公开(公告)号：US20150224071A1

公开(公告)日：2015-08-13

申请号：US14558440

申请日：2014-12-02

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

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

IPC: A61K31/18 ,  A61K31/397 ,  A61K31/40 ,  A61K31/5375 ,  A61K31/41 ,  A61K31/44 ,  A61K31/4164

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.

Abstract translation: 本发明提供具有以下通式的新化合物及其药学上可接受的盐，其中变量RA，下标n，环A，X2，L，下标m，X1，B，R1，R2，R3，R4，R5和RN具有 本文所述的含义，以及含有这些化合物的组合物和使用这些化合物和组合物的方法。

公开(公告)号：US10711004B2

公开(公告)日：2020-07-14

申请号：US16558718

申请日：2019-09-03

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Brian Safina ,  Daniel Shore ,  Jack Terrett ,  Elisia Villemure ,  Matthew Volgraf ,  Stuart Ward ,  Aijun Lu ,  Robin Larouche-Gauthier ,  Francis Beaumier ,  Martin Dery ,  Lea Constantineau-Forget ,  Chantal Grand-Maitre ,  Luce Lepissier

IPC: C07D473/30 ,  C07D471/04 ,  C07D487/04 ,  C07D473/08

Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US10179767B2

公开(公告)日：2019-01-15

申请号：US15161085

申请日：2016-05-20

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Sultan Chowdhury ,  Christoph Martin Dehnhardt ,  Abid Hasan ,  Ivan William Hemeon ,  Qi Jia ,  Jun Li ,  Zhiguo Liu ,  Daniel F. Ortwine ,  Brian Safina ,  Daniel Sutherlin ,  Shaoyi Sun ,  Andrew D. White ,  Wei Gong ,  Alla Yurevna Zenova ,  Jiuxiang Zhu

IPC: A01N43/00 ,  A61K31/00 ,  C07D211/22 ,  C07D211/48 ,  C07D211/34 ,  C07D405/08 ,  C07D401/12 ,  C07D401/08 ,  C07D211/42 ,  C07D221/20 ,  C07D401/04 ,  C07D211/38 ,  C07D211/62

Abstract: The invention provides compounds having activity as sodium channel (e.g., NaV1.7) inhibitors that are useful for treating sodium channel-mediated diseases or conditions, such as pain, as well as other diseases and conditions associated with the mediation of sodium channels, and compositions containing such compounds and methods for using such compounds and compositions.

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：US20170002017A1

公开(公告)日：2017-01-05

申请号：US15017282

申请日：2016-02-05

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: C07D491/107 ,  C07C311/51 ,  C07D307/12 ,  C07D213/82 ,  C07D205/04 ,  C07D207/48 ,  C07D295/26 ,  C07D257/04 ,  C07D311/58 ,  C07D209/52 ,  C07D307/18 ,  C07D211/22 ,  C07D233/84

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.

Abstract translation: 和其药学上可接受的盐，其中变量RA，下标n，环A，X2，L，下标m，X1，B，R1，R2，R3，R4，R5和RN具有本文所述的含义， 化合物和使用这些化合物和组合物的方法。

公开(公告)号：US20160297754A1

公开(公告)日：2016-10-13

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 Ortwine ,  Brian Safina ,  Shaoyi Sun ,  Daniel P. Sutherlin ,  Alla Yurevna Zenova

IPC: C07C311/51 ,  C07D213/82 ,  C07D213/64 ,  C07D205/04 ,  C07D471/08 ,  C07D405/12 ,  C07D295/26 ,  C07D233/84 ,  C07D257/04 ,  C07D207/46 ,  C07C307/06 ,  C07D311/58

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.

Abstract translation: 和其药学上可接受的盐，其中变量RA，下标n，环A，X2，L，下标m，X1，B，R1，R2，R3，R4，R5和RN具有本文所述的含义， 化合物和使用这些化合物和组合物的方法。

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：US10544215B2

公开(公告)日：2020-01-28

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: A61K47/68 ,  C07K16/28

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：US10125098B2

公开(公告)日：2018-11-13

申请号：US15988956

申请日：2018-05-24

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: C07D207/16 ,  C07D277/06 ,  C07D413/14 ,  C07D413/12 ,  C07D401/10 ,  C07D401/12 ,  C07C235/54 ,  C07D405/10 ,  C07D403/14 ,  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：US10071957B2

公开(公告)日：2018-09-11

申请号：US14413218

申请日：2013-07-05

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Christoph Martin Dehnhardt ,  Sultan Chowdhury ,  Thilo Focken ,  Michael Edward Grimwood ,  Ivan William Hemeon ,  Brian Safina ,  Daniel P. Sutherlin

IPC: C07D205/04 ,  C07D209/08 ,  C07D213/63 ,  C07D213/64 ,  C07D213/69 ,  C07D213/74 ,  C07D215/20 ,  C07D217/02 ,  C07D231/56 ,  C07D277/24 ,  C07D277/34 ,  C07D277/62 ,  C07D305/08 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07C307/06

CPC classification number: C07C307/06 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/444 ,  C07C2601/04 ,  C07D205/04 ,  C07D209/08 ,  C07D213/63 ,  C07D213/64 ,  C07D213/69 ,  C07D213/74 ,  C07D215/20 ,  C07D217/02 ,  C07D231/56 ,  C07D277/24 ,  C07D277/34 ,  C07D277/62 ,  C07D305/08 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

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