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公开(公告)号:US6159975A
公开(公告)日:2000-12-12
申请号:US247240
申请日:1999-02-10
IPC分类号: C07D519/00 , C07D401/12 , A61K31/407 , C07D215/06 , C07D471/04 , C07D487/06
CPC分类号: C07D519/00
摘要: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
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2.
公开(公告)号:US07015235B2
公开(公告)日:2006-03-21
申请号:US10468515
申请日:2002-02-25
申请人: Mark T. Goulet , Ravi P. Nargund , Iyassu K. Sebhat , Feroze Ujjainwalla , Thomas F. Walsh , Daniel Warner , Zhixiong Ye , Jonathan R. Young , Raman K. Bakshi
发明人: Mark T. Goulet , Ravi P. Nargund , Iyassu K. Sebhat , Feroze Ujjainwalla , Thomas F. Walsh , Daniel Warner , Zhixiong Ye , Jonathan R. Young , Raman K. Bakshi
IPC分类号: A61K31/445 , C07D211/06
CPC分类号: C07D491/08 , A61K31/445 , C07D211/62 , C07D211/64 , C07D401/06 , C07D401/14 , C07D413/06 , C07D413/14
摘要: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
摘要翻译: 某些新的4-取代N-酰化哌啶衍生物是人黑皮质素受体的激动剂,特别是人黑皮质素-4受体(MC-4R)的选择性激动剂。 因此,它们可用于治疗,控制或预防对MC-4R的活化反应的疾病和病症,例如肥胖,糖尿病,性功能障碍,包括勃起功能障碍和女性性功能障碍。
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公开(公告)号:US6110931A
公开(公告)日:2000-08-29
申请号:US276028
申请日:1999-03-25
IPC分类号: A61P5/02 , C07D519/00 , A61K31/437 , A61K31/4375 , C07D471/04 , C07D487/04
CPC分类号: C07D519/00
摘要: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
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公开(公告)号:US6025366A
公开(公告)日:2000-02-15
申请号:US275754
申请日:1999-03-25
IPC分类号: C07D471/04 , C07D519/00 , A61K31/435
CPC分类号: C07D471/04
摘要: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
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公开(公告)号:US07091216B2
公开(公告)日:2006-08-15
申请号:US10521821
申请日:2003-08-01
申请人: Richard B. Toupence , John S. Debenham , Mark T. Goulet , Christina B. Madsen-Duggan , Thomas F. Walsh , Shrenik K. Shah
发明人: Richard B. Toupence , John S. Debenham , Mark T. Goulet , Christina B. Madsen-Duggan , Thomas F. Walsh , Shrenik K. Shah
IPC分类号: A61K31/44 , C07D409/02
CPC分类号: C07D491/04 , C07D453/06
摘要: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译: 结构式(I)的新型化合物是大麻素-1(CB1)受体的拮抗剂和/或反向激动剂,可用于治疗,预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病,记忆缺陷,认知障碍,偏头痛,神经病,包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症,脑血管 事故和头部创伤,焦虑症,压力,癫痫,帕金森病,运动障碍和精神分裂症。 这些化合物还可用于治疗药物滥用障碍,治疗肥胖或进食障碍,以及治疗哮喘,便秘,慢性肠假性梗阻和肝硬化。
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公开(公告)号:US06228867B1
公开(公告)日:2001-05-08
申请号:US09275951
申请日:1999-03-25
IPC分类号: A61K31345
CPC分类号: C07D519/00
摘要: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
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公开(公告)号:US6077847A
公开(公告)日:2000-06-20
申请号:US275950
申请日:1999-03-25
IPC分类号: C07D471/04 , A61K31/44
CPC分类号: C07D471/04
摘要: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
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公开(公告)号:US5985892A
公开(公告)日:1999-11-16
申请号:US275752
申请日:1999-03-25
IPC分类号: C07D471/04 , A61K31/435
CPC分类号: C07D471/04
摘要: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
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公开(公告)号:US07012084B2
公开(公告)日:2006-03-14
申请号:US10468517
申请日:2002-02-25
IPC分类号: A61K31/445 , C07D211/06
CPC分类号: C07D413/06 , C07D211/26 , C07D211/28 , C07D211/62 , C07D413/14
摘要: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
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公开(公告)号:US5998432A
公开(公告)日:1999-12-07
申请号:US276029
申请日:1999-03-25
IPC分类号: C07D519/00 , A61K31/435 , C07D471/04
CPC分类号: C07D519/00
摘要: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
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