发明公开
EP1214075A1 POLYMORPHS OF N-METHYL-N-(3- 3- 2-THIENYLCARBONYL]-PYRAZOL- 1,5-$g(a)]-PYRIMIDIN-7-YL PHENYL)ACETAMIDE AND COMPOSITIONS AND METHODS RELATED THERETO
有权
N-甲基-N-（3-（2-噻吩羰基）吡唑并[1,5-a]嘧啶-7-基苯基）乙酰胺和组合物以及方法相关的多晶型
- 专利标题： POLYMORPHS OF N-METHYL-N-(3- 3- 2-THIENYLCARBONYL]-PYRAZOL- 1,5-$g(a)]-PYRIMIDIN-7-YL PHENYL)ACETAMIDE AND COMPOSITIONS AND METHODS RELATED THERETO
- 专利标题（中）： N-甲基-N-（3-（2-噻吩羰基）吡唑并[1,5-a]嘧啶-7-基苯基）乙酰胺和组合物以及方法相关的多晶型
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申请号： EP00957941.8申请日： 2000-09-01
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公开(公告)号： EP1214075A1公开(公告)日： 2002-06-19
- 发明人: THIELE, William, J. , O'DONNELL, Patrick, B.
- 申请人： Neurocrine Biosciences, Inc.
- 申请人地址： 10555 Science Center Drive San Diego, CA 92121-1102 US
- 专利权人： Neurocrine Biosciences, Inc.
- 当前专利权人： Neurocrine Biosciences, Inc.
- 当前专利权人地址： 10555 Science Center Drive San Diego, CA 92121-1102 US
- 代理机构： Grünecker, Kinkeldey, Stockmair & SchwanhäusserAnwaltssozietät
- 优先权： US389524 19990902; US421620 19991019
- 国际公布： WO0115700 20010308
- 主分类号： A61K31/519
- IPC分类号： A61K31/519 ; C07D487/02
摘要：
Polymorphs of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide (Compound (1)), and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Processes for making the same, as well as related compositions and methods are also disclosed, particularly with regard to treatment of insomnia. A polymorph Form (I) possessing exception physical and heat stability is provided. A polymorph Form II.
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