公开(公告)号：US11547701B2

公开(公告)日：2023-01-10

申请号：US17018196

申请日：2020-09-11

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: C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/4355 ,  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:

公开(公告)号：US11242344B2

公开(公告)日：2022-02-08

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 ,  A61P35/00 ,  C07D417/14 ,  C07D413/14 ,  C07D403/04

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.

公开(公告)号：US20210171545A1

公开(公告)日：2021-06-10

申请号：US16944581

申请日：2020-07-31

Applicant: Integral Early Discovery, 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.

公开(公告)号：US10696692B2

公开(公告)日：2020-06-30

申请号：US14382141

申请日：2013-03-01

Applicant: Forma TM, LLC ,  Genentech, Inc.

Inventor： Kenneth W Bair ,  Timm R Baumeister ,  Alexandre J Buckmelter ,  Karl H Clodfelter ,  Peter Dragovich ,  Francis Gosselin ,  Janet Gunzner-Toste ,  Bingsong Han ,  Jian Lin ,  Xiongcai Liu ,  Dominic J Reynolds ,  Chase C Smith ,  Zhongguo Wang ,  Mark Zak ,  Yamin Zhang ,  Guiling Zhao ,  Xiaozhang Zheng ,  Po-Wai Yuen

IPC: A61K51/00 ,  A61M36/14 ,  C07D519/00 ,  C07D471/04 ,  C07D495/04 ,  C07D487/04 ,  C07D491/048 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/551 ,  A61K45/06

Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

公开(公告)号：US10532108B2

公开(公告)日：2020-01-14

申请号：US16271549

申请日：2019-02-08

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.

公开(公告)号：US10456382B2

公开(公告)日：2019-10-29

申请号：US16212360

申请日：2018-12-06

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: C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  A61K31/4355 ,  A61K31/496 ,  A61K31/437 ,  C07D491/04 ,  C07D495/04 ,  A61K31/4365 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06

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:

公开(公告)号：US20190300521A1

公开(公告)日：2019-10-03

申请号：US16372345

申请日：2019-04-01

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

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.

公开(公告)号：US20180339998A1

公开(公告)日：2018-11-29

申请号：US15936086

申请日：2018-03-26

Applicant: Forma TM, LLC ,  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 ,  A61K45/06 ,  C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/496 ,  A61K31/497 ,  A61K31/513 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/438 ,  C07D495/04 ,  C07D491/048 ,  C07D487/04 ,  A61K31/501

Abstract: Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

公开(公告)号：US10058613B2

公开(公告)日：2018-08-28

申请号：US15281830

申请日：2016-09-30

Applicant: Genentech, Inc.

Inventor： Peter Dragovich ,  Thomas Pillow ,  Jack Sadowsky ,  Mark X. Sliwkowski ,  BinQing Wei

IPC: C07K16/00 ,  A61K45/06 ,  C07K16/28 ,  C07D519/00 ,  C07K16/32 ,  A61K31/5517 ,  A61K47/68

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.

公开(公告)号：US12152040B2

公开(公告)日：2024-11-26

申请号：US17198240

申请日：2021-03-10

Applicant: Genentech, Inc.

Inventor： Robert Anthony Blake ,  Peter Dragovich ,  Lewis J. Gazzard ,  Susan Kaufman ,  Tracy Kleinheinz ,  Thomas Pillow ,  Steven T. Staben ,  Binqing Wei

IPC: C07D495/14 ,  A61P35/00 ,  C07D495/16

Abstract: The present disclosure relates to compounds and salts thereof that are useful for inhibiting target polypeptides and proteins, in particular, bromodomain (e.g., BRD4) proteins. Also disclosed are pharmaceutical compositions comprising the compounds, or a salt (e.g., a pharmaceutically acceptable salt) thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated diseases or disorders.