| 摘要 |
PURPOSE:To provide a new pyridylthiazolidine N-oxide derivative having PAF antagonistic activity, useful as an anti-asthematic agent, anti-inflammatory agent, antineoplastic agent or a mitigative agent for shock symptoms. CONSTITUTION:The compound of formula I (R<1> is H or hydrocarbon; R<2> is H, carboxyl, etc.; R<3> is oxo group (=O), H, etc.; R<4> is H, lower alkyl, etc.; R<5> and R<6> are each H, hydrocarbon, etc.; R<7> is H, cyano, acyl, etc.; R<8> is of formula II; R<9> is Netc.; R<12> and R<13> are each H, of formula III, etc.; R<14> and R<15> are each H or hydrocarbon; R<16> is H, lower alkoxy, etc. ; R<17> and R<18> are each H, morpholinyl, etc.), e.g. 1-(3-methyl-3-phenylbutyl)-4-{[2-(1-oxide-3- pyridine)-4thiazolidinyl]carbonyl}piperazine fumaric acid salt 0.4 hydrate of formula IV. The compound of the formula IV can be obtained according to the routes in compliance with the reaction formulas beginning with a 2-(1- oxide-3-pyridyl)thiazolidine-4-carboxylic acid of formula V and 1-(3-methyl-3- phenylbutyl)piperazine of formula VI. |
