发明授权
EP1587789B1 SELECTIVE SEROTONIN 2A/2C RECEPTOR INVERSE AGONISTS AS THERAPEUTICS FOR NEURODEGENERATIVE DISEASES
有权
选择性血清素2A / 2C受体反相激动剂作为治疗神经退行性疾病
- 专利标题: SELECTIVE SEROTONIN 2A/2C RECEPTOR INVERSE AGONISTS AS THERAPEUTICS FOR NEURODEGENERATIVE DISEASES
- 专利标题(中): 选择性血清素2A / 2C受体反相激动剂作为治疗神经退行性疾病
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申请号: EP04702584.6申请日: 2004-01-15
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公开(公告)号: EP1587789B1公开(公告)日: 2008-09-03
- 发明人: WEINER, David, M. , DAVIS, Robert, E. , BRANN, Mark, R. , NASH, Norman , ANDERSSON , Carl - Magnus A. , ULDAM , Allan K.
- 申请人: Acadia Pharmaceuticals Inc.
- 申请人地址: 3911 Sorrento Valley Blvd. San Diego, CA 92121-1402 US
- 专利权人: Acadia Pharmaceuticals Inc.
- 当前专利权人: Acadia Pharmaceuticals Inc.
- 当前专利权人地址: 3911 Sorrento Valley Blvd. San Diego, CA 92121-1402 US
- 代理机构: Plougmann & Vingtoft A/S
- 优先权: US441406P 20030116; US479346P 20030617
- 国际公布: WO2004064738 20040805
- 主分类号: C07D211/06
- IPC分类号: C07D211/06 ; A61K31/4468 ; A61P25/14 ; A61P25/16 ; A61P25/18 ; A61P25/28 ; A61P25/24 ; A61P25/06
摘要:
Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
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