公开(公告)号：US10729738B2

公开(公告)日：2020-08-04

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 ,  A61K47/54 ,  A61K47/68 ,  A61K47/64 ,  A61K47/55 ,  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.

公开(公告)号：US20160326142A1

公开(公告)日：2016-11-10

申请号：US15152212

申请日：2016-05-11

Applicant: Genentech, Inc.

Inventor： Jason BURCH ,  Frederick Brookfield ,  Richard A. Goldsmith ,  Kevin Hon Luen Lau ,  Colin H. MacKinnon ,  Daniel Fred Ortwine ,  Zhonghua Pei

IPC: C07D403/12 ,  C07D491/107 ,  C07D401/14 ,  C07D405/14 ,  C07D487/10 ,  C07D413/14 ,  C07D491/044 ,  C07D417/14 ,  C07D495/10 ,  C07D403/14 ,  C07D409/14

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/10 ,  C07D491/044 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10 ,  Y02P20/582

Abstract: Provided herein are compounds of formula (AA): stereoisomers or a pharmaceutically acceptable salt thereof, wherein A, Ra, p, R5 and R6 are defined herein, compositions including the compounds and methods of manufacturing and using the compounds for the treatment of diseases.

Abstract translation: 立体异构体或其药学上可接受的盐，其中A，Ra，p，R 5和R 6在本文中定义，包括化合物的组合物以及制备和使用化合物治疗疾病的方法。

公开(公告)号：US20150158851A1

公开(公告)日：2015-06-11

申请号：US14618827

申请日：2015-02-10

Applicant: Genentech, Inc.

Inventor： Jason Burch ,  Frederick Brookfield ,  Richard A. Goldsmith ,  Kevin Hon Luen Lau ,  Colin H. MacKinnon ,  Daniel Fred Ortwine ,  Zhonghua Pei

IPC: C07D403/12 ,  C07D491/107 ,  C07D401/14 ,  C07D405/14 ,  C07D487/10 ,  C07D413/14 ,  C07D491/044 ,  C07D417/14 ,  C07D495/10 ,  C07D403/14 ,  C07D409/14

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/10 ,  C07D491/044 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10 ,  Y02P20/582

Abstract: Provided herein are compounds of formula (AA): stereoisomers or a pharmaceutically acceptable salt thereof, wherein A, Ra, p, R5 and R6 are defined herein, compositions including the compounds and methods of manufacturing and using the compounds for the treatment of diseases.

Abstract translation: 本文提供了式（AA）的化合物：其立体异构体或其药学上可接受的盐，其中A，Ra，p，R 5和R 6在本文中定义，包括化合物的组合物和制备和使用该化合物治疗疾病的方法。

公开(公告)号：US20140309210A1

公开(公告)日：2014-10-16

申请号：US14178527

申请日：2014-02-12

Applicant: Genentech, Inc.

Inventor： Jason Burch ,  Richard A. Goldsmith ,  Daniel Fred Ortwine ,  Richard Pastor ,  Zhonghua Pei

IPC: C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D491/052 ,  C07D417/14 ,  C07D471/04 ,  C07D409/14 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052

Abstract: A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.

Abstract translation: 式I的化合物：立体异构体或其药学上可接受的盐，其中X，X 1，X 2，X 3，R 1，R 2，R 3，R 4，R 5和R 6在本文中描述，包括化合物的组合物和制备和使用化合物的方法 用于治疗疾病。