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：US20130252962A1

公开(公告)日：2013-09-26

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: C07D491/107 ,  C07D495/20 ,  C07D498/20 ,  C07D513/20 ,  C07D491/20

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.

公开(公告)号：US20250129044A1

公开(公告)日：2025-04-24

申请号：US18669938

申请日：2024-05-21

Applicant: XENON PHARMACEUTICALS INC.

Inventor： Verner Alexander LOFSTRAND ,  Jung Yun KIM ,  Helen CLEMENT ,  Kristen Nicole BURFORD ,  Paul CHARIFSON ,  Michael CLARK

IPC: C07D401/12 ,  C07D211/56 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/08 ,  C07D487/08 ,  C07D487/10 ,  C07D497/08 ,  C07D498/04 ,  C07D498/08

Abstract: The present disclosure is directed to compounds of formula (I): wherein X, Y, Z, R1, R2a, R2b, R3, and L 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：US12178811B2

公开(公告)日：2024-12-31

申请号：US17093183

申请日：2020-11-09

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Cynthia Louise Harden ,  Gregory N. Beatch

IPC: A61K31/472 ,  A61K9/00 ,  A61P25/24

Abstract: In certain embodiments, the present disclosure is directed to methods for treating depressive disorders in 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 human 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：US12171759B1

公开(公告)日：2024-12-24

申请号：US18604727

申请日：2024-03-14

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Simon Neil Pimstone

IPC: A61K31/472 ,  A61P25/24

Abstract: The present disclosure is directed to, among other things, methods and uses for treating anhedonia in a subject, such as a human, wherein the methods comprise 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, and the uses comprise Compound A for use in treating anhedonia in a subject, such as a human. The present disclosure is further directed to various improved methods of therapy and administration of Compound A.

公开(公告)号：US20240408076A1

公开(公告)日：2024-12-12

申请号：US18604727

申请日：2024-03-14

Applicant: Xenon Pharmaceuticals Inc.,

Inventor： Simon Neil Pimstone

IPC: A61K31/472 ,  A61P25/24

Abstract: The present disclosure is directed to, among other things, methods and uses for treating anhedonia in a subject, such as a human, wherein the methods comprise 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, and the uses comprise Compound A for use in treating anhedonia in a subject, such as a human. The present disclosure is further directed to various improved methods of therapy and administration of Compound A.

公开(公告)号：US20240279182A1

公开(公告)日：2024-08-22

申请号：US18540582

申请日：2023-12-14

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Paul Robert Bichler ,  Jean-Jacques Alexandre Cadieux ,  Matthew David Tandy ,  Gregory N. Beatch

IPC: C07D217/04

CPC classification number: C07D217/04 ,  C07B2200/13

Abstract: The present disclosure provides solid state forms of a selective potassium channel modulator and pharmaceutical compositions comprising the solid state crystalline forms and pharmaceutically acceptable excipients, and methods for preparing and using the solid state forms and the pharmaceutical compositions thereof.

公开(公告)号：US20230404913A1

公开(公告)日：2023-12-21

申请号：US18248661

申请日：2021-04-09

Applicant: Xenon Pharmaceuticals, Inc.

Inventor： Jean-Jacques Alexandre Cadieux ,  Matthew David Tandy

IPC: A61K9/00 ,  A61K9/16 ,  A61K9/20 ,  A61K9/10 ,  A61K9/28 ,  A61K31/635 ,  A23L33/00 ,  A23L33/125

CPC classification number: A61K9/0053 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/1617 ,  A61K9/2054 ,  A61K9/2013 ,  A61K9/10 ,  A61K9/2866 ,  A61K31/635 ,  A23L33/40 ,  A23L33/125

Abstract: Provided herein are certain pharmaceutical compositions comprising (S)-4-((1-benzylpyrrolidin-3-yl)(methyl)amino)-2-fluoro-5-methyl-N-(thiazol-4-yl)benzene-sulfonamide (Compound A), or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient. The pharmaceutical compositions can be present in form of an immediate release tablet, a granular formulation, a stable suspension oral dosage form or a multi-particulate sprinkle dosage form. Methods for the treatment of a disease or a condition associated with Naj4.6 activity, such as epilepsy, are described.