公开(公告)号：US12054486B2

公开(公告)日：2024-08-06

申请号：US17951640

申请日：2022-09-23

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Verner Alexander Lofstrand ,  Jung Yun Kim ,  Helen Clement ,  Kristen Nicole Burford ,  Paul Charifson ,  Shawn Johnstone ,  Juliette Sabbatani ,  Jan Felix Scholtes ,  Wei Zhang ,  Shaoyi Sun

IPC: C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/052

CPC classification number: C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/052

Abstract: The present disclosure is directed to compounds of formula (1):






wherein X, Y, R1, R2 and R3 are as described herein, as stereoisomers, enantiomers or tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, and pharmaceutical compositions comprising the compounds of formula (I), as described herein, which are useful as voltage-gated sodium channel modulators and are therefore are useful in treating seizure disorders such as epilepsy.

公开(公告)号：US20200157089A1

公开(公告)日：2020-05-21

申请号：US16556055

申请日：2019-08-29

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Jean-Christophe Andrez ,  Kristen Nicole Burford ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Qi Jia ,  Verner Alexander Lofstrand ,  Shaoyi Sun ,  Steven Sigmund Wesolowski ,  Michael Scott Wilson ,  Alla Yurevna Zenova

IPC: C07D417/14 ,  C07D417/12 ,  C07D401/14 ,  C07D401/12 ,  C07D409/12 ,  C07D487/08 ,  C07D471/04 ,  C07D413/12

Abstract: This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy and/or epileptic seizure disorders.

公开(公告)号：US09546164B2

公开(公告)日：2017-01-17

申请号：US14603273

申请日：2015-01-22

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 ,  C07D453/02 ,  A61K31/337 ,  A61K31/397 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4412 ,  A61K31/495 ,  C07D237/08 ,  C07D241/04 ,  C07D205/04 ,  C07D207/12 ,  C07D211/42 ,  C07D305/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D403/04 ,  C07D487/08 ,  C07D265/30 ,  C07D211/60

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.

Abstract translation: 本发明提供具有通式I的化合物及其药学上可接受的盐，其中变量RA，RAA，下标n，环A，X2，L，下标m，X1，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：US09487535B2

公开(公告)日：2016-11-08

申请号：US13794147

申请日：2013-03-11

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Shaoyi Sun ,  Jianmin Fu ,  Sultan Chowdhury ,  Ivan William Hemeon ,  Michael Edward Grimwood ,  Tarek Suhayl Mansour

IPC: C07D491/20 ,  C07D209/34 ,  C07D405/10 ,  C07D491/107

CPC classification number: C07D491/20 ,  C07D209/34 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D491/107

Abstract: This invention is directed to asymmetric syntheses of certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract translation: 本发明涉及某些螺 - 羟吲哚衍生物的不对称合成，其可用于治疗和/或预防钠通道介导的疾病或病症如疼痛。

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：US11639351B2

公开(公告)日：2023-05-02

申请号：US17183401

申请日：2021-02-24

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Jean-Christophe Andrez ,  Kristen Nicole Burford ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Qi Jia ,  Verner Alexander Lofstrand ,  Shaoyi Sun ,  Steven Sigmund Wesolowski ,  Michael Scott Wilson ,  Alla Yurevna Zenova

IPC: A61K31/4436 ,  A61K31/444 ,  C07D417/14 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/08

Abstract: This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy and/or epileptic seizure disorders.

公开(公告)号：US20170066777A1

公开(公告)日：2017-03-09

申请号：US15265549

申请日：2016-09-14

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Shaoyi Sun ,  Jianmin Fu ,  Sultan Chowdhury ,  Ivan William Hemeon ,  Michael Edward Grimwood ,  Tarek Suhayl Mansour

IPC: C07D491/20 ,  C07D405/14 ,  C07D405/04 ,  C07D405/06

CPC classification number: C07D491/20 ,  C07D209/34 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D491/107

Abstract: This invention is directed to asymmetric syntheses of certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract translation: 本发明涉及某些螺 - 羟吲哚衍生物的不对称合成，其可用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。

公开(公告)号：US09550775B2

公开(公告)日：2017-01-24

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 ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Ivan William Hemeon ,  Brian Safina ,  Tao Sheng ,  Shaoyi Sun ,  Michael Scott Wilson ,  Alla Yurevna Zenova

IPC: C07D401/14 ,  A61K31/437 ,  C07D471/04 ,  C07D519/00 ,  C07D471/08

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：US20150291623A1

公开(公告)日：2015-10-15

申请号：US14542367

申请日：2014-11-14

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Mikhail Chafeev ,  Sultan Chowdhury ,  Lauren Fraser ,  Jianmin Fu ,  Jonathan Langille ,  Shifeng Liu ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov ,  Mark Wood ,  Alla Yurevna Zenova ,  Qi Jia ,  Jean-Jacques Alexandre Cadieux ,  Simon J. Gauthier ,  Amy Frances Douglas ,  Tom Hsieh ,  Nagasree Chakka ,  Zoran Cikojevic

IPC: C07D513/20 ,  C07D519/00 ,  C07D491/22 ,  C07D491/20 ,  C07D498/20

CPC classification number: C07D513/22 ,  C07D491/10 ,  C07D491/107 ,  C07D491/20 ,  C07D491/22 ,  C07D495/20 ,  C07D498/20 ,  C07D513/20 ,  C07D519/00

Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract translation: 本发明涉及螺 - 羟吲哚化合物，作为立体异构体，对映体，其互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。

公开(公告)号：US08933236B2

公开(公告)日：2015-01-13

申请号：US13899469

申请日：2013-05-21

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 ,  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.

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。