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：US20170107243A1

公开(公告)日：2017-04-20

申请号：US15297384

申请日：2016-10-19

Applicant: Genentech, Inc.

Inventor： Thomas Pillow

IPC: C07H15/207 ,  A61K39/395 ,  A61K47/48

CPC classification number: C07H15/207 ,  A61K39/39558 ,  A61K47/545 ,  A61K47/6807 ,  A61K47/6809

Abstract: The invention relates generally to a calicheamicin molecule activated with a leaving group. The invention further relates generally to an antibody-drug conjugate comprising an antibody directly conjugated by a disulfide to one or more calicheamicin molecules.

公开(公告)号：US20150165063A1

公开(公告)日：2015-06-18

申请号：US14305643

申请日：2014-06-16

Applicant: Genentech, Inc.

Inventor： John Flygare ,  Thomas Pillow ,  Brian Safina ,  Vishal Verma ,  Binqing Wei ,  William Denny ,  Anna Giddens ,  Ho Lee ,  Guo-Liang Lu ,  Christian Miller ,  Gordon Rewcastle ,  Moana Tercel ,  Muriel Bonnet

IPC: A61K47/48 ,  C07K16/18 ,  C07K16/32 ,  C07D401/14 ,  C07K5/062 ,  C07F9/6558 ,  C07D403/14 ,  C07H15/24 ,  C07K16/28 ,  C07D209/62

Abstract: The invention provides antibody-drug conjugates comprising an antibody conjugated to a 1-(chloromethyl)-2,3-dihydro-1H-benzo[e]indole (CBI) dimer drug moiety via a linker, and methods of using the antibody-drug conjugates.

Abstract translation: 本发明提供包含通过接头与1-（氯甲基）-2,3-二氢-1H-苯并[e]吲哚（CBI）二烯体（CBI）二聚体药物部分缀合的抗体的抗体 - 药物偶联物，以及使用抗体药物 共轭物

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.

公开(公告)号：US20230233700A1

公开(公告)日：2023-07-27

申请号：US17990988

申请日：2022-11-21

Applicant: Genentech, Inc.

Inventor： Thomas Pillow ,  Peter Dragovich

IPC: A61K47/68 ,  C07K16/28 ,  C07K16/22 ,  A61K47/65

CPC classification number: A61K47/6803 ,  C07K16/2863 ,  C07K16/22 ,  A61K47/65 ,  A61K47/6889

Abstract: The subject matter described herein is directed to methods of preparing certain antibody-drug conjugates (ADCs) wherein the antibody is linked to the drug through a linker, wherein the drug contains a heteroaryl group having a secondary nitrogen, and the linker is attached to the drug via the secondary nitrogen. The resulting conjugates are useful in treating various diseases and conditions.

公开(公告)号：US10730900B2

公开(公告)日：2020-08-04

申请号：US16444326

申请日：2019-06-18

Applicant: Genentech, Inc.

Inventor： Thomas Pillow

IPC: C07H15/207 ,  A61K39/44 ,  A61K47/54 ,  A61K47/68 ,  A61K39/395

Abstract: The invention relates generally to a calicheamicin molecule activated with a leaving group. The invention further relates generally to an antibody-drug conjugate comprising an antibody directly conjugated by a disulfide to one or more calicheamicin molecules.

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：US20200087297A1

公开(公告)日：2020-03-19

申请号：US16697706

申请日：2019-11-27

Applicant: Genentech, Inc.

Inventor： John A. Flygare ,  Thomas Pillow ,  Leanna Staben

IPC: C07D417/14 ,  C07D471/02 ,  C07D403/12 ,  C07D403/14

Abstract: This invention relates to quaternary amine linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.

公开(公告)号：US20180125995A1

公开(公告)日：2018-05-10

申请号：US15612193

申请日：2017-06-02

Applicant: Genentech, Inc.

Inventor： Eric Brown ,  Wouter Hazenbos ,  Isidro Hotzel ,  Kimberly Kajihara ,  Sophie M. Lehar ,  Sanjeev Mariathasan ,  Thomas Pillow ,  Leanna Staben ,  Vishal Verma ,  Binqing Wei ,  Yi Xia ,  Min Xu

IPC: A61K47/68 ,  C07K16/12 ,  A61K31/5383 ,  A61K45/06 ,  A61P31/04

CPC classification number: A61K47/6803 ,  A61K31/5383 ,  A61K45/06 ,  A61K47/6835 ,  A61K47/6889 ,  A61P31/04 ,  C07K16/1271 ,  C07K2317/21

Abstract: The invention provides rF1 antibody antibiotic conjugates and methods of using same.

公开(公告)号：US20180021450A1

公开(公告)日：2018-01-25

申请号：US15611985

申请日：2017-06-02

Applicant: Genentech, Inc.

Inventor： Eric Brown ,  Wouter Hazenbos ,  Isidro Hotzel ,  Kimberly Kajihara ,  Sophie M. Lehar ,  Sanjeev Mariathasan ,  Thomas Pillow ,  Leanna Staben ,  Vishal Verma ,  Binqing Wei ,  Min Xu

IPC: A61K47/68 ,  A61K31/4468 ,  A61K39/40 ,  A61K31/496

CPC classification number: A61K47/6809 ,  A61K31/4468 ,  A61K31/496 ,  A61K39/40 ,  A61K47/6803 ,  A61K47/6835 ,  A61K47/6889

Abstract: The invention provides anti-Staphylococcus aureus antibody rifamycin antibiotic conjugates and methods of using same.