公开(公告)号：US20180230079A1

公开(公告)日：2018-08-16

申请号：US15896970

申请日：2018-02-14

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Ivan William HEMEON ,  Brian SAFINA ,  Daniel SUTHERLIN

IPC: C07C62/38 ,  C07C62/34 ,  C07D211/22 ,  C07C323/61 ,  C07C317/44 ,  C07C313/04 ,  C07C229/48 ,  A61P17/04 ,  A61P25/00 ,  A61P29/00

CPC classification number: C07C62/38 ,  A61P17/04 ,  A61P25/00 ,  A61P29/00 ,  C07C62/34 ,  C07C69/757 ,  C07C229/48 ,  C07C313/04 ,  C07C317/44 ,  C07C323/61 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/74 ,  C07D211/22

Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RAA, n, ring A, X1, L, m, X2, R2, R3, R4, R5, X, and R6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US20160009710A1

公开(公告)日：2016-01-14

申请号：US14772735

申请日：2014-03-14

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Paul Robert BICHLER ,  Sultan CHOWDHURY ,  Shannon Marie DECKER ,  Christopher Martin DEHNHARDT ,  Thilo FOCKEN ,  Michael Edward GRIMWOOD ,  Ivan William HEMEON ,  Brian SAFINA ,  Tao SHENG ,  Shaoyi SUN ,  Michael Scott WILSON ,  Alla Yurevna ZENOVA

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D471/08 ,  C07D519/00

Abstract: The invention provides compounds having the general formula: [insert formula (I)] (I) and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, 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化合物：[插入式（I）]（I）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，R1，R2，R3 ，R4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：US20180265465A1

公开(公告)日：2018-09-20

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 ,  C07D471/08 ,  C07D401/12 ,  C07C235/54 ,  C07D405/10 ,  C07D403/14

CPC classification number: C07D207/16 ,  C07C235/42 ,  C07C235/52 ,  C07C235/54 ,  C07C2103/74 ,  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：US20200157240A1

公开(公告)日：2020-05-21

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

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：US20200002340A1

公开(公告)日：2020-01-02

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：US20180291014A1

公开(公告)日：2018-10-11

申请号：US15939112

申请日：2018-03-28

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

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

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：US20160340309A1

公开(公告)日：2016-11-24

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: C07D211/22 ,  C07D211/34 ,  C07D405/08 ,  C07D401/04 ,  C07D401/08 ,  C07D211/42 ,  C07D221/20 ,  C07D211/48 ,  C07D401/12

CPC classification number: C07D211/22 ,  C07D211/34 ,  C07D211/38 ,  C07D211/42 ,  C07D211/48 ,  C07D211/62 ,  C07D221/20 ,  C07D401/04 ,  C07D401/08 ,  C07D401/12 ,  C07D405/08

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.

Abstract translation: 本发明提供了具有钠通道活性的化合物（例如，NaV1.7）抑制剂，其可用于治疗钠通道介导的疾病或病症，例如疼痛，以及与钠通道调停相关的其它疾病和病症，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：US20150322002A1

公开(公告)日：2015-11-12

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: C07C307/06 ,  C07D205/04 ,  C07D217/02 ,  C07D413/12 ,  C07D277/24 ,  C07D209/08 ,  C07D213/69 ,  C07D401/12

CPC classification number: C07C307/06 ,  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.

Abstract translation: 本发明提供具有通式（I）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，环D，R1和RN具有如上所述的含义 和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：US20220055977A1

公开(公告)日：2022-02-24

申请号：US17396283

申请日：2021-08-06

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Ivan William HEMEON ,  Brian SAFINA ,  Daniel SUTHERLIN

IPC: C07C62/38 ,  C07C62/34 ,  C07C229/48 ,  C07D211/22 ,  C07C317/44 ,  C07C323/61 ,  C07C69/757 ,  A61P25/00 ,  A61P29/00 ,  A61P17/04 ,  C07C313/04

Abstract: The invention provides a method of treating a disease or condition in a mammal by administering a compound having the general formula I: or a pharmaceutically acceptable salt thereof, wherein the variables RAA, n, ring A, X1, L, m, X2, R2, R3, R4, R5, X, and R6 have the meaning as described herein.

公开(公告)号：US20210253548A1

公开(公告)日：2021-08-19

申请号：US17152185

申请日：2021-01-19

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Chien-an CHEN ,  Sultan CHOWDHURY ,  Shannon Marie DECKER ,  Christoph Martin DEHNHARDT ,  Ivan William HEMEON ,  Steven MCKERRALL ,  Brian SAFINA ,  Tao SHENG ,  Dan SUTHERLIN

IPC: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D231/56 ,  C07D403/04 ,  C07D405/04 ,  C07D403/06 ,  C07D403/12 ,  A61P29/00

Abstract: The invention provides compounds having the general formula (I): and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, n, ring A, X2, L, m, 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.