发明名称 |
Esters of (+)-alpha-( 2,3- dimethoxyphenyl) -1-(2-(4- fluorophenyl) ethyl)-4- piperidinemethanol and their use as prodrugs of the 5HT2A receptor antagonist MDL 110,907 |
摘要 |
Esters of (2,3-dimethoxy-phenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol (MDL 100907) (I), are new. Esters of (+)-alpha-(2,3-dimethoxy- phenyl)-1-[2(4-fluorophenyl)ethyl]-4-piperidine methanol of formula (I) and their stereoisomers and salts are new. [Image] R : 4-20C alkyl. ACTIVITY : Neuroleptic; Antimanic; Antidepressant; Tranquilizer; Antiaddictive; Cardiant; Antianginal; Thrombolytic; Eating-Disorders-Gen.; Vasotropic; Antiarrhythmic; Sedative. (+)-alpha-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl(ethyl]-4- piperidine methanol decanoate (120 mg/kg equivalent to MDL-100907) was administered to (+/-)-DOI HCl injected male Sprague-Dawley rats. (+/-)-DOI HCl induces several quantifiable behaviours in rats. Significantly antagonized DOI-induced behavior in the rats was observed for a full 28 days. The effect was no longer significant at day 40. MECHANISM OF ACTION : Antiserotonin-2A. |
申请公布号 |
AU1083099(A) |
申请公布日期 |
2000.05.01 |
申请号 |
AU19990010830 |
申请日期 |
1998.10.14 |
申请人 |
AVENTIS PHARMACEUTICALS INC. |
发明人 |
ALBERT A. CARR;LUC E. VAN HIJFTE;RAYMOND W. KOSLEY |
分类号 |
C07D211/48;A61K;A61K31/445;A61P7/02;A61P9/06;A61P9/10;A61P25/00;A61P25/18;A61P25/22;A61P25/24;A61P25/30;C07D;C07D211/22 |
主分类号 |
C07D211/48 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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