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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。
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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
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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。
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公开(公告)号:US20120302547A1
公开(公告)日:2012-11-29
申请号:US13569899
申请日:2012-08-08
申请人: Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
发明人: Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
IPC分类号: A61K31/4365 , A61P3/04 , A61K31/496 , C07D495/04 , A61K31/5377
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R 1,R a,R b,R 2,L 1,R 3,R 4和R 5如所定义,或其药学上可接受的盐,对映体,非对映异构体或其非对映异构体的混合物 用于治疗,肥胖和相关疾病。
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公开(公告)号:US07838543B2
公开(公告)日:2010-11-23
申请号:US11719576
申请日:2005-12-16
申请人: James Peter Beck , Brian David Wakefield , Frederic Laurent Cordier , Esteban Dominguez-Manzanares , Kevin Matthew Gardinier , Peter Michael Greenen , Kenneth Allen Savin
发明人: James Peter Beck , Brian David Wakefield , Frederic Laurent Cordier , Esteban Dominguez-Manzanares , Kevin Matthew Gardinier , Peter Michael Greenen , Kenneth Allen Savin
IPC分类号: A01N43/78 , A61K31/425 , C07D417/00 , C07D277/60
CPC分类号: C07D263/58 , C07D277/68 , C07D277/82 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein Ar1, L1, R1, q, X, R2, R3, R4, and R5 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Ar 1,L 1,R 1,q,X,R 2,R 3,R 4和R 5如所定义,或其药学上可接受的盐,溶剂合物或对映异构体可用于治疗,预防或改善与肥胖症和相关疾病相关的症状 。
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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
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公开(公告)号:US08263772B2
公开(公告)日:2012-09-11
申请号:US12298792
申请日:2007-06-08
申请人: Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
发明人: Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
IPC分类号: C07D515/04 , A61K31/4365
CPC分类号: C07D495/04
摘要: The present invention relates to a melanin concentrating hormone antagonist compound of formula (1): 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(1)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如上定义,或其药学上可接受的盐,对映异构体,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。
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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。
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公开(公告)号:US20090170913A1
公开(公告)日:2009-07-02
申请号:US11719576
申请日:2005-12-16
申请人: James Peter Beck , Brian David Wakefield , Frederic Laurent Cordier , Esteban Dominguez-Manzanares , Kevin Matthew Gardinier , Peter Michael Greenen , Kenneth Allen Savin
发明人: James Peter Beck , Brian David Wakefield , Frederic Laurent Cordier , Esteban Dominguez-Manzanares , Kevin Matthew Gardinier , Peter Michael Greenen , Kenneth Allen Savin
IPC分类号: A61K31/428 , C07D417/04 , A61P3/04
CPC分类号: C07D263/58 , C07D277/68 , C07D277/82 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein Ar1, L1, R1, q, X, R2, R3, R4, and R5 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Ar 1,L 1,R 1,q,X,R 2,R 3,R 4和R 5如所定义,或其药学上可接受的盐,溶剂合物或对映异构体可用于治疗,预防或改善与肥胖症和相关疾病相关的症状 。
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公开(公告)号:US20090093456A1
公开(公告)日:2009-04-09
申请号:US12298792
申请日:2007-06-08
申请人: Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
发明人: Macklin Brian Arnold , Yen Dao , Kevin Matthew Gardinier , David Joseph Garmene , Steven James Green , Erik James Hembre , Jianliang Lu
IPC分类号: A61K31/4365 , C07D495/04 , A61K31/5377
CPC分类号: C07D495/04
摘要: The present invention relates to a melanin concentrating hormone antagonist compound of formula (1): 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(1)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如上定义,或其药学上可接受的盐,对映异构体,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。
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