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公开(公告)号：US20220389020A1
公开(公告)日：2022-12-08
申请号：US17648045
申请日：2022-01-14
申请人： Genentech, Inc.
发明人： Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark E. Zak , Aihe Zhou , Bing-Yan Zhu , Christopher Hurley
IPC分类号： C07D487/04 , A61P17/06 , A61P35/02 , A61K31/519 , A61P29/00
摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.
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公开(公告)号：US20220306635A1
公开(公告)日：2022-09-29
申请号：US17068574
申请日：2020-10-12
发明人： Xingyu Lin , Po-wai Yuen , Rohan Mendonca , Brendan Parr , Richard Pastor , Zhonghua Pei , Lewis Gazzard , Firoz Jaipuri , Sanjeev Kumar , Xiaokai Li , Roheeth Pavana , Hima Potturi , Venkata Velvadapu , Jesse Waldo , Zuhui Zhang , Guosheng Wu , Benjamin Douglas Sellers
IPC分类号： C07D487/04 , A61P35/00 , A61K38/16 , A61K45/06 , C07D519/00
摘要： Presently provided are inhibitors of cellularly expressed TD02 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
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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：US20190016726A1
公开(公告)日：2019-01-17
申请号：US16065397
申请日：2016-12-23
发明人： Xingyu Lin , Po-wai Yuen , Rohan Mendonca , Brendan Parr , Richard Pastor , Zhonghua Pei , Lewis Gazzard , Firoz Jaipuri , Sanjeev Kumar , Xiaokai Li , Roheeth Pavana , Hima Potturi , Venkata Velvadapu , Jesse Waldo , Zuhui Zhang , Guosheng Wu
IPC分类号： C07D487/04 , A61P35/00 , C07D519/00 , A61K38/16
摘要： Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
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5.发明申请公开(公告)号：US20170145020A1
公开(公告)日：2017-05-25
申请号：US15424536
申请日：2017-02-03
申请人： Genentech, Inc.
发明人： Mark Edward Zak , Nicholas Charles Ray , Simon Charles Goodacre , Rohan Mendonca , Terry Kellar , Yun-Xing Cheng , Wei Li , Po-Wei Yuen
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/519 , A61P11/06 , C07D403/14 , C07D487/04 , C07D519/00
摘要： Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.
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公开(公告)号：US20220204517A1
公开(公告)日：2022-06-30
申请号：US17654131
申请日：2022-03-09
申请人： Genentech, Inc.
发明人： Yun-Xing Cheng , Paul Gibbons , Terry Kellar , Wei Li , Rohan Mendonca , Po-wai Yuen , Mark Edward Zak , Lei Zhang
IPC分类号： C07D487/04 , C07D519/00
摘要： Compounds of Formula (00A) and salts thereof, wherein R1, R2 R3, R4 and n are defined herein, are useful as inhibitors of one or more Janus kinases. Also provided are pharmaceutical compositions that include a compound of Formula (00A) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
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公开(公告)号：US20210163417A1
公开(公告)日：2021-06-03
申请号：US16921297
申请日：2020-07-06
申请人： Genentech, Inc.
发明人： Bryan Chan , Joy Drobnick , Lewis Gazzard , Timothy Heffron , Jun Liang , Sushant Malhotra , Rohan Mendonca , Naomi Rajapaksa , Craig Stivala , John Tellis , Weiru Wang , BinQing Wei , Aihe Zhou , Matthew W. Cartwright , Michael Lainchbury , Emanuela Gancia , Eileen Seward , Andrew Madin , David Favor , Kin Chiu Fong , Yonghan Hu , Andrew Good
IPC分类号： C07D217/22 , A61K31/549 , A61P35/00 , A61K45/06 , C07D401/04 , A61K31/4725 , A61K31/506 , A61K31/501 , C07D471/04 , C07D413/04 , C07D413/14 , A61K31/5377 , C07D417/04 , A61K31/4985 , C07D401/14 , C07D487/04 , A61K31/551 , C07D498/04 , A61K31/5383 , C07D405/14 , C07D519/00 , C07D498/14 , C07D513/04 , A61K31/554 , A61K31/55 , A61K31/472 , C07D409/14 , C07D491/04 , C07D487/14
摘要： Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) 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 isoquinoline compounds.
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8.发明申请公开(公告)号：US20190322661A1
公开(公告)日：2019-10-24
申请号：US16438135
申请日：2019-06-11
申请人： Genentech, Inc.
发明人： Mark Edward Zak , Nicholas Charles Ray , Simon Charles Goodacre , Rohan Mendonca , Terry Kellar , Yun-Xing Cheng , Wei Li , Po-wai Yuen
IPC分类号： C07D471/04 , C07D487/04 , C07D403/14 , A61K31/519 , C07D519/00 , A61P11/06
摘要： Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.
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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：US20180282282A1
公开(公告)日：2018-10-04
申请号：US15942333
申请日：2018-03-30
申请人： Genentech, Inc.
发明人： Bryan Chan , Joy Drobnick , Lewis Gazzard , Timothy Heffron , Jun Liang , Sushant Malhotra , Rohan Mendonca , Naomi Rajapaksa , Craig Stivala , John Tellis , Weiru Wang , BinQing Wei , Aihe Zhou , Matthew W. Cartwright , Michael Lainchbury , Emanuela Gancia , Eileen Seward , Andrew Madin , David Favor , Kin Chiu Fong , Yonghan Hu , Andrew Good
IPC分类号： C07D217/22 , A61K31/472 , A61P35/00 , A61K45/06 , C07D401/04 , A61K31/4725 , A61K31/506 , A61K31/501 , C07D471/04 , C07D413/04 , C07D413/14 , A61K31/5377 , C07D417/04 , A61K31/4985 , C07D401/14 , C07D487/04 , A61K31/551 , C07D498/04 , A61K31/5383 , C07D405/14 , C07D519/00 , C07D498/14 , C07D513/04 , A61K31/554 , A61K31/55 , A61K31/549
摘要： Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibitng HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.
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