公开(公告)号：US20240316033A1

公开(公告)日：2024-09-26

申请号：US18679045

申请日：2024-05-30

申请人： Xenon Pharmaceuticals Inc.

发明人： Gregory N. Beatch

IPC分类号： A61K31/472 ,  A61K9/00 ,  A61P25/08

CPC分类号： A61K31/472 ,  A61K9/0053 ,  A61P25/08

摘要： In certain embodiments, the present disclosure is directed to methods and uses for treating seizure disorders in a human, wherein the methods and uses comprise orally administering a therapeutically effective amount of the voltage-gated potassium channel allosteric modulator, 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, for example, under fed conditions. The present disclosure is further directed to various improved methods of therapy and administration of Compound A.

公开(公告)号：US12054486B2

公开(公告)日：2024-08-06

申请号：US17951640

申请日：2022-09-23

申请人： Xenon Pharmaceuticals Inc.

发明人： 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分类号： C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/052

CPC分类号： C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/052

摘要： 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：US11957675B2

公开(公告)日：2024-04-16

申请号：US17668340

申请日：2022-02-09

申请人： XENON PHARMACEUTICALS INC.

发明人： Simon Neil Pimstone

IPC分类号： A61K31/472 ,  A61P25/24

CPC分类号： A61K31/472 ,  A61P25/24

摘要： 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：US20220193070A1

公开(公告)日：2022-06-23

申请号：US17532909

申请日：2021-11-22

申请人： XENON PHARMACEUTICALS INC. ,  THE UNIVERSITY OF BRITISH COLUMBIA

发明人： Robin Paul SHERRINGTON ,  Mary B. CONNOLLY

IPC分类号： A61K31/495 ,  A61P25/08

摘要： In certain embodiments, the present disclosure is directed to methods and uses of flunarizine, including for treating absence seizures in a human patient, such as absence seizures in childhood absence epilepsy (CAE), wherein the methods comprise administering (e.g., orally) to a patient in need thereof a therapeutically effective amount of flunarizine. The present disclosure is further directed to various improved methods of therapy and administration of flunarizine.

公开(公告)号：US11203572B2

公开(公告)日：2021-12-21

申请号：US17011355

申请日：2020-09-03

申请人： GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

发明人： Sultan Chowdhury ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Ivan William Hemeon ,  Steven McKerrall ,  Daniel Sutherlin

IPC分类号： C07C381/10 ,  C07D401/12 ,  C07D205/04 ,  C07D211/22 ,  C07D211/42 ,  C07D213/69 ,  A61P25/04

摘要： 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, ring B, R1, 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：US10745392B2

公开(公告)日：2020-08-18

申请号：US16440459

申请日：2019-06-13

申请人： Xenon Pharmaceuticals Inc.

发明人： Kristen Nicole Burford ,  Thilo Focken ,  Verner Alexander Lofstrand ,  Michael Scott Wilson ,  Alla Yurevna Zenova

IPC分类号： C07D417/12 ,  A61P25/08 ,  C07D277/52 ,  C07D413/12

摘要： 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：US20200157089A1

公开(公告)日：2020-05-21

申请号：US16556055

申请日：2019-08-29

申请人： Xenon Pharmaceuticals Inc.

发明人： 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分类号： C07D417/14 ,  C07D417/12 ,  C07D401/14 ,  C07D401/12 ,  C07D409/12 ,  C07D487/08 ,  C07D471/04 ,  C07D413/12

摘要： 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：US20200071313A1

公开(公告)日：2020-03-05

申请号：US16555983

申请日：2019-08-29

申请人： Xenon Pharmaceuticals Inc.

发明人： Jean-Christophe Andrez ,  Kristen Nicole Burford ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Qi Jia ,  Verner Alexander Lofstrand ,  Steven Sigmund Wesolowski ,  Michael Scott Wilson

IPC分类号： C07D417/14 ,  C07D409/14 ,  C07D401/14 ,  A61P25/08 ,  C07C53/18

摘要： This invention is directed to heteroaryl-substituted sulfonamide 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.

公开(公告)号：US20200030260A1

公开(公告)日：2020-01-30

申请号：US16523568

申请日：2019-07-26

申请人： Xenon Pharmaceuticals Inc.

发明人： Robin Paul Sherrington ,  Jean-Jacques Alexandre Cadieux ,  Parisa Karimi Tari ,  Jeffrey Paul Bechard

IPC分类号： A61K31/137 ,  A61K31/24 ,  A61P25/08

摘要： In certain embodiments, the present disclosure is directed to methods and uses for treating a mammal having an epileptic seizure disorder or being at risk for having an epileptic seizure disorder, comprising administering certain herein disclosed isolated fenfluramine enantiomers that are surprisingly effective as anti-epilepsy drugs (AEDs), despite having lower anti-seizure potency than fenfluramine racemate, by virtue of also being less cardiotoxic than fenfluramine racemate. Preferred embodiments contemplate treatment of Dravet syndrome; other preferred embodiments contemplate treatment of other epileptic seizure disorders.

公开(公告)号：US20190031607A1

公开(公告)日：2019-01-31

申请号：US16150070

申请日：2018-10-02

申请人： GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

发明人： 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 Salvatore SAFINA ,  Shaoyi SUN ,  Michael Scott WILSON ,  Alla Yurevna ZENOVA

IPC分类号： C07D207/16 ,  C07C235/52 ,  C07D209/02 ,  C07D401/10 ,  C07D205/04 ,  C07D207/22 ,  C07D211/20 ,  C07C235/42 ,  C07D211/38 ,  C07D409/06 ,  C07D265/30 ,  C07D413/12 ,  C07D263/26 ,  C07C235/54 ,  C07D417/12 ,  C07D305/08 ,  C07D213/69 ,  C07D403/04 ,  C07D231/06 ,  C07D209/52 ,  C07D221/22 ,  C07D209/54 ,  C07D403/12 ,  C07D211/60 ,  C07D207/10 ,  C07D401/12 ,  C07D471/08 ,  C07D413/14 ,  C07D207/08 ,  C07D405/10 ,  C07D403/14 ,  C07D451/02 ,  C07D401/14 ,  C07D263/04 ,  C07D277/06

CPC分类号： 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

摘要： 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.