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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
Applicant: Genentech, Inc.
Inventor: Thomas Pillow , Peter Dragovich
CPC classification number: A61K47/6803 , A61K47/65 , A61K47/6889 , C07K16/22 , C07K16/2863
Abstract: 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
Applicant: Genentech, Inc.
Inventor: Thomas Pillow , Jack Sadowsky , Leanna Staben , Steven Staben , Binqing Wei , Ingrid Wertz , Pragya Adhikari , Nicole Blaquiere , Peter Dragovich , Wayne Fairbrother
IPC: A61K31/551 , A61K47/54 , A61K47/68 , A61K47/65 , A61P37/06 , A61P35/00 , C07K16/28 , C07K16/32 , C12N9/00
CPC classification number: A61K31/551 , A61K47/545 , A61K47/65 , A61K47/68 , A61P35/00 , A61P37/06 , C07K16/2827 , C07K16/32 , C12N9/93 , C12Y203/02007
Abstract: 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
Applicant: Genentech, Inc.
Inventor: Nicole Blaquiere , Peter Dragovich , Lewis J. Gazzard , Thomas Pillow , Steven T. Staben , Binqing Wei , Jianfeng Xin
IPC: C07D471/16 , C07D493/10 , C07D403/04 , C07D417/14 , C07D413/14 , A61P35/00
Abstract: 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
Applicant: Genentech, Inc.
Inventor: Thomas Pillow , Jack Sadowsky , Leanna Staben , Steven Staben , Binqing Wei , Ingrid Wertz , Pragya Adhikari , Nicole Blaquiere , Peter Dragovich , Wayne Fairbrother
Abstract: 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
Applicant: Genentech, Inc.
Inventor: Peter Dragovich , Thomas Pillow , Jack Sadowsky , Mark X. Sliwkowski , BinQing Wei
IPC: A61K45/06 , C07D519/00 , A61K47/68 , C07K16/32 , C07K16/28 , A61K31/5517
CPC classification number: A61K45/06 , A61K31/5517 , A61K47/6803 , A61K47/6851 , A61K47/6855 , A61K47/6889 , C07D519/00 , C07K16/2803 , C07K16/32 , C07K2317/40 , C07K2317/522 , C07K2317/567
Abstract: 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
Applicant: Valo Health, Inc. , Genentech, Inc.
Inventor: Kenneth W. Bair , Timm R. Baumeister , Peter Dragovich , Xiongcai Liu , Snahel Patel , Po-Wai Yuen , Mark Zak , Guiling Zhao , Yamin Zhang , Xiaozhang Zheng
IPC: 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
Abstract: 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
Applicant: Forma TM, LLC , Genentech, Inc.
Inventor: 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: 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
Abstract: 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
Applicant: Forma TM, LLC , Genentech, Inc.
Inventor: 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: 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
Abstract: 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
Applicant: Genentech, Inc.
Inventor: Peter Dragovich , Thomas Pillow , Jack Sadowsky , Mark X. Sliwkowski , BinQing Wei
IPC: A61K45/06 , A61K47/68 , A61K31/5517 , C07K16/32 , C07D519/00 , C07K16/28
CPC classification number: A61K45/06 , A61K31/5517 , A61K47/6803 , A61K47/6851 , A61K47/6855 , A61K47/6889 , C07D519/00 , C07K16/2803 , C07K16/32 , C07K2317/40 , C07K2317/522 , C07K2317/567
Abstract: 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:US10022354B2
公开(公告)日:2018-07-17
申请号:US15482584
申请日:2017-04-07
Applicant: GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
Inventor: Kwong Wah Lai , Jun Liang , Birong Zhang , Sharada Labadie , Daniel Ortwine , Peter Dragovich , James Kiefer , Victor S. Gehling , Jean-Christophe Harmange
IPC: C07D237/04 , A61K31/41 , A61K31/4025 , C07D207/04
Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
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