公开(公告)号：US20240076295A1

公开(公告)日：2024-03-07

申请号：US18108045

申请日：2023-02-10

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Andrew P. Crew ,  Jing Wang ,  Michael Berlin ,  Peter Dragovich ,  Huifen Chen ,  Leanna Staben

IPC: C07D417/14 ,  A61K47/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/54 ,  A61P35/00 ,  C07D413/14

CPC classification number: C07D417/14 ,  A61K47/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/545 ,  A61P35/00 ,  C07D413/14

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

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：US20160279261A1

公开(公告)日：2016-09-29

申请号：US15182429

申请日：2016-06-14

Applicant: Ho Huat Lee ,  Moana Tercel ,  Genentech, Inc.

Inventor： Ho Huat Lee ,  Moana Tercel ,  John A. Flygare ,  Janet Gunzner-Toste ,  Thomas H. Pillow ,  Brian Safina ,  Leanna Staben ,  Vishal Verma ,  BinQing Wei ,  Guiling Zhao

IPC: A61K47/48 ,  C07K16/30 ,  C07K16/28

CPC classification number: C07K16/30 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6889 ,  A61K2039/505 ,  C07K16/28 ,  C07K16/2851 ,  C07K16/2863 ,  C07K2317/24 ,  C07K2317/56 ,  C07K2317/76

Abstract: This invention relates to peptidomimetic 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：US11104673B2

公开(公告)日：2021-08-31

申请号：US16697706

申请日：2019-11-27

Applicant: Genentech, Inc.

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

IPC: A61K39/00 ,  C07D417/14 ,  C07D403/14 ,  C07D403/12 ,  C07D471/02 ,  A61K47/68

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：US09999681B2

公开(公告)日：2018-06-19

申请号：US15181825

申请日：2016-06-14

Applicant: Genentech, Inc.

Inventor： John Flygare ,  Janet Gunzner-Toste ,  Thomas Pillow ,  Brian Safina ,  Vishal Verma ,  Binqing Wei ,  Guiling Zhao ,  Leanna Staben

IPC: C07K16/30 ,  C07K16/28 ,  A61K47/48 ,  A61K47/68

CPC classification number: A61K47/6803 ,  A61K47/6809 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/28 ,  C07K16/2851 ,  C07K16/30 ,  C07K2317/24 ,  C07K2317/56 ,  C07K2317/76

Abstract: This invention relates to peptidomimetic 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：US20180016325A1

公开(公告)日：2018-01-18

申请号：US15718876

申请日：2017-09-28

Applicant: Genentech, Inc.

Inventor： Eric J. Brown ,  Martine Darwish ,  John Flygare ,  Wouter Hazenbos ,  Byoung Chul Lee ,  Sophie M. Lehar ,  Sanjeev Mariathasan ,  John Hiroshi Morisaki ,  Thomas H. Pillow ,  Leanna Staben ,  Richard Vandlen ,  Klaus Koefoed ,  Magnus Strandh ,  Peter S. Andersen

IPC: C07K16/12 ,  A61K45/06 ,  A61K39/40 ,  A61K31/4025 ,  A61K31/5386

CPC classification number: C07K16/1271 ,  A61K31/4025 ,  A61K31/5386 ,  A61K39/40 ,  A61K45/06 ,  A61K47/6809 ,  A61K47/6835 ,  C07K2317/21 ,  C07K2317/522 ,  C07K2317/55 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/624 ,  C07K2317/92

Abstract: The invention provides anti-wall teichoic acid antibodies and antibiotic conjugates thereof, and methods of using the same.

公开(公告)号：US20170232113A1

公开(公告)日：2017-08-17

申请号：US15583492

申请日：2017-05-01

Applicant: Genentech, Inc.

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

IPC: A61K47/48 ,  C07K19/00

CPC classification number: C07D417/14 ,  A61K47/6803 ,  A61K47/6805 ,  A61K47/6851 ,  A61K47/6889 ,  C07D403/12 ,  C07D403/14 ,  C07D471/02

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：US20160074529A1

公开(公告)日：2016-03-17

申请号：US14945716

申请日：2015-11-19

Applicant: GENENTECH, INC.

Inventor： Eric J. Brown ,  John Flygare ,  Wouter Hazenbos ,  Sophie M. Lehar ,  Sanjeev Mariathasan ,  John Hiroshi Morisaki ,  Thomas H. Pillow ,  Leanna Staben ,  Richard Vandlen ,  Klaus Koefoed ,  Magnus Strandh ,  Peter S. Andersen

IPC: A61K47/48 ,  A61K31/7048 ,  A61K31/4709 ,  A61K38/12 ,  A61K31/4375 ,  A61K31/4436 ,  A61K31/7056 ,  A61K31/439

CPC classification number: A61K47/6849 ,  A61K31/395 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4436 ,  A61K31/4709 ,  A61K31/7048 ,  A61K31/7056 ,  A61K38/12 ,  A61K47/6801 ,  A61K47/6803 ,  A61K47/6809 ,  A61K47/6835 ,  A61K47/6851 ,  C07K16/1271 ,  C07K2317/21 ,  C07K2317/522 ,  C07K2317/55 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/624 ,  C07K2317/92

Abstract: The invention provides anti-wall teichoic acid antibodies and antibiotic conjugates thereof, and methods of using the same.

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：US20200038378A1

公开(公告)日：2020-02-06

申请号：US16590329

申请日：2019-10-01

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： ANDREW P. CREW ,  Jing Wang ,  Michael Berlin ,  Peter Dragovich ,  Huifen Chen ,  Leanna Staben

IPC: A61K31/427 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/437 ,  A61K31/4245 ,  A61K31/541 ,  A61K31/496 ,  A61K47/54

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.