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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.
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公开(公告)号:US12090211B2
公开(公告)日:2024-09-17
申请号:US17990988
申请日:2022-11-21
Applicant: Genentech, Inc.
Inventor: Thomas Pillow , Peter Dragovich
CPC classification number: A61K47/6803 , A61K47/65 , A61K47/6889 , C07K16/22 , C07K16/2863
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.
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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.
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公开(公告)号:US20210309660A1
公开(公告)日:2021-10-07
申请号:US16858004
申请日:2020-04-24
Applicant: Genentech, Inc.
Inventor: Nicole Blaquiere , Peter Dragovich , Lewis J. Gazzard , Thomas Pillow , Steven T. Staben , Binqing Wei , Jianfeng Xin
IPC: C07D471/16 , C07D493/10 , C07D403/04 , C07D417/14 , C07D413/14 , A61P35/00
Abstract: The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands.
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公开(公告)号:US20200222545A1
公开(公告)日:2020-07-16
申请号:US16827083
申请日:2020-03-23
Applicant: Genentech, Inc.
Inventor: Thomas Pillow , Andrew G. Polson , Bing Zheng
IPC: A61K47/54 , C07K19/00 , C07D407/12 , A61K45/06 , A61K47/68 , A61K31/357 , G01N33/567
Abstract: The invention relates generally to a silvestrol molecule activated with a leaving group. The invention further relates generally to an antibody-drug conjugate comprising an antibody conjugated by a linker to one or more silvestrol drug moieties and methods of treatment.
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公开(公告)号:US10556895B2
公开(公告)日:2020-02-11
申请号:US15583492
申请日:2017-05-01
Applicant: Genentech, Inc.
Inventor: John A. Flygare , Thomas Pillow , Leanna Staben
IPC: C07D417/14 , C07D403/14 , C07D403/12 , 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.
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公开(公告)号:US10533058B2
公开(公告)日:2020-01-14
申请号:US15104388
申请日:2014-12-16
Applicant: GENENTECH INC. , MEDIMMUNE LIMITED
Inventor: John Flygare , Janet Gunzner-Toste , Thomas Pillow , Brian Safina , Vishal Verma , Binqing Wei , Guiling Zhao , Leanna Staben , Philip Wilson Howard , Luke Masterson
IPC: A61K47/68 , A61K31/5517 , C07K16/30 , C07K16/28
Abstract: This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, pharmaceutical compositions containing them, and to their use in therapy for the prevention treatment of cancer.
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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
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.
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公开(公告)号:US10077318B2
公开(公告)日:2018-09-18
申请号:US14851348
申请日:2015-09-11
Applicant: Genentech, Inc.
Inventor: Sunil Bhakta , Hans Erickson , Jagath R. Junutula , Katherine Kozak , Rachana Ohri , Thomas Pillow
IPC: C07K16/00 , C07K16/32 , C07K16/18 , C07K16/28 , C07K16/30 , A61K51/10 , C07K16/40 , G01N33/58 , A61K47/68 , A61K39/00
CPC classification number: C07K16/32 , A61K47/6803 , A61K47/6809 , A61K47/6817 , A61K47/6849 , A61K47/6869 , A61K51/10 , A61K2039/505 , C07K16/00 , C07K16/18 , C07K16/28 , C07K16/2803 , C07K16/3069 , C07K16/3092 , C07K16/40 , C07K2317/40 , C07K2317/73 , C07K2317/94 , G01N33/582
Abstract: Cysteine engineered antibodies comprising a free cysteine amino acid in the heavy chain or light chain are prepared by mutagenizing a nucleic acid sequence of a parent antibody and replacing one or more amino acid residues by cysteine to encode the cysteine engineered antibody; expressing the cysteine engineered antibody; and isolating the cysteine engineered antibody.
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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.
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