公开(公告)号：US20250084096A1

公开(公告)日：2025-03-13

申请号：US18913161

申请日：2024-10-11

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.

公开(公告)号：US20200085965A1

公开(公告)日：2020-03-19

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 ,  A61K31/5517 ,  A61P35/00

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：US20230067037A1

公开(公告)日：2023-03-02

申请号：US17239086

申请日：2021-04-23

Applicant: Genentech, Inc.

Inventor： Peter DRAGOVICH ,  Thomas PILLOW ,  Robert Anthony BLAKE ,  Ingrid WERTZ

IPC: A61K47/68 ,  A61K31/427 ,  A61K31/5517 ,  A61K31/661

Abstract: The subject matter described herein is directed to antibody-CIDE conjugates (Ab-CIDEs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.

公开(公告)号：US20210221821A1

公开(公告)日：2021-07-22

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 ,  C07D495/16 ,  A61P35/00

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.

公开(公告)号：US20190175749A1

公开(公告)日：2019-06-13

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：US20170368039A1

公开(公告)日：2017-12-28

申请号：US15352184

申请日：2016-11-15

Applicant: Forma TM, LLC ,  Genentech, Inc.

Inventor： BAIR W. Kenneth ,  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 ,  C07D491/04 ,  C07D487/04 ,  C07D471/04 ,  A61K31/55 ,  A61K31/4365 ,  A61K31/5377 ,  A61K31/519 ,  A61K31/497 ,  A61K31/496 ,  A61K31/437 ,  C07D495/04 ,  A61K45/06

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:

公开(公告)号：US20170001990A1

公开(公告)日：2017-01-05

申请号：US15266222

申请日：2016-09-15

Applicant: Genentech, Inc.

Inventor： Jinhua CHEN ,  Charles Z. DING ,  Peter DRAGOVICH ,  Benjamin FAUBER ,  Zhenting GAO ,  Sharada S. LABADIE ,  Kwong Wah LAI ,  Hans Edward PURKEY ,  Kirk ROBARGE ,  Binqing WEI ,  Aihe ZHOU

IPC: C07D409/14 ,  C07D401/04 ,  C07D417/04 ,  C07D491/107 ,  C07D211/86 ,  C07D417/14 ,  C07D491/048 ,  C07D405/14 ,  C07D491/08 ,  C07D498/08 ,  C07D409/04 ,  C07D413/14

CPC classification number: C07D409/14 ,  C07D211/86 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D487/08 ,  C07D491/048 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

Abstract: The invention provides novel compounds having the general formula: and tautomers and pharmaceutically acceptable salts thereof, wherein A1, A2, A3, A4, R1, R4, R5, R6, R7 and R8 are as defined herein, compositions including the compounds and methods of using the compounds.

Abstract translation: 本发明提供具有通式（I）的新化合物及其互变异构体及其药学上可接受的盐，其中A1，A2，A3，A4，R1，R4，R5，R6，R7和R8如本文所定义，包括化合物和 使用化合物的方法。

公开(公告)号：US20160002266A1

公开(公告)日：2016-01-07

申请号：US14382210

申请日：2013-03-01

Applicant: GENENTECH, INC. ,  FORMA TM, LLC

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 ,  A61K31/438 ,  C07D495/04 ,  C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  C07D471/04 ,  C07D491/048

CPC classification number: C07D519/00 ,  A61K31/438 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04

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

Abstract translation: 提供酰氨基螺环酰胺和磺酰胺化合物，包含这些化合物的药物组合物，以及使用这些化合物的治疗方法。