发明授权
US08236806B2 Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same
有权
哌嗪基 - 丙基 - 吡唑衍生物作为多巴胺D4受体拮抗剂，以及含有它们的药物组合物
- 专利标题： Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same
- 专利标题（中）： 哌嗪基 - 丙基 - 吡唑衍生物作为多巴胺D4受体拮抗剂，以及含有它们的药物组合物
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申请号： US12530312申请日： 2007-07-13
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公开(公告)号： US08236806B2公开(公告)日： 2012-08-07
- 发明人: Jae Yang Kong , Woo-Kyu Park , Heeyeong Cho , Daeyoung Jeong , Gildon Choi , Hun Yeong Koh , Sang Hee Kim , Ae Nim Pae , Yong Seo Cho , Joo Hwan Cha , Hyunah Choo , Sang Eun Chae , Hee-Yoon Lee
- 申请人： Jae Yang Kong , Woo-Kyu Park , Heeyeong Cho , Daeyoung Jeong , Gildon Choi , Hun Yeong Koh , Sang Hee Kim , Ae Nim Pae , Yong Seo Cho , Joo Hwan Cha , Hyunah Choo , Sang Eun Chae , Hee-Yoon Lee
- 申请人地址： KR Daejeon
- 专利权人： Korea Research Institute of Chemical Technology
- 当前专利权人： Korea Research Institute of Chemical Technology
- 当前专利权人地址： KR Daejeon
- 代理机构： Lowe Hauptman Ham & Berner, LLP
- 优先权： KR10-2007-0022845 20070308
- 国际申请： PCT/KR2007/003415 WO 20070713
- 国际公布： WO2008/108517 WO 20080912
- 主分类号： A61K31/496
- IPC分类号： A61K31/496 ; C07D231/12 ; C07D401/04 ; C07D409/04
摘要：
The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.
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