公开(公告)号：US10005724B2

公开(公告)日：2018-06-26

申请号：US15321335

申请日：2015-07-07

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Jean-Christophe Andrez ,  Philippe Bergeron ,  Paul Robert Bichler ,  Sultan Chowdhury ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Wei Gong ,  Michael Edward Grimwood ,  Abid Hasan ,  Ivan William Hemeon ,  Qi Jia ,  Brian Safina ,  Shaoyi Sun ,  Michael Scott Wilson ,  Alla Yurevna Zenova

IPC: C07C235/54 ,  C07D207/16 ,  C07D405/10 ,  C07D401/12 ,  C07D471/08 ,  C07D403/14 ,  C07D401/10 ,  C07D413/12 ,  C07D413/14 ,  C07D277/06

CPC classification number: C07D207/16 ,  C07C235/42 ,  C07C235/52 ,  C07C235/54 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2603/74 ,  C07D205/04 ,  C07D207/08 ,  C07D207/10 ,  C07D207/22 ,  C07D209/02 ,  C07D209/52 ,  C07D209/54 ,  C07D211/20 ,  C07D211/38 ,  C07D211/60 ,  C07D213/69 ,  C07D221/22 ,  C07D231/06 ,  C07D263/04 ,  C07D263/26 ,  C07D265/30 ,  C07D277/06 ,  C07D305/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/10 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D451/02 ,  C07D471/08

Abstract: The invention provides compounds having the general Formula (I); and pharmaceutically acceptable salts thereof; wherein the variables RA, RAA, subscript n, subscript q, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US20160354485A1

公开(公告)日：2016-12-08

申请号：US15182444

申请日：2016-06-14

Applicant: Genentech, Inc.

Inventor： John A. Flygare ,  Thomas H. 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 ,  C07K16/28

CPC classification number: C07K16/28 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6869 ,  C07D209/60 ,  C07D403/14 ,  C07D487/04 ,  C07F9/65583 ,  C07F9/6561 ,  C07K2317/56

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.

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：US08952169B2

公开(公告)日：2015-02-10

申请号：US13899526

申请日：2013-05-21

Applicant: Genentech, Inc. ,  Xenon Pharmaceuticals Inc.

Inventor： Jean-Christophe Andrez ,  Sultan Chowdhury ,  Shannon Marie Decker ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Ivan William Hemeon ,  Qi Jia ,  Jun Li ,  Daniel F. Ortwine ,  Brian Safina ,  Tao Sheng ,  Shaoyi Sun ,  Daniel P. Sutherlin ,  Michael Scott Wilson ,  Alla Yurevna Zenova

IPC: C07C311/51 ,  C07D403/12 ,  C07D213/82 ,  C07D213/64 ,  C07D205/04 ,  C07D311/58 ,  A61K31/445 ,  A61K31/44 ,  A61K31/18 ,  C07D265/30 ,  C07D233/84 ,  C07D257/04 ,  C07C307/06 ,  C07D295/26 ,  C07D207/48 ,  C07D311/70 ,  C07D413/12 ,  C07D451/02 ,  C07D307/12 ,  C07D309/08 ,  C07D311/72 ,  C07D405/12 ,  C07D491/107 ,  C07D211/22 ,  C07D295/192 ,  C07D211/96 ,  C07D307/18

CPC classification number: C07D491/107 ,  A61K31/18 ,  A61K31/397 ,  A61K31/40 ,  A61K31/41 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/5375 ,  C07B2200/05 ,  C07C307/06 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/10 ,  C07C2602/18 ,  C07C2602/20 ,  C07C2602/42 ,  C07C2602/44 ,  C07C2602/50 ,  C07C2603/66 ,  C07C2603/68 ,  C07C2603/74 ,  C07D205/04 ,  C07D207/46 ,  C07D207/48 ,  C07D209/52 ,  C07D211/22 ,  C07D211/96 ,  C07D213/64 ,  C07D213/82 ,  C07D233/84 ,  C07D257/04 ,  C07D265/30 ,  C07D295/192 ,  C07D295/26 ,  C07D307/12 ,  C07D307/18 ,  C07D309/08 ,  C07D311/58 ,  C07D311/70 ,  C07D311/72 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D451/02 ,  C07D471/08

Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US11692043B2

公开(公告)日：2023-07-04

申请号：US16696455

申请日：2019-11-26

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: C07K16/30 ,  A61K47/68 ,  A61K31/5517 ,  C07K16/28

CPC classification number: C07K16/3092 ,  A61K31/5517 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6867 ,  A61K47/6869 ,  A61K47/6889 ,  C07K16/2851 ,  C07K16/30 ,  C07K16/3061 ,  C07K16/3069 ,  C07K2317/24 ,  C07K2317/51 ,  C07K2317/515 ,  C07K2317/56

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.

公开(公告)号：US10787446B2

公开(公告)日：2020-09-29

申请号：US15939112

申请日：2018-03-28

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Philippe Bergeron ,  Kristen Burford ,  Sultan Chowdhury ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Abid Hasan ,  Kwong Wah Lai ,  Zhiguo Liu ,  Steven McKerrall ,  Teresa Phuongtram Nguyen ,  Brian Safina ,  Daniel Sutherlin ,  Tao Wang

IPC: C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  A61P17/04 ,  C07D401/12 ,  C07D491/107

Abstract: The invention provides a compound of formula: or a salt thereof, wherein the variables RAA, n, ring A, ring B, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, and R9 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US10442836B2

公开(公告)日：2019-10-15

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: A61K47/68 ,  C07K16/28 ,  C07D207/40 ,  C07D209/60 ,  C07K5/062 ,  C07D487/04 ,  C07D209/62 ,  C07D401/14 ,  C07D403/14 ,  C07F9/6558 ,  C07H15/24 ,  C07K16/32 ,  C07D401/12 ,  C07D471/04 ,  C07K16/00 ,  C07K16/30 ,  A61K47/55 ,  C07F9/572 ,  C07F9/6561

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.

公开(公告)号：US09771376B2

公开(公告)日：2017-09-26

申请号：US15133030

申请日：2016-04-19

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Sultan Chowdhury ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Ivan William Hemeon ,  Qi Jia ,  Daniel F. Ortwine ,  Brian Safina ,  Shaoyi Sun ,  Daniel P. Sutherlin ,  Alla Yurevna Zenova

IPC: C07D257/04 ,  C07D471/08 ,  C07D207/46 ,  C07D213/64 ,  C07C311/51 ,  C07D233/84 ,  C07D205/04 ,  C07D491/107 ,  C07D403/12 ,  C07D213/82 ,  C07D311/58 ,  C07D265/30 ,  C07C307/06 ,  C07D295/26 ,  C07D207/48 ,  C07D311/70 ,  C07D413/12 ,  C07D451/02 ,  C07D307/12 ,  C07D309/08 ,  C07D311/72 ,  C07D405/12 ,  C07D211/22 ,  C07D295/192 ,  C07D211/96 ,  C07D307/18 ,  A61K31/18 ,  A61K31/397 ,  A61K31/40 ,  A61K31/41 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/5375 ,  C07D209/52

CPC classification number: C07D491/107 ,  A61K31/18 ,  A61K31/397 ,  A61K31/40 ,  A61K31/41 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/5375 ,  C07B2200/05 ,  C07C307/06 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/10 ,  C07C2602/18 ,  C07C2602/20 ,  C07C2602/42 ,  C07C2602/44 ,  C07C2602/50 ,  C07C2603/66 ,  C07C2603/68 ,  C07C2603/74 ,  C07D205/04 ,  C07D207/46 ,  C07D207/48 ,  C07D209/52 ,  C07D211/22 ,  C07D211/96 ,  C07D213/64 ,  C07D213/82 ,  C07D233/84 ,  C07D257/04 ,  C07D265/30 ,  C07D295/192 ,  C07D295/26 ,  C07D307/12 ,  C07D307/18 ,  C07D309/08 ,  C07D311/58 ,  C07D311/70 ,  C07D311/72 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D451/02 ,  C07D471/08

Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US09694002B2

公开(公告)日：2017-07-04

申请号：US15275131

申请日：2016-09-23

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Jean-Christophe Andrez ,  Paul Robert Bichler ,  Chien-An Chen ,  Sultan Chowdhury ,  Shannon Marie Decker ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Ivan William Hemeon ,  Qi Jia ,  Jun Li ,  Zhiguo Liu ,  Daniel F. Ortwine ,  Brian Safina ,  Daniel Sutherlin ,  Tao Sheng ,  Shaoyi Sun ,  Andrew D. White ,  Michael Scott Wilson ,  Alla Yurevna Zenova ,  Jiuxiang Zhu

IPC: C07D211/32 ,  C07D211/54 ,  C07D233/68 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/4523

CPC classification number: A61K31/445 ,  A61K31/337 ,  A61K31/397 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4412 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/495 ,  C07D205/04 ,  C07D207/12 ,  C07D211/22 ,  C07D211/32 ,  C07D211/42 ,  C07D211/54 ,  C07D211/60 ,  C07D233/68 ,  C07D237/08 ,  C07D241/04 ,  C07D265/30 ,  C07D305/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D453/02 ,  C07D487/08 ,  C07F7/0812

Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US20160279260A1

公开(公告)日：2016-09-29

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: A61K47/48 ,  C07K16/30 ,  C07K16/28

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.

Abstract translation: 本发明涉及肽模拟接头及其抗体药物偶联物，含有它们的药物组合物及其在治疗中用于预防或治疗癌症的用途。