公开(公告)号：US09480677B2

公开(公告)日：2016-11-01

申请号：US14510634

申请日：2014-10-09

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Mikhail Chafeev ,  Jianmin Fu ,  Jean-Jacques Alexandre Cadieux

IPC: A61K31/407 ,  C07D491/22 ,  C07D491/20

CPC classification number: C07D491/20 ,  A61K31/407 ,  C07B57/00 ,  C07B2200/07 ,  C07D491/22

Abstract: This invention is directed to the (S)-enantiomer of the compound of formula (I): or a pharmaceutically acceptable solvate or prodrug thereof. This (S)-enantiomer is useful for the treatment of diseases or conditions, such as pain, which are ameliorated or alleviated by the modulation of voltage-gated sodium channels.

Abstract translation: 本发明涉及式（I）化合物的（S） - 对映异构体的制备方法：该（S） - 对映体可用于治疗疾病或病症如疼痛，其被改善或缓解 通过电压门控钠通道的调制。

公开(公告)号：US09260446B2

公开(公告)日：2016-02-16

申请号：US14272297

申请日：2014-05-07

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Jean-Jacques Alexandre Cadieux ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jianmin Fu ,  Qi Ji ,  Stefanie Abel ,  Emad El-Sayed ,  Elke Huthmann ,  Thomas Isarno

IPC: C07D491/20

CPC classification number: C07D491/20 ,  C07D405/04

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

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：US20140296245A1

公开(公告)日：2014-10-02

申请号：US14355552

申请日：2012-10-30

Applicant: XENON PHARMACEUTICALS INC.

Inventor： Shaoyi Sun ,  Alla Yurevna Zenova ,  Mikhail Chafeev ,  Qi Jia ,  Zaihui Zhang ,  Renata Marcella Oballa

IPC: C07D417/12 ,  C07D285/08 ,  C07D257/06 ,  C07D277/52 ,  C07D261/14 ,  C07D239/42 ,  C07D285/135

CPC classification number: C07D239/42 ,  C07D211/22 ,  C07D257/06 ,  C07D261/14 ,  C07D277/52 ,  C07D285/08 ,  C07D285/135 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

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

Abstract translation: 本发明涉及苯磺酰胺化合物，作为立体异构体，对映异构体，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钠通道介导的疾病或病症，例如疼痛。

公开(公告)号：US20130317000A1

公开(公告)日：2013-11-28

申请号：US13899469

申请日：2013-05-21

Applicant: XENON PHARMACEUTICALS INC. ,  GENENTECH, 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 ,  C07D413/12 ,  C07D295/26 ,  C07D233/84 ,  C07D207/48 ,  C07D451/02 ,  C07C307/06 ,  C07D311/70

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：US20240342156A1

公开(公告)日：2024-10-17

申请号：US18415139

申请日：2024-01-17

Applicant: Xenon Pharmaceuticals Inc.

Inventor： James Philip Johnson, JR. ,  Gregory N. Beatch

IPC: A61K31/472 ,  A61K9/00 ,  A61P23/00

CPC classification number: A61K31/472 ,  A61K9/0053 ,  A61P23/00

Abstract: In certain embodiments, the present disclosure is directed to methods for treating pain in a subject, such as a human, wherein the methods comprise orally administering a therapeutically effective amount of N-[4-(6-fluoro-3,4-dihydro-1H-isoquinolin-2-yl)-2,6-dimethylphenyl]-3,3-dimethylbutanamide (Compound A), to the subject in need thereof. The present disclosure is further directed to various improved methods of therapy and administration of Compound A.

公开(公告)号：US20240101531A1

公开(公告)日：2024-03-28

申请号：US18330100

申请日：2023-06-06

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Paul Scott Charifson ,  Christoph Martin Dehnhardt ,  Julien A. Delbrouck ,  Thilo Focken ,  Wei Gong ,  Shawn Johnstone ,  Xiangyu Li ,  Jia Yi Mo ,  Juliette Sabbatani ,  Hong Wang ,  Steven Sigmund Wesolowski ,  Alla Yurevna Zenova ,  Wei Zhang

IPC: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D495/04 ,  C07D513/04 ,  C07D471/04 ,  C07D491/048 ,  C07D491/107 ,  C07D498/04 ,  C07D413/14 ,  C07D487/04 ,  C07D417/14 ,  C07D409/14 ,  C07B59/00 ,  A61P25/08

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D495/04 ,  C07D513/04 ,  C07D471/04 ,  C07D491/048 ,  C07D491/107 ,  C07D498/04 ,  C07D413/14 ,  C07D487/04 ,  C07D417/14 ,  C07D409/14 ,  C07B59/002 ,  A61P25/08 ,  C07B2200/05

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




wherein m, n, Y, R1, R2, R3, R4 and R5 are each 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 potassium channel modulators and are therefore are useful in treating seizure disorders such as epilepsy.

公开(公告)号：US20220288057A1

公开(公告)日：2022-09-15

申请号：US17668316

申请日：2022-02-09

Applicant: XENON PHARMACEUTICALS INC.

Inventor： James Philip JOHNSON, JR.

IPC: A61K31/472 ,  A61K31/19 ,  A61K31/4015 ,  A61K31/4166 ,  A61K31/165 ,  A61K31/41 ,  A61P25/08

Abstract: In certain embodiments, the present disclosure is directed to methods and uses for treating seizure disorders in a human in need thereof, wherein the methods and uses comprise conjointly administering N-[4-(6-fluoro-3,4-dihydro-1H-isoquinolin-2-yl)-2,6-dimethylphenyl]-3,3-dimethylbutanamide (Compound A) and an antiseizure medication (ASM) to the human in amounts that are therapeutically effective when conjointly administered. The present disclosure is further directed to various improved methods of therapy and administration of Compound A.

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.