发明名称 |
4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY |
摘要 |
The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives having S configuration at the 4-position of their 4,5-dihydro pyrazole ring which are potent antagonists of the cannabis CB1-receptor.The compounds have the general formula (I) wherein- R and R1 are the same or different and represent 3-pyridyl or 4-pyridyl or phenyl which may be substituted with halogen or methoxy,- R2 and R3 are the same or different and represent hydrogen, alkyl (1-3 C) or dimethylamino- R4 represents phenyl which may be substituted with 1 or 2 substituents selected from the group halogen atoms, trifluoromethyl, methoxy and alkyl (1-3 C)and tautomers, prodrugs and salts thereof.These enantiomers are much more potent and selective antagonists of the cannabis CB1-receptor, than the other enantiomer.
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申请公布号 |
WO02076949(A1) |
申请公布日期 |
2002.10.03 |
申请号 |
WO2002EP03079 |
申请日期 |
2002.03.18 |
申请人 |
SOLVAY PHARMACEUTICALS B.V.;LANGE, JOSEPHUS, H.M.;KRUSE, CORNELIS, G;TIPKER, JACOBUS;HOOGENDOORN, JAN |
发明人 |
LANGE, JOSEPHUS, H.M.;KRUSE, CORNELIS, G;TIPKER, JACOBUS;HOOGENDOORN, JAN |
分类号 |
C07D231/06;A61K31/415;A61K31/4439;A61P1/00;A61P3/04;A61P9/10;A61P25/00;A61P25/04;A61P25/08;A61P25/14;A61P25/16;A61P25/18;A61P25/22;A61P25/24;A61P25/28;A61P43/00;C07D231/08;C07D401/04;(IPC1-7):C07D231/06 |
主分类号 |
C07D231/06 |
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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