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公开(公告)号:US20060160794A1
公开(公告)日:2006-07-20
申请号:US10559852
申请日:2004-06-03
申请人: Albert Amegadzie , Kevin Gardinier , Erik Hembre , Philip Hipskind , Louis Jungheim , Brian Muehl , Kenneth Savin , Keneth Thrasher , Steven Boyd
发明人: Albert Amegadzie , Kevin Gardinier , Erik Hembre , Philip Hipskind , Louis Jungheim , Brian Muehl , Kenneth Savin , Keneth Thrasher , Steven Boyd
IPC分类号: A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/4192 , A61K31/4172 , C07D403/02 , C07D413/02 , C07D417/02
CPC分类号: C07D401/04 , C07D249/04 , C07D249/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/06 , C07D417/12 , C07D487/04
摘要: The present invention relates to selective NK-1 receptor antagonists of Formula (I) or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
摘要翻译: 本发明涉及式(I)的选择性NK-1受体拮抗剂或其药学上可接受的盐,用于治疗与过速速激肽相关的疾病。
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公开(公告)号:US20080090860A1
公开(公告)日:2008-04-17
申请号:US11895278
申请日:2007-08-23
申请人: Kevin Gardinier , Douglas Gernert , Timothy Grese , David Neel , Christopher Mapes , Pierre-Yves Michellys , Marcus Boehm
发明人: Kevin Gardinier , Douglas Gernert , Timothy Grese , David Neel , Christopher Mapes , Pierre-Yves Michellys , Marcus Boehm
IPC分类号: A61K31/437 , A61K31/343 , A61K31/381 , A61K31/405 , A61P17/00 , A61P3/06 , A61P35/00 , C07D209/18 , C07D231/56 , C07D471/04 , C07D333/64 , C07D333/52 , C07D307/82 , C07D261/20 , C07D217/04 , A61P9/00 , A61P3/10 , A61P25/28 , A61K31/472 , A61K31/416 , A61K31/423
CPC分类号: C07D261/20 , C07D209/12 , C07D215/14 , C07D217/16 , C07D231/56 , C07D307/80 , C07D307/85 , C07D333/56 , C07D333/60 , C07D333/70 , C07D471/04 , C07D495/04
摘要: The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof.
摘要翻译: 本发明涉及由结构式I表示的化合物及其药学上可接受的盐,溶剂合物和水合物:本发明还涉及药物组合物,使用方法和制备由结构式I表示的化合物及其药学上可接受的盐,溶剂合物的方法 及其水合物。
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公开(公告)号:US20070088018A1
公开(公告)日:2007-04-19
申请号:US10596495
申请日:2004-12-13
申请人: Jennifer Allen , Albert Amegadzie , Kevin Gardinier , George Gregory , Steven Hitchcock , Paul Hoogestraat , Winton Jones , Daryl Smith
发明人: Jennifer Allen , Albert Amegadzie , Kevin Gardinier , George Gregory , Steven Hitchcock , Paul Hoogestraat , Winton Jones , Daryl Smith
IPC分类号: A61K31/541 , A61K31/5377 , A61K31/501 , A61K31/497 , A61K31/496 , C07D471/02
CPC分类号: C07D209/10 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/40 , C07D209/42 , C07D209/96 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D417/04 , C07D471/04 , C07D471/10 , C07D491/10
摘要: Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.
摘要翻译: 公开了结构式(I)的新型化合物。 作为大麻素-1(CB1)受体的调节剂,这些化合物可用于治疗,预防和抑制由CB1受体介导的疾病。 因此,本发明的化合物可用于治疗,预防和抑制精神病,记忆缺陷,认知障碍,偏头痛,神经病,神经炎症性疾病(例如,多发性硬化症,吉兰巴利综合症和炎性后遗症 病毒性脑炎),脑血管意外,头部创伤,焦虑症,压力,癫痫,帕金森病和精神分裂症。 这些化合物也可用于治疗药物滥用障碍,特别是鸦片剂,酒精和尼古丁。 所述化合物还可用于治疗与过量食物摄入和与其相关的并发症相关的肥胖或进食障碍。
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公开(公告)号:US20050239786A1
公开(公告)日:2005-10-27
申请号:US10512249
申请日:2003-04-22
申请人: Albert Amegadzie , Kevin Gardinier , Erik Hembre , Jian Hong , Louis Jungheim , Brian Muehl , David Remick , Michael Robertson , Kenneth Savin
发明人: Albert Amegadzie , Kevin Gardinier , Erik Hembre , Jian Hong , Louis Jungheim , Brian Muehl , David Remick , Michael Robertson , Kenneth Savin
IPC分类号: A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/5025 , A61K31/503 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P1/04 , A61P1/08 , A61P11/06 , A61P17/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07D249/06 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04 , C07D43/02
CPC分类号: C07D401/04 , C07D249/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D487/04
摘要: This application relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and its use as an inhibitor of the NK-1 subtype of tachykinin receptors, as well as a process for its preparation and intermediates therefor. (I) wherein: D is a C1-C3 alkane-diyl; R1 is phenyl, which is optionally substituted with one to three substitutents independently selected from the group consisting of halo, C1-C4 alkyl, C1-C4 alkoxy, cyano, difluoromethyl, trifluoromethyl, and trifluoromethoxy; R4 is a radical selected from the group consisting of: (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH)
摘要翻译: 本申请涉及式(I)化合物或其药学上可接受的盐,其药物组合物及其作为速激肽受体的NK-1亚型的抑制剂的用途,以及其制备方法及其中间体。 (I)其中:D是C 1 -C 3烷烃二基; R 1是苯基,其任选地被一至三个独立地选自卤素,C 1 -C 4烷基的取代基取代, C 1 -C 4烷氧基,氰基,二氟甲基,三氟甲基和三氟甲氧基; (I),(IB),(IC),(ID),(IE),(IF),(IG),(IH)
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公开(公告)号:US20050239776A1
公开(公告)日:2005-10-27
申请号:US10512248
申请日:2003-04-22
申请人: Albert Amegadzie , Kevin Gardinier , Erik Hembre , Jian Hong , Louis Jungheim , Brian Muehl , David Remick , Michael Robertson , Kenneth Savin
发明人: Albert Amegadzie , Kevin Gardinier , Erik Hembre , Jian Hong , Louis Jungheim , Brian Muehl , David Remick , Michael Robertson , Kenneth Savin
IPC分类号: A61K31/4192 , A61K31/422 , A61K31/4439 , A61K31/444 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P1/00 , A61P1/04 , A61P1/08 , A61P3/10 , A61P7/12 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/04 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P27/02 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D249/04 , C07D249/06 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D413/02 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/02 , C07D417/14 , C07D43/02
CPC分类号: C07D249/06 , C07D249/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/06 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/14
摘要: The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
摘要翻译: 本发明涉及式(I)的选择性NK-1受体拮抗剂; 或其药学上可接受的盐,用于治疗与过速的速激肽相关的病症。
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