告)号:US10010549B2
公开(公告)日:2018-07-03
申请号:US14927267
申请日:2015-10-29
Applicant: Genentech, Inc.
Inventor: Anthony Estrada , Liting Dong , Kevin X. Chen , Paul Gibbons , Malcolm Huestis , Terry Kellar , Wen Liu , Changyou Ma , Joseph Lyssikatos , Alan Olivero , Snahel Patel , Daniel Shore , Michael Siu
IPC: A61K31/506 , A61K31/4545 , A61K31/5377 , A61K31/55 , A61K35/30 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D471/18 , C07D487/08 , C07D491/08 , C07D495/08 , C07D519/00 , C07D471/08 , A61K45/06 , A61K31/5386 , A61K31/553 , C07D417/14 , C07D487/14 , C07D487/18 , A61K31/444
CPC classification number: A61K31/506 , A61K31/444 , A61K31/4545 , A61K31/5377 , A61K31/5386 , A61K31/55 , A61K31/553 , A61K35/30 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D471/18 , C07D487/08 , C07D487/14 , C07D487/18 , C07D491/08 , C07D495/08 , C07D519/00 , A61K2300/00
Abstract: The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula I-I all have the meaning as defined herein.
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公开(公告)号:US20180133219A1
公开(公告)日:2018-05-17
申请号:US15868301
申请日:2018-01-11
Applicant: Genentech, Inc.
Inventor: Anthony Estrada , Liting Dong , Kevin X. Chen , Paul Gibbons , Malcolm Huestis , Terry Kellar , Wen Liu , Changyou Ma , Joseph Lyssikatos , Alan Olivero , Snahel Patel , Daniel Shore , Michael Siu
IPC: A61K31/506 , A61K31/444 , A61K35/30 , C07D487/14 , A61K31/553 , C07D417/14 , C07D487/18 , A61K31/55 , C07D401/14 , A61K31/5377 , C07D495/08 , A61K31/4545 , C07D519/00 , A61K31/5386 , A61K45/06 , C07D471/08 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D471/18 , C07D487/08 , C07D491/08
CPC classification number: A61K31/506 , A61K31/444 , A61K31/4545 , A61K31/5377 , A61K31/5386 , A61K31/55 , A61K31/553 , A61K35/30 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D471/18 , C07D487/08 , C07D487/14 , C07D487/18 , C07D491/08 , C07D495/08 , C07D519/00 , A61K2300/00
Abstract: The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula I-I all have the meaning as defined herein.
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公开(公告)号:US11643421B2
公开(公告)日:2023-05-09
申请号:US17115095
申请日:2020-12-08
Applicant: Genentech, Inc.
Inventor: Andreas Stumpf , Remy Angelaud , Andrew McClory , Herbert Yajima , Chudi Ndubaku , Alan Olivero
IPC: C07D498/14 , C07D487/04 , C07D498/22 , A61P35/00 , A61K9/00 , A61K31/495 , A61K31/5383 , A61K39/395 , A61K45/06
CPC classification number: C07D498/14 , A61K9/0053 , A61K31/495 , A61K31/5383 , A61K39/3955 , A61K45/06 , A61P35/00 , C07D487/04 , C07D498/22
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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公开(公告)号:US20210253599A1
公开(公告)日:2021-08-19
申请号:US17115095
申请日:2020-12-08
Applicant: Genentech, Inc.
Inventor: Andreas Stumpf , Remy Angelaud , Andrew McClory , Herbert Yajima , Chudi Ndubaku , Alan Olivero
IPC: C07D498/14 , C07D487/04 , C07D498/22 , A61P35/00 , A61K9/00 , A61K31/495 , A61K31/5383 , A61K39/395 , A61K45/06
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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公开(公告)号:US10906918B2
公开(公告)日:2021-02-02
申请号:US15780328
申请日:2016-12-16
Applicant: GENENTECH, INC.
Inventor: Andreas Stumpf , Remy Angelaud , Andrew McClory , Herbert Yajima , Chudi Ndubaku , Alan Olivero
IPC: C07D498/14 , C07D487/04 , C07D498/22 , A61P35/00 , A61K9/00 , A61K31/495 , A61K31/5383 , A61K39/395 , A61K45/06
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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公开(公告)号:US20160152632A9
公开(公告)日:2016-06-02
申请号:US14316166
申请日:2014-06-26
Applicant: F.HOFFMANN-LA ROCHE AG , GENENTECH, INC.
Inventor: Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzer-Toste , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Bing-Yan Zhu
IPC: C07D495/04 , A61K45/06 , A61K31/551 , A61K31/5377 , C07D491/048
CPC classification number: A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048 , C07D495/04
Abstract: Compounds of Formulae Ia, 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 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化合物和立体异构体,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条件中的这种病症的方法。
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公开(公告)号:US20140309216A1
公开(公告)日:2014-10-16
申请号:US14316166
申请日:2014-06-26
Applicant: F.HOFFMANN-LA ROCHE AG , GENENTECH, INC.
Inventor: Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzer-Toste , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Bing-Yan Zhu
IPC: C07D495/04 , A61K45/06 , A61K31/551 , A61K31/5377 , C07D491/048
CPC classification number: A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048 , C07D495/04
Abstract: Compounds of Formulae Ia, 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 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化合物和立体异构体,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条件中的这种病症的方法。
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8.
公开(公告)号:US20230242550A1
公开(公告)日:2023-08-03
申请号:US18189623
申请日:2023-03-24
Applicant: Genentech, Inc.
Inventor: Andreas Stumpf , Remy Angelaud , Andrew McClory , Herbert Yajima , Chudi Ndubaku , Alan Olivero
IPC: C07D498/14 , C07D487/04 , C07D498/22 , A61P35/00 , A61K9/00 , A61K31/495 , A61K31/5383 , A61K39/395 , A61K45/06
CPC classification number: C07D498/14 , C07D487/04 , C07D498/22 , A61P35/00 , A61K9/0053 , A61K31/495 , A61K31/5383 , A61K39/3955 , A61K45/06
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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9.
公开(公告)号:US20180354970A1
公开(公告)日:2018-12-13
申请号:US15780328
申请日:2016-12-16
Applicant: GENENTECH, INC.
Inventor: Andreas Stumpf , Remy Angelaud , Andrew McClory , Herbert Yajima , Chudi Ndubaku , Alan Olivero
IPC: C07D498/14 , A61P35/00 , A61K9/00 , A61K45/06 , A61K39/395 , A61K31/495 , A61K31/5383
CPC classification number: C07D498/14 , A61K9/0053 , A61K31/495 , A61K31/5383 , A61K39/3955 , A61K45/06 , A61P35/00 , C07D487/04 , C07D498/22
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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公开(公告)号:US09943519B2
公开(公告)日:2018-04-17
申请号:US14316166
申请日:2014-06-26
Applicant: F.HOFFMANN-LA ROCHE AG , GENENTECH, INC.
Inventor: Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzer-Toste , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Bing-Yan Zhu
IPC: C07D413/14 , A61K31/535 , A61K31/5377 , C07D491/04 , C07D495/04 , A61K31/551 , A61K45/06 , C07D491/048
CPC classification number: A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048 , C07D495/04
Abstract: Compounds of Formulae Ia, 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 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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