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公开(公告)号:US07084156B2
公开(公告)日:2006-08-01
申请号:US10496615
申请日:2002-11-22
申请人: Robert J. DeVita , Lehua Chang , Danny Chaung , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas W. Sailer , Jonathan R. Young
发明人: Robert J. DeVita , Lehua Chang , Danny Chaung , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas W. Sailer , Jonathan R. Young
IPC分类号: C07D215/38 , C07D215/16 , A61K31/47
CPC分类号: C07D215/227 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D491/04 , C07D495/10
摘要: The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
摘要翻译: 本发明涉及通式I的化合物及其药学上可接受的盐,其可用作黑色素浓缩激素受体拮抗剂,特别是MCH-1R拮抗剂。 因此,本发明的化合物可用于治疗或预防与食物过量摄取及其并发症,骨关节炎,某些癌症,艾滋病消瘦,恶病质,虚弱(特别是老年人)相关的肥胖或进食障碍,精神障碍压力, 认知障碍,性功能,生殖功能,肾功能,运动障碍,注意力缺陷障碍(ADD),药物滥用障碍和运动障碍,亨廷顿病,癫痫,记忆功能和脊髓性肌肉萎缩。 因此,式I化合物可用于治疗这些病症,以及制备用于治疗这些病症的药物。 作为制备这些化合物的方法,公开了包含式(I)化合物之一作为活性成分的药物制剂。
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公开(公告)号:US20050026915A1
公开(公告)日:2005-02-03
申请号:US10496615
申请日:2002-11-22
申请人: Robert DeVita , Lehua Chang , Danny Chaung , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas Sailer , Jonathan Young
发明人: Robert DeVita , Lehua Chang , Danny Chaung , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas Sailer , Jonathan Young
IPC分类号: C07D215/38 , A61K31/403 , A61K31/407 , A61K31/439 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/54 , A61K31/55 , A61P1/14 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/00 , A61P7/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/12 , A61P15/00 , A61P19/02 , A61P21/00 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P35/00 , A61P43/00 , C07D215/22 , C07D215/227 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D453/00 , C07D471/08 , C07D487/08 , C07D487/10 , C07D491/04 , C07D491/08 , C07D495/10 , A61K31/541 , C07D413/02 , C07D417/02 , C07
CPC分类号: C07D215/227 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D491/04 , C07D495/10
摘要: The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
摘要翻译: 本发明涉及通式I的化合物及其药学上可接受的盐,其可用作黑色素浓缩激素受体拮抗剂,特别是MCH-1R拮抗剂。 因此,本发明的化合物可用于治疗或预防与食物过量摄取及其并发症,骨关节炎,某些癌症,艾滋病消瘦,恶病质,虚弱(特别是老年人)相关的肥胖或进食障碍,精神障碍压力, 认知障碍,性功能,生殖功能,肾功能,运动障碍,注意力缺陷障碍(ADD),药物滥用障碍和运动障碍,亨廷顿病,癫痫,记忆功能和脊髓性肌肉萎缩。 因此,式I化合物可用于治疗这些病症,以及制备用于治疗这些病症的药物。 作为制备这些化合物的方法,公开了包含式(I)化合物之一作为活性成分的药物制剂。
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公开(公告)号:US20050009815A1
公开(公告)日:2005-01-13
申请号:US10496614
申请日:2002-11-22
申请人: Robert DeVita , Lehua Chang , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas Sailer
发明人: Robert DeVita , Lehua Chang , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas Sailer
IPC分类号: A61K31/4706 , A61K31/4709 , A61K31/473 , A61K31/496 , A61K31/519 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/02 , A61P13/12 , A61P15/00 , A61P19/02 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , A61P25/30 , A61P31/18 , A61P35/00 , A61P43/00 , C07D215/42 , C07D215/48 , C07D219/10 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/04 , C07D487/04 , C07D521/00 , C07F7/22 , A61K31/541 , A61K31/5377
CPC分类号: C07D231/12 , C07D215/42 , C07D219/10 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/04 , C07D487/04 , C07F7/2208
摘要: The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
摘要翻译: 本发明涉及通式I的化合物及其药学上可接受的盐,其可用作黑色素浓缩激素受体拮抗剂,特别是MCH-1R拮抗剂。 因此,本发明的化合物可用于治疗或预防与食物过量摄取及其并发症,骨关节炎,某些癌症,艾滋病消瘦,恶病质,虚弱(特别是老年人)相关的肥胖或进食障碍,精神障碍压力, 认知障碍,性功能,生殖功能,肾功能,运动障碍,注意力缺陷障碍(ADD),药物滥用障碍和运动障碍,亨廷顿病,癫痫,记忆功能和脊髓性肌肉萎缩。 因此,式I化合物可用于治疗这些病症,以及制备用于治疗这些病症的药物。 作为制备这些化合物的方法,公开了包含式(I)化合物之一作为活性成分的药物制剂。
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公开(公告)号:US08785634B2
公开(公告)日:2014-07-22
申请号:US13638976
申请日:2011-04-21
申请人: Fa-Xiang Ding , JinLong Jiang , Dong-Ming Shen , Hong Shen , Zhi-Cai Shi
发明人: Fa-Xiang Ding , JinLong Jiang , Dong-Ming Shen , Hong Shen , Zhi-Cai Shi
IPC分类号: C07D401/00
CPC分类号: C07D491/20 , C07D491/10
摘要: Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
摘要翻译: 结构式(I)的化合物是脯氨酰羧肽酶(PrCP)的抑制剂。 本发明的化合物可用于预防和治疗与PrCP的酶活性相关的病症,例如异常代谢,包括肥胖症; 糖尿病; 代谢综合征; 肥胖相关疾病; 和糖尿病相关疾病。
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