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公开(公告)号:US09187464B2
公开(公告)日:2015-11-17
申请号:US14125378
申请日:2012-06-15
申请人: Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Tram H. Hoang , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
发明人: Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Tram H. Hoang , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
IPC分类号: C07D263/02 , A61K31/423 , C07D413/14 , C07D417/14 , C07D495/04 , C07F9/6558 , C07D419/14
CPC分类号: C07D413/14 , C07D417/14 , C07D419/14 , C07D495/04 , C07F9/65583
摘要: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
摘要翻译: 本发明涉及其中R1,(R2)Y,R3,R4,X和A具有本说明书中给出的含义的式(I)的螺氨酸甲酯化合物。 本发明还提供含有化合物或其药学上可接受的盐的药物组合物,并且涉及它们在治疗或预防与TRPV4不平衡相关的病症中作为TRPV4拮抗剂的用途。
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公开(公告)号:US09212127B2
公开(公告)日:2015-12-15
申请号:US11660693
申请日:2005-08-22
申请人: Lloyd S. Gray , Timothy L. MacDonald , Doris M. Haverstick , Jaclyn R. Patterson , William F. McCalmont
发明人: Lloyd S. Gray , Timothy L. MacDonald , Doris M. Haverstick , Jaclyn R. Patterson , William F. McCalmont
IPC分类号: C07C217/58 , C07C217/60 , C07C217/62 , A61K31/137 , A61K31/138 , A61K45/06
CPC分类号: A61K31/14 , A61K31/085 , A61K31/12 , A61K31/137 , A61K31/138 , A61K45/06 , C07C217/58 , C07C217/60 , C07C217/62 , A61K2300/00
摘要: The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, wherein R1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; Z is NH, NCH3, O, S, or CH2; Y is NH, O, or CH2 with the proviso that Y and Z are not the same; R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; and R3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.
摘要翻译: 本发明提供式(I)的新型T型钙通道抑制剂,其用于治疗与通过T型钙通道流入胞外钙相关的哺乳动物中的疾病或病症,其中R 1为C 1 -C 4烷基, 羟基或C 1 -C 4烷氧基; Z是NH,NCH 3,O,S或CH 2; Y是NH,O或CH 2,条件是Y和Z不相同; R2是H,卤素,NH2,C1-C4烷基,羟基或C1-C4烷氧基; m和n独立地选自1-5的整数,条件是m + n = 2-9的整数; 并且R 3是H,卤素,NH 2,C 1 -C 4烷基,羟基或C 1 -C 4烷氧基。
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公开(公告)号:US20140113916A1
公开(公告)日:2014-04-24
申请号:US14125370
申请日:2012-06-15
申请人: Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
发明人: Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
IPC分类号: C07D413/14 , C07D413/06
CPC分类号: C07D413/14 , C07D263/52 , C07D413/06 , C07D413/08
摘要: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
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公开(公告)号:US20100280005A1
公开(公告)日:2010-11-04
申请号:US12450620
申请日:2008-04-04
申请人: Jonh J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , John Gleason , Alexey V. Ishchenko , Brian Lawhorn , Gerard McGeehan , Jaclyn R. Patterson , Simon F. Semus , Robert D. Simpson , Suresh B. Singh , Colin Tice , Tritin Tran , Zhenrong Xu , Jing Yuan , Wei Zhao
发明人: Jonh J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , John Gleason , Alexey V. Ishchenko , Brian Lawhorn , Gerard McGeehan , Jaclyn R. Patterson , Simon F. Semus , Robert D. Simpson , Suresh B. Singh , Colin Tice , Tritin Tran , Zhenrong Xu , Jing Yuan , Wei Zhao
IPC分类号: A61K31/445 , C07D211/60 , C07D401/02 , C07D413/02 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K31/58 , A61P9/12
CPC分类号: C07D211/22 , C07D401/06
摘要: Disclosed are compounds of Formula I, wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
摘要翻译: 公开了式I的化合物,其中R,R 1,R 2,R 3,X,Y,A,Q,E和G如本文所定义。 这些化合物与天冬氨酸蛋白酶结合以抑制其活性,并且可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 还公开了使用式I化合物在有需要的受试者中改善或治疗天冬氨酸蛋白酶相关病症的方法。
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公开(公告)号:US09487507B2
公开(公告)日:2016-11-08
申请号:US14125370
申请日:2012-06-15
申请人: Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
发明人: Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
IPC分类号: A01N43/76 , A61K31/42 , C07D263/52 , C07D498/00 , C07D413/14 , C07D413/06 , C07D413/08
CPC分类号: C07D413/14 , C07D263/52 , C07D413/06 , C07D413/08
摘要: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
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公开(公告)号:US20140121206A1
公开(公告)日:2014-05-01
申请号:US14125378
申请日:2012-06-15
申请人: Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Tram H. Hoang , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
发明人: Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Tram H. Hoang , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
IPC分类号: C07D413/14 , C07D495/04 , C07D417/14
CPC分类号: C07D413/14 , C07D417/14 , C07D419/14 , C07D495/04 , C07F9/65583
摘要: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
摘要翻译: 本发明涉及其中R1,(R2)Y,R3,R4,X和A具有本说明书中给出的含义的式(I)的螺氨酸甲酯化合物。 本发明还提供含有化合物或其药学上可接受的盐的药物组合物,并且涉及它们在治疗或预防与TRPV4不平衡相关的病症中作为TRPV4拮抗剂的用途。
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公开(公告)号:US20100179109A1
公开(公告)日:2010-07-15
申请号:US12450631
申请日:2008-04-04
申请人: Jonh J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiano Ghirlanda , Alexey V. Ishchenko , Lara S. Kallander , Brian Lawhorn , Colin A. Leach , Qing Lu , Gerard McGeehan , Jaclyn R. Patterson , Robert D. Simpson , Suresh B. Singh , Patrick Stoy , Lamont R. Terrell , Colin Tice , Zhenrong Xu , Jing Yuan , Catherine C. K. Yuan , Jing Zhang , Wei Zhao
发明人: Jonh J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiano Ghirlanda , Alexey V. Ishchenko , Lara S. Kallander , Brian Lawhorn , Colin A. Leach , Qing Lu , Gerard McGeehan , Jaclyn R. Patterson , Robert D. Simpson , Suresh B. Singh , Patrick Stoy , Lamont R. Terrell , Colin Tice , Zhenrong Xu , Jing Yuan , Catherine C. K. Yuan , Jing Zhang , Wei Zhao
IPC分类号: A61K31/675 , C07D211/34 , A61K31/445 , C07D265/30 , A61K31/5375 , C07D413/06 , A61K31/5377 , A61K31/535 , A61K31/517 , A61K31/554 , A61K31/4965 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/47 , A61K31/566 , A61P25/28 , A61P33/06 , A61P31/18 , A61P9/12 , A61P9/10 , A61P25/22 , A61P27/06
CPC分类号: C07D211/96 , C07D211/22 , C07D401/10 , C07D401/12
摘要: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
摘要翻译: 公开了式(I)的化合物,其中R,R 1,R 2,R 3,X,Y,A,Q,E和G如本文所定义。 这些化合物与天冬氨酸蛋白酶结合以抑制其活性,并且可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 还公开了使用式I化合物在有需要的受试者中改善或治疗天冬氨酸蛋白酶相关病症的方法。
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公开(公告)号:US20090234019A1
公开(公告)日:2009-09-17
申请号:US11660693
申请日:2005-08-22
申请人: Lloyd S. Gray , Timothy L. MacDonald , Doris M. Haverstick , Jaclyn R. Patterson , William F. McClamont
发明人: Lloyd S. Gray , Timothy L. MacDonald , Doris M. Haverstick , Jaclyn R. Patterson , William F. McClamont
IPC分类号: A61K31/138 , C07C211/27 , A61P35/00
CPC分类号: A61K31/14 , A61K31/085 , A61K31/12 , A61K31/137 , A61K31/138 , A61K45/06 , C07C217/58 , C07C217/60 , C07C217/62 , A61K2300/00
摘要: The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, whereinR1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy;Z is NH, NCH3, O, S, or CH2;Y is NH, O, or CH2 with the proviso that Y and Z are not the same;R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy;m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; andR3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.
摘要翻译: 本发明提供式(I)的新型T型钙通道抑制剂,其用于治疗与通过T型钙通道流入胞外钙相关的哺乳动物中的疾病或病症,其中R 1为C 1 -C 4烷基, 羟基或C 1 -C 4烷氧基; Z是NH,NCH 3,O,S或CH 2; Y是NH,O或CH 2,条件是Y和Z不相同; R2是H,卤素,NH2,C1-C4烷基,羟基或C1-C4烷氧基; m和n独立地选自1-5的整数,条件是m + n = 2-9的整数; 并且R 3是H,卤素,NH 2,C 1 -C 4烷基,羟基或C 1 -C 4烷氧基。
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