公开(公告)号：US20130317001A1

公开(公告)日：2013-11-28

申请号：US13899526

申请日：2013-05-21

Applicant: XENON PHARMACEUTICALS INC. ,  GENENTECH, 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: C07D403/12 ,  C07D213/64 ,  C07D205/04 ,  C07D311/58 ,  C07D295/26 ,  C07D233/84 ,  C07D257/04 ,  C07C311/51 ,  C07C307/06 ,  C07D213/82 ,  C07D265/30

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：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：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：US09458178B2

公开(公告)日：2016-10-04

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 ,  C07D491/10 ,  C07D491/107 ,  C07D491/20 ,  C07D491/22 ,  C07D495/20 ,  C07D498/20 ,  C07D519/00

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：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：US08916580B2

公开(公告)日：2014-12-23

申请号：US13787558

申请日：2013-03-06

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: A61K31/44 ,  C07D491/107 ,  C07D491/10 ,  C07D491/22 ,  C07D491/20 ,  C07D498/20 ,  C07D495/20 ,  C07D513/20

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：US20140024583A1

公开(公告)日：2014-01-23

申请号：US13942404

申请日：2013-07-15

Applicant: Novartis AG ,  Xenon Pharmaceuticals Inc.

Inventor： Natalie Dales ,  Julia Fonarev ,  Jianmin Fu ,  Duanjie Hou ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Vandna Raina ,  Shaoyi Sun ,  Zaihui Zhang

IPC: C07D409/04 ,  A61K31/444 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/497 ,  C07F7/08 ,  C07D417/14 ,  A61K31/4436

CPC classification number: A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07F7/0834

Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.

Abstract translation: 本发明提供调节硬脂酰辅酶A去饱和酶活性的杂环衍生物。 还包括使用这些衍生物调节硬脂酰辅酶A去饱和酶活性的方法和包含这些衍生物的药物组合物。

公开(公告)号：US20130274483A1

公开(公告)日：2013-10-17

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 ,  C07D405/10 ,  C07D209/34 ,  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：US20230203007A1

公开(公告)日：2023-06-29

申请号：US17951644

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 ,  Michael Clark ,  Steve Wesolowski ,  Ravi Munuganti ,  Ramkumar Rajamani

IPC: C07D401/14 ,  C07D401/04 ,  C07D487/04 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  C07D213/82 ,  C07D213/74 ,  C07D491/107 ,  C07D498/08 ,  C07D471/10 ,  C07D471/08 ,  C07D487/10 ,  C07D417/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/14 ,  C07F7/08

CPC classification number: C07D401/14 ,  C07D213/74 ,  C07D213/82 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D471/14 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D498/08 ,  C07F7/0812

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





wherein R1, R2, R3, R3a, R4, Y, and X 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：US20230144095A1

公开(公告)日：2023-05-11

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 ,  C07D401/14 ,  C07D413/14 ,  C07D401/04 ,  C07D491/052 ,  C07D487/04

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

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.