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公开(公告)号：US10711004B2
公开(公告)日：2020-07-14
申请号：US16558718
申请日：2019-09-03
申请人： Genentech, Inc.
发明人： Huifen Chen , Brian Safina , Daniel Shore , Jack Terrett , Elisia Villemure , Matthew Volgraf , Stuart Ward , Aijun Lu , Robin Larouche-Gauthier , Francis Beaumier , Martin Dery , Lea Constantineau-Forget , Chantal Grand-Maitre , Luce Lepissier
IPC分类号： C07D473/30 , C07D471/04 , C07D487/04 , C07D473/08
摘要： The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
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公开(公告)号：US20180327420A1
公开(公告)日：2018-11-15
申请号：US16044862
申请日：2018-07-25
申请人： Genentech, Inc.
发明人： Marie-Gabrielle Braun , Keira Garland , Emily Hanan , Hans Purkey , Steven T. Staben , Robert Andrew Heald , Jamie Knight , Calum Macleod , Aijun Lu , Guosheng Wu , Siew Kuen Yeap
IPC分类号： C07D498/04 , C07D519/00 , C07D498/06 , A61K31/5365 , A61K31/4188 , A61K31/498 , A61K31/4196 , C07D491/044 , A61K31/428 , A61K31/4439 , A61K31/5383 , A61K31/553 , A61K45/06 , A61K31/423
CPC分类号： C07D498/04 , A61K31/4188 , A61K31/4196 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/498 , A61K31/5365 , A61K31/5383 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/06 , C07D519/00
摘要： Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
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公开(公告)号：US11034692B1
公开(公告)日：2021-06-15
申请号：US16542129
申请日：2019-08-15
申请人： Genentech, Inc.
发明人： Bryan Chan , Blake Daniels , Joy Drobnick , Lewis Gazzard , Timothy Heffron , Malcolm Huestis , Jun Liang , Sushant Malhotra , Rohan Mendonca , Naomi Rajapaksa , Michael Siu , Craig Stivala , John Tellis , Weiru Wang , BinQing Wei , Aihe Zhou , Matthew W. Cartwright , Emanuela Gancia , Graham Jones , Michael Lainchbury , Andrew Madin , Eileen Seward , David Favor , Kin Chiu Fong , Andrew Good , Yonghan Hu , Baihua Hu , Aijun Lu
IPC分类号： C07D471/04 , A61K45/06 , A61P35/00 , A61K31/444 , A61K31/4375 , A61K31/506 , C07D519/00 , A61K31/4545 , A61K31/4725 , A61K31/5383 , A61K31/496 , A61K31/5377 , A61K31/5025 , A61K31/551 , A61K31/55
摘要： Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.
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公开(公告)号：US10435414B2
公开(公告)日：2019-10-08
申请号：US16044862
申请日：2018-07-25
申请人： Genentech, Inc.
发明人： Marie-Gabrielle Braun , Keira Garland , Emily Hanan , Hans Purkey , Steven T. Staben , Robert Andrew Heald , Jamie Knight , Calum Macleod , Aijun Lu , Guosheng Wu , Siew Kuen Yeap
IPC分类号： A61K31/4188 , A61K31/424 , A61K31/498 , A61K31/5365 , A61K45/06 , C07D498/04 , C07D498/06 , C07D519/00 , A61K31/4196 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/5383 , A61K31/553 , C07D491/044
摘要： Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
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公开(公告)号：US10407424B2
公开(公告)日：2019-09-10
申请号：US15942321
申请日：2018-03-30
申请人： Genentech, Inc.
发明人： Bryan Chan , Naomi Rajapaksa , Michael Siu , Craig Stivala , John Tellis , Weiru Wang , BinQing Wei , Aihe Zhou , Matthew W. Cartwright , Emanuela Gancia , Graham Jones , Blake Daniels , Michael Lainchbury , Andrew Madin , Eileen Seward , David Favor , Kin Chiu Fong , Andrew Good , Yonghan Hu , Baihua Hu , Aijun Lu , Joy Drobnick , Lewis Gazzard , Timothy Heffron , Malcolm Huestis , Jun Liang , Sushant Malhotra , Rohan Mendonca
IPC分类号： C07D471/04 , A61K31/55 , A61P35/00 , A61K31/444 , A61K31/4375 , A61K31/506 , C07D519/00 , A61K31/4545 , A61K31/4725 , A61K31/5383 , A61K31/496 , A61K31/5377 , A61K31/5025 , A61K31/551 , A61K45/06
摘要： Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.
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公开(公告)号：US20180065983A1
公开(公告)日：2018-03-08
申请号：US15258175
申请日：2016-09-07
申请人： Genentech, Inc.
发明人： Marie-Gabrielle Braun , Keira Garland , Emily Hanan , Hans Purkey , Steven T. Staben , Robert Andrew Heald , Jamie Knight , Calum Macleod , Aijun Lu , Guosheng Wu , Siew Kuen Yeap
IPC分类号： C07D498/04 , A61K31/553 , A61K31/5383 , A61K31/498 , A61K31/4439 , A61K31/428 , A61K31/423 , A61K31/4196 , C07D491/044 , A61K45/06 , C07D519/00
CPC分类号： C07D498/04 , A61K31/4188 , A61K31/4196 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/498 , A61K31/5365 , A61K31/5383 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/06 , C07D519/00
摘要： Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
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公开(公告)号：US10280165B2
公开(公告)日：2019-05-07
申请号：US15783373
申请日：2017-10-13
申请人： Genentech, Inc.
发明人： Matthew Volgraf , Yu Jiang , Elisia Villemure , Benjamin Sellers , Guosheng Wu , Aijun Lu
IPC分类号： A61K31/519 , C07D471/04 , A61P25/00
摘要： The invention relates to pyridopyrimidinone compounds of formula I or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5 and R6 are as defined herein, as well as pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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公开(公告)号：US10179782B2
公开(公告)日：2019-01-15
申请号：US15042310
申请日：2016-02-12
申请人： Genentech, Inc.
发明人： Anthony Estrada , Elisia Villemure , Vishal Verma , Daniel Shore , Matthew Volgraf , Baihua Hu , Aijun Lu
IPC分类号： C07D417/14 , C07D403/12 , C07D401/14 , C07D405/14 , C07D401/12 , C07D403/14 , C07D409/14 , C07D417/12 , C07F9/6512
摘要： The invention is concerned with the compounds of formula I: and salts thereof and other compounds of formulas II-IX as disclosed herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formulas I-IX as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain or asthma.
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公开(公告)号：US20180282328A1
公开(公告)日：2018-10-04
申请号：US15942321
申请日：2018-03-30
申请人： Genentech, Inc.
发明人： Bryan Chan , Blake Daniels , Joy Drobnick , Lewis Gazzard , Timothy Heffron , Malcolm Huestis , Jun Liang , Sushant Malhotra , Rohan Mendonca , Naomi Rajapaksa , Michael Siu , Craig Stivala , John Tellis , Weiru Wang , BinQing Wei , Aihe Zhou , Matthew W. Cartwright , Emanuela Gancia , Graham Jones , Michael Lainchbury , Andrew Madin , Eileen Seward , David Favor , Kin Chiu Fong , Andrew Good , Yonghan Hu , Baihua Hu , Aijun Lu
IPC分类号： C07D471/04 , A61K45/06 , A61P35/00 , A61K31/444 , A61K31/4375 , A61K31/506 , C07D519/00 , A61K31/4545 , A61K31/4725 , A61K31/5383 , A61K31/496 , A61K31/5377 , A61K31/5025 , A61K31/551 , A61K31/55
CPC分类号： C07D471/04 , A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61K31/551 , A61K45/06 , A61P35/00 , C07D519/00
摘要： Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.
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公开(公告)号：US20180127414A1
公开(公告)日：2018-05-10
申请号：US15783373
申请日：2017-10-13
申请人： Genentech, Inc.
发明人： Matthew Volgraf , Yu Jiang , Elisia Villemure , Benjamin Sellers , Guosheng Wu , Aijun Lu
IPC分类号： C07D471/04 , A61P25/00
CPC分类号： C07D471/04 , A61P25/00
摘要： The invention relates to pyridopyrimidinone compounds of formula I or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5 and R6 are as defined herein, as well as pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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