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.

公开(公告)号：US20180326062A1

公开(公告)日：2018-11-15

申请号：US16036575

申请日：2018-07-16

Applicant: Genentech, Inc.

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

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

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：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.

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：US20170095570A1

公开(公告)日：2017-04-06

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: A61K47/48 ,  A61K45/06 ,  C07K16/32 ,  A61K31/5517

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：US11666581B2

公开(公告)日：2023-06-06

申请号：US16194897

申请日：2018-11-19

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 ,  A61K47/65 ,  A61K47/68 ,  A61P35/00 ,  A61P37/06 ,  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.

公开(公告)号：US20190175612A1

公开(公告)日：2019-06-13

申请号：US16194897

申请日：2018-11-19

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 ,  A61P35/00 ,  A61P37/06 ,  A61K47/65 ,  C12N9/00 ,  C07K16/32 ,  C07K16/28

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.

公开(公告)号：US20180185486A1

公开(公告)日：2018-07-05

申请号：US15899612

申请日：2018-02-20

Applicant: Genentech, Inc.

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

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

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：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.

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.