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公开(公告)号：US20210171545A1
公开(公告)日：2021-06-10
申请号：US16944581
申请日：2020-07-31
发明人： Kenneth W. Bair , Timm R. Baumeister , Peter Dragovich , Xiongcai Liu , Snahel Patel , Po-Wai Yuen , Mark Zak , Guiling Zhao , Yamin Zhang , Xiaozhang Zheng
IPC分类号： C07D519/00 , C07D495/04 , C07D471/04 , C07D487/04 , C07D491/048 , A61K31/438 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K31/444 , A61K31/4545 , A61K31/506 , A61K31/513
摘要： Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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公开(公告)号：US12090211B2
公开(公告)日：2024-09-17
申请号：US17990988
申请日：2022-11-21
申请人： Genentech, Inc.
发明人： Thomas Pillow , Peter Dragovich
CPC分类号： A61K47/6803 , A61K47/65 , A61K47/6889 , C07K16/22 , C07K16/2863
摘要： The subject matter described herein is directed to methods of preparing certain antibody-drug conjugates (ADCs) wherein the antibody is linked to the drug through a linker, wherein the drug contains a heteroaryl group having a secondary nitrogen, and the linker is attached to the drug via the secondary nitrogen. The resulting conjugates are useful in treating various diseases and conditions.
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公开(公告)号：US11666581B2
公开(公告)日：2023-06-06
申请号：US16194897
申请日：2018-11-19
申请人： Genentech, Inc.
发明人： Thomas Pillow , Jack Sadowsky , Leanna Staben , Steven Staben , Binqing Wei , Ingrid Wertz , Pragya Adhikari , Nicole Blaquiere , Peter Dragovich , Wayne Fairbrother
IPC分类号： A61K31/551 , A61K47/54 , A61K47/68 , A61K47/65 , A61P37/06 , A61P35/00 , C07K16/28 , C07K16/32 , C12N9/00
CPC分类号： A61K31/551 , A61K47/545 , A61K47/65 , A61K47/68 , A61P35/00 , A61P37/06 , C07K16/2827 , C07K16/32 , C12N9/93 , C12Y203/02007
摘要： The subject matter described herein is directed to antibody-PROTAC conjugates (PACs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.
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公开(公告)号：US20210309660A1
公开(公告)日：2021-10-07
申请号：US16858004
申请日：2020-04-24
申请人： Genentech, Inc.
发明人： Nicole Blaquiere , Peter Dragovich , Lewis J. Gazzard , Thomas Pillow , Steven T. Staben , Binqing Wei , Jianfeng Xin
IPC分类号： C07D471/16 , C07D493/10 , C07D403/04 , C07D417/14 , C07D413/14 , A61P35/00
摘要： The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands.
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公开(公告)号：US20190175612A1
公开(公告)日：2019-06-13
申请号：US16194897
申请日：2018-11-19
申请人： Genentech, Inc.
发明人： Thomas Pillow , Jack Sadowsky , Leanna Staben , Steven Staben , Binqing Wei , Ingrid Wertz , Pragya Adhikari , Nicole Blaquiere , Peter Dragovich , Wayne Fairbrother
摘要： The subject matter described herein is directed to antibody-PROTAC conjugates (PACs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.
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公开(公告)号：US20180185486A1
公开(公告)日：2018-07-05
申请号：US15899612
申请日：2018-02-20
申请人： Genentech, Inc.
IPC分类号： A61K45/06 , C07D519/00 , A61K47/68 , C07K16/32 , C07K16/28 , A61K31/5517
CPC分类号： A61K45/06 , A61K31/5517 , A61K47/6803 , A61K47/6851 , A61K47/6855 , A61K47/6889 , C07D519/00 , C07K16/2803 , C07K16/32 , C07K2317/40 , C07K2317/522 , C07K2317/567
摘要： The invention provides antibody-drug conjugates comprising an antibody conjugated to a pyrrolobenzodiazepine drug moiety via a disulfide linker, pyrrolobenzodiazepine linker-drug intermediates, and methods of using the antibody-drug conjugates.
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公开(公告)号：US11485745B2
公开(公告)日：2022-11-01
申请号：US16944581
申请日：2020-07-31
申请人： Valo Health, Inc. , Genentech, Inc.
发明人： Kenneth W. Bair , Timm R. Baumeister , Peter Dragovich , Xiongcai Liu , Snahel Patel , Po-Wai Yuen , Mark Zak , Guiling Zhao , Yamin Zhang , Xiaozhang Zheng
IPC分类号： C07D519/00 , C07D495/04 , C07D471/04 , C07D487/04 , C07D491/048 , A61K31/438 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K31/444 , A61K31/4545 , A61K31/506 , A61K31/513
摘要： Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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公开(公告)号：US20190388405A1
公开(公告)日：2019-12-26
申请号：US16538208
申请日：2019-08-12
申请人： Forma TM, LLC , Genentech, Inc.
发明人： Kenneth W. Bair , Timm R. Baumeister , Alexandre J. Buckmelter , Karl H. Clodfelter , Peter Dragovich , Francis Gosselin , Bingsong Han , Jian Lin , Dominic J. Reynolds , Bruce Roth , Chase C. Smith , Zhongguo Wang , Po-Wai Yuen , Xiaozhang Zheng
IPC分类号： A61K31/4355 , C07D491/048 , C07D487/04 , A61K45/06 , A61K31/55 , A61K31/5377 , A61K31/519 , A61K31/497 , A61K31/496 , A61K31/437 , A61K31/4365 , C07D495/04 , C07D491/04 , C07D471/04
摘要： The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号：US10272072B2
公开(公告)日：2019-04-30
申请号：US15352184
申请日：2016-11-15
申请人： Forma TM, LLC , Genentech, Inc.
发明人： Kenneth W. Bair , Timm R. Baumeister , Alexandre Joseph Buckmelter , Karl H. Clodfelter , Peter Dragovich , Francis Gosselin , Bingsong Han , Jian Lin , Dominic J. Reynolds , Bruce Roth , Chase C. Smith , Zhongguo Wang , Po-Wai Yuen , Xiaozhang Zheng
IPC分类号： A61K31/4353 , A61K31/497 , A61K31/5377 , A61K31/4355 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/4365 , A61K31/437 , A61K31/496 , A61K31/519 , A61K31/55 , A61K45/06 , C07D487/04 , C07D491/048
摘要： The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号：US20180326062A1
公开(公告)日：2018-11-15
申请号：US16036575
申请日：2018-07-16
申请人： Genentech, Inc.
IPC分类号： A61K45/06 , A61K47/68 , A61K31/5517 , C07K16/32 , C07D519/00 , C07K16/28
CPC分类号： A61K45/06 , A61K31/5517 , A61K47/6803 , A61K47/6851 , A61K47/6855 , A61K47/6889 , C07D519/00 , C07K16/2803 , C07K16/32 , C07K2317/40 , C07K2317/522 , C07K2317/567
摘要： The invention provides antibody-drug conjugates comprising an antibody conjugated to a pyrrolobenzodiazepine drug moiety via a disulfide linker, pyrrolobenzodiazepine linker-drug intermediates, and methods of using the antibody-drug conjugates.
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