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公开(公告)号：US20170112891A1
公开(公告)日：2017-04-27
申请号：US15293743
申请日：2016-10-14
Applicant: Genentech, Inc.
Inventor： Peter Dragovich , Zhonghua Pei , Thomas Pillow , Jack Sadowsky , Jinhua Chen , John Wai
IPC: A61K38/05 , A61K31/5365 , A61K31/5517
Abstract: The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.
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公开(公告)号：US20240076295A1
公开(公告)日：2024-03-07
申请号：US18108045
申请日：2023-02-10
Applicant: Arvinas Operations, Inc. , Genentech, Inc.
Inventor： Andrew P. Crew , Jing Wang , Michael Berlin , Peter Dragovich , Huifen Chen , Leanna Staben
IPC: C07D417/14 , A61K47/10 , A61K47/18 , A61K47/22 , A61K47/54 , A61P35/00 , C07D413/14
CPC classification number: C07D417/14 , A61K47/10 , A61K47/18 , A61K47/22 , A61K47/545 , A61P35/00 , C07D413/14
Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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公开(公告)号：US20230346753A1
公开(公告)日：2023-11-02
申请号：US18073768
申请日：2022-12-02
Applicant: Valo Health, Inc. , 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 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/4365 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D487/04 , C07D491/048
CPC classification number: A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04
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：US20230330102A1
公开(公告)日：2023-10-19
申请号：US18310913
申请日：2023-05-02
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 , A61K47/68 , A61K47/65 , A61P37/06 , A61P35/00 , 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：US20210244717A1
公开(公告)日：2021-08-12
申请号：US17018196
申请日：2020-09-11
Applicant: Valo Early Discovery, Inc. , 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 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/4365 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/519 , A61K31/5377 , 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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Patent Agency Ranking
公开(公告)号：US20190201544A1
公开(公告)日：2019-07-04
申请号：US16354905
申请日：2019-03-15
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：US20170312252A1
公开(公告)日：2017-11-02
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: A61K31/41 , A61K31/4025 , C07D207/04 , C07D237/04
CPC classification number: A61K31/41 , A61K31/4025 , C07D207/04 , C07D237/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14
Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses, 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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公开(公告)号：US20170002086A1
公开(公告)日：2017-01-05
申请号：US15181618
申请日：2016-06-14
Applicant: Genentech, Inc.
Inventor： Paul Polakis , Peter Dragovich , Thomas Harden Pillow , Shang-Fan Yu
CPC classification number: C07K16/30 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6889 , A61K2039/505 , C07K16/28 , C07K16/2803 , C07K16/3015 , C07K16/3023 , C07K16/3092 , C07K16/32 , C07K16/40 , C07K2317/515
Abstract: The invention provides immunoconjugates and methods of using the same.
Abstract translation: 本发明提供了免疫缀合物及其使用方法。
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公开(公告)号：US11576979B2
公开(公告)日：2023-02-14
申请号：US16689286
申请日：2019-11-20
Applicant: GENENTECH, INC.
Inventor： Peter Dragovich , Zhonghua Pei , Thomas Pillow , Jack Sadowsky , Vishal Verma , Donglu Zhang
IPC: A61K47/68 , A61P35/00 , A61K31/5517
Abstract: The invention relates generally to pyrrolobenzodiazepine monomer and dimer prodrugs having a glutathione-activated disulfide prodrug moiety, a DT-diaphorase-activated quinone prodrug moiety or a reactive oxygen species-activated aryl boronic acid or aryl boronic ester prodrug moiety. The invention further relates to pyrrolobenzodiazepine prodrug dimer-antibody conjugates.
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公开(公告)号：US11547762B2
公开(公告)日：2023-01-10
申请号：US16354905
申请日：2019-03-15
Applicant: Genentech, Inc.
Inventor： Thomas Pillow , Peter Dragovich
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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