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公开(公告)号:US10035801B2
公开(公告)日:2018-07-31
申请号:US14775405
申请日:2014-03-13
Applicant: CONSTELLATION PHARMACEUTICALS, INC. , GENENTECH, INC.
Inventor: Brian K. Albrecht , Steven F. Bellon , Victor S. Gehling , Jean-Christophe Harmange , Kwong Wah Lai , Jun Liang , Peter Dragovich , Daniel F. Ortwine , Sharada Labadie , Birong Zhang , James Richard Kiefer
IPC: C07D487/04 , A61K31/519 , A61K45/06 , A61K31/5377 , A61K31/337 , A61K31/517 , A61K31/437 , C12N9/99 , C07D498/04 , C07D487/14
CPC classification number: C07D487/04 , A61K31/337 , A61K31/437 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D487/14 , C07D498/04 , C12N9/99
Abstract: Provided are compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.
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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。
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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.
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公开(公告)号:US10179767B2
公开(公告)日:2019-01-15
申请号:US15161085
申请日:2016-05-20
Applicant: GENENTECH, INC. , XENON PHARMACEUTICALS INC.
Inventor: Sultan Chowdhury , Christoph Martin Dehnhardt , Abid Hasan , Ivan William Hemeon , Qi Jia , Jun Li , Zhiguo Liu , Daniel F. Ortwine , Brian Safina , Daniel Sutherlin , Shaoyi Sun , Andrew D. White , Wei Gong , Alla Yurevna Zenova , Jiuxiang Zhu
IPC: A01N43/00 , A61K31/00 , C07D211/22 , C07D211/48 , C07D211/34 , C07D405/08 , C07D401/12 , C07D401/08 , C07D211/42 , C07D221/20 , C07D401/04 , C07D211/38 , C07D211/62
Abstract: The invention provides compounds having activity as sodium channel (e.g., NaV1.7) inhibitors that are useful for treating sodium channel-mediated diseases or conditions, such as pain, as well as other diseases and conditions associated with the mediation of sodium channels, and compositions containing such compounds and methods for using such compounds and compositions.
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公开(公告)号:US20170002017A1
公开(公告)日:2017-01-05
申请号:US15017282
申请日:2016-02-05
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: C07D491/107 , C07C311/51 , C07D307/12 , C07D213/82 , C07D205/04 , C07D207/48 , C07D295/26 , C07D257/04 , C07D311/58 , C07D209/52 , C07D307/18 , C07D211/22 , C07D233/84
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: 和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, 化合物和使用这些化合物和组合物的方法。
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公开(公告)号:US08754077B2
公开(公告)日:2014-06-17
申请号:US14154008
申请日:2014-01-13
Applicant: Genentech, Inc.
Inventor: James J. Crawford , Daniel F. Ortwine , BinQing Wei , Wendy B. Young
IPC: A61K31/5377 , A61K31/502 , A61K31/5383
CPC classification number: A61K31/506 , A61K31/502 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D401/10 , C07D401/14 , C07D405/14 , C07D413/14 , C07D487/04 , C07D498/04 , C07D513/04
Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula I where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Abstract translation: 提供了其中X 1,X 2和X 3中的一个或两个为N的式I化合物,其包括用于抑制Btk激酶的立体异构体,互变异构体及其药学上可接受的盐,以及用于 治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式I化合物进行体外,原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。
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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.
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公开(公告)号:US09771376B2
公开(公告)日:2017-09-26
申请号:US15133030
申请日:2016-04-19
Applicant: GENENTECH, INC. , XENON PHARMACEUTICALS INC.
Inventor: Sultan Chowdhury , Christoph Martin Dehnhardt , Thilo Focken , Michael Edward Grimwood , Ivan William Hemeon , Qi Jia , Daniel F. Ortwine , Brian Safina , Shaoyi Sun , Daniel P. Sutherlin , Alla Yurevna Zenova
IPC: C07D257/04 , C07D471/08 , C07D207/46 , C07D213/64 , C07C311/51 , C07D233/84 , C07D205/04 , C07D491/107 , C07D403/12 , C07D213/82 , C07D311/58 , C07D265/30 , C07C307/06 , C07D295/26 , C07D207/48 , C07D311/70 , C07D413/12 , C07D451/02 , C07D307/12 , C07D309/08 , C07D311/72 , C07D405/12 , C07D211/22 , C07D295/192 , C07D211/96 , C07D307/18 , A61K31/18 , A61K31/397 , A61K31/40 , A61K31/41 , A61K31/4164 , A61K31/44 , A61K31/5375 , C07D209/52
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.
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公开(公告)号:US09694002B2
公开(公告)日:2017-07-04
申请号:US15275131
申请日:2016-09-23
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 , A61K31/445 , A61K31/4545 , A61K31/4523
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.
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