-
公开(公告)号:US08101764B2
公开(公告)日:2012-01-24
申请号:US12296557
申请日:2007-06-08
申请人: Albert Kudzovi Amegadzie , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu , Patrick Gianpietro Spinazze
发明人: Albert Kudzovi Amegadzie , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu , Patrick Gianpietro Spinazze
IPC分类号: C07D513/02
CPC分类号: C07D495/04
摘要: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
摘要翻译: 本发明涉及式(I)的黑色素浓缩激素拮抗剂化合物:其中R1,Ra,Rb,R2,L1,R3,R4和R5如上所定义,或其药学上可接受的盐,对映体,非对映体或非对映异构体的混合物 其用于治疗,肥胖和相关疾病。
-
公开(公告)号:US20100016350A1
公开(公告)日:2010-01-21
申请号:US12296557
申请日:2007-06-08
申请人: Albert Kudzovi Amegadzie , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianlaing Lu , Patrick Gianpietro Spinazze
发明人: Albert Kudzovi Amegadzie , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianlaing Lu , Patrick Gianpietro Spinazze
IPC分类号: A61K31/4365 , C07D495/04 , A61P3/04
CPC分类号: C07D495/04
摘要: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
摘要翻译: 本发明涉及式(I)的黑色素浓缩激素拮抗剂化合物:其中R1,Ra,Rb,R2,L1,R3,R4和R5如上所定义,或其药学上可接受的盐,对映体,非对映体或非对映异构体的混合物 其用于治疗,肥胖和相关疾病。
-
公开(公告)号:US20090233919A1
公开(公告)日:2009-09-17
申请号:US11721079
申请日:2005-12-16
申请人: Albert Kudzovi Amegadzie , James Peter Beck , Kevin Matthew Gardinier , Erik James Hembre , James Craig Ruble , Brian David Wakefield
发明人: Albert Kudzovi Amegadzie , James Peter Beck , Kevin Matthew Gardinier , Erik James Hembre , James Craig Ruble , Brian David Wakefield
IPC分类号: A61K31/536 , C07D513/02 , A61K31/4365 , C07D417/14 , A61K31/496 , C07D265/36 , C07D413/14 , A61K31/5377 , A61P3/04
CPC分类号: C07D513/04
摘要: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein w, R1, q, p, R2, t, Ar1, L1, R3 and R4 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.
摘要翻译: 本发明涉及式(I)的黑色素浓缩激素拮抗剂化合物; 其中w,R1,q,p,R2,t,Ar1,L1,R3和R4如上所定义,或其药学上可接受的盐,溶剂化物或对映异构体可用于治疗,预防或改善与肥胖相关的症状和相关 疾病
-
公开(公告)号:US07320994B2
公开(公告)日:2008-01-22
申请号:US10512249
申请日:2003-04-22
申请人: Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , Erik James Hembre , Jian Eric Hong , Louis Nickolaus Jungheim , Brian Stephen Muehl , David Michael Remick , Michael Alan Robertson , Kenneth Allen Savin
发明人: Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , Erik James Hembre , Jian Eric Hong , Louis Nickolaus Jungheim , Brian Stephen Muehl , David Michael Remick , Michael Alan Robertson , Kenneth Allen Savin
IPC分类号: A61K31/41 , C07D249/04
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)
-
公开(公告)号:US07902356B2
公开(公告)日:2011-03-08
申请号:US11721079
申请日:2005-12-16
申请人: Albert Kudzovi Amegadzie , James Peter Beck , Kevin Matthew Gardinier , Erik James Hembre , James Craig Ruble , Kenneth Allen Savin , Brian David Wakefield
发明人: Albert Kudzovi Amegadzie , James Peter Beck , Kevin Matthew Gardinier , Erik James Hembre , James Craig Ruble , Kenneth Allen Savin , Brian David Wakefield
IPC分类号: C07D265/36 , C07D413/00 , C07D401/00 , C07D513/02
CPC分类号: C07D513/04
摘要: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein w, R1, q, p, R2, t, Ar1, L1, R3 and R4 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.
摘要翻译: 本发明涉及式(I)的黑色素浓缩激素拮抗剂化合物; 其中w,R1,q,p,R2,t,Ar1,L1,R3和R4如上所定义,或其药学上可接受的盐,溶剂化物或对映异构体可用于治疗,预防或改善与肥胖相关的症状和相关 疾病
-
公开(公告)号:US07179804B2
公开(公告)日:2007-02-20
申请号:US10512248
申请日:2003-04-22
申请人: Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , Erik James Hembre , Jian Eric Hong , Louis Nickolaus Jungheim , Michael Alan Robertson , Kenneth Allen Savin
发明人: Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , Erik James Hembre , Jian Eric Hong , Louis Nickolaus Jungheim , Michael Alan Robertson , Kenneth Allen Savin
IPC分类号: A61K31/4192 , A61K31/4406 , A61K31/4409 , A61K31/497 , A61K31/541 , A61K31/5377 , C07D261/08 , C07D413/06 , C07D417/14 , C07F7/10
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
-
公开(公告)号:US20080287504A1
公开(公告)日:2008-11-20
申请号:US11840417
申请日:2007-08-17
申请人: Jennifer Rebecca Allen , Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , George Stuart Gregory , Stephen Andrew Hitchcock , Paul J. Hoogestraat , Winton Dennis Jones, JR. , Daryl Lynn Smith
发明人: Jennifer Rebecca Allen , Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , George Stuart Gregory , Stephen Andrew Hitchcock , Paul J. Hoogestraat , Winton Dennis Jones, JR. , Daryl Lynn Smith
IPC分类号: A61K31/404 , A61K31/4439 , A61P3/04
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。
-
公开(公告)号:US07276516B2
公开(公告)日:2007-10-02
申请号:US10596495
申请日:2004-12-13
申请人: Jennifer Rebecca Allen , Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , George Stuart Gregory , Steven Andrew Hitchcock , Paul J. Hoogestraat , Winton Dennis Jones, Jr. , Daryl Lynn Smith
发明人: Jennifer Rebecca Allen , Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , George Stuart Gregory , Steven Andrew Hitchcock , Paul J. Hoogestraat , Winton Dennis Jones, Jr. , Daryl Lynn Smith
IPC分类号: A01N43/42 , A01N43/38 , A61K31/44 , C07D471/02 , C07D491/02
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
-
公开(公告)号:US07595339B2
公开(公告)日:2009-09-29
申请号:US11840417
申请日:2007-08-17
申请人: Jennifer Rebecca Allen , Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , George Stuart Gregory , Stephen Andrew Hitchcock , Paul J. Hoogestraat , Winton Dennis Jones, Jr. , Daryl Lynn Smith
发明人: Jennifer Rebecca Allen , Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , George Stuart Gregory , Stephen Andrew Hitchcock , Paul J. Hoogestraat , Winton Dennis Jones, Jr. , Daryl Lynn Smith
IPC分类号: A61K31/40
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。
-
-
-
-
-
-
-
-