公开(公告)号：US20190241558A1

公开(公告)日：2019-08-08

申请号：US16198581

申请日：2018-11-21

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： Patrick Cyr ,  Sarah Bronner ,  F. Anthony Romero ,  Steven Magnuson ,  Vickie Hsiao-Wei Tsui ,  Jeremy M. Murray ,  John Wai ,  Kwong Wah Lai ,  Fei Wang ,  Kevin X. Chen

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to a compound formula (I): and to salts thereof, wherein R1, R2 X, and Y have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

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.