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nya pyridylderivat, year foereningar innehaollande laekemedel och foerfarande foer deras framstaellning

机译:新的吡啶基衍生物,含药用化合物的年化合物及其制备方法

摘要

The present invention relates to novel pyridyl derivatives of the general formula IMAGE in which R6 is a pyridine group which is optionally substituted in the 3- or 4-position by an alkyl group, and X, Y, A, n and R3 to R6, R7 and R8 are as defined in Claim 1, their enantiomers, and their cis- and trans-isomers, if R4 and R5 together represent a carbon-carbon bond, which derivatives have useful properties. The compounds of the above general formula I, in which R7 represents a cyano group and Y represents an alkoxy, phenoxy, alkylthio of phenylthio group, are intermediates and the other compounds have useful pharmacological properties, in particular antithrombotic effects, and at the same time the novel compounds are additionally thromboxane antagonists (TRA) and thromboxane synthesis inhibitors (TSI) and thus also inhibit the effects mediated by thromboxane. Further, these compounds also have an effect on PGE2 production in the lung and on PGD2, PGE2 and PGF2 alpha production in human platelets.
机译:本发明涉及通式的新型吡啶基衍生物,其中R6是吡啶基,其任选地在3-或4-位被烷基取代,并且X,Y,A,n和R3被取代。如果R4和R5一起代表碳-碳键,则R6,R7和R8如权利要求1所定义,它们的对映异构体以及它们的顺式和反式异构体,这些衍生物具有有用的性质。上述通式I的化合物是中间体,其中R 7代表氰基,Y代表苯硫基的烷氧基,苯氧基,烷硫基,它们是中间体,其他化合物同时具有有用的药理性质,特别是抗血栓形成作用该新型化合物另外是血栓烷拮抗剂(TRA)和血栓烷合成抑制剂(TSI),因此也抑制了血栓烷介导的作用。此外,这些化合物还影响肺中PGE 2的产生以及人血小板中PGD 2,PGE 2和PGF 2α的产生。

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