Carbostyril derivatives as antithrombotic agents

Details Carbostyril derivatives as antithrombotic agents Carbostyril derivatives as antithrombotic agents

C - Chemistry, Metallurgy

07

D

C07D 215/22 (2006.01) A61K 31/47 (2006.01) C07D 215/227 (2006.01) C07D 215/26 (2006.01)

Patent

CA 2207185

The present invention is directed to a carbostyril derivative of the formula (1): Image wherein A is lower alkylene, R is H, halogen or lower alkoxy, R1 and R2 are each lower alkyl unsubstituted or substituted by OH, lower alkoxy, phenyl-lower alkoxy or lower alkanoyloxy; cycloalkyl unsubstituted or substituted by OH, hydroxy-lower alkoxy or lower alkanoyloxy; or amino unsubstituted or substituted by lower alkyl or cycloalkyl, R3 is H, lower alkyl, lower alkenyl or hydroxy-lower alkyl, and the bond between 3- and 4-positions of the carbostyril nucleus is single or double, provided that when R and R3 are H, R1 and R2 should not be either unsubstituted lower alkyl or unsubstituted cycloalkyl, or a salt thereof. The carbostyril derivatives of the present invention show antithrombotic activities, intima thickening inhibitory activity, the platelet mass dissociating activity and increasing activity of blood flow in the brain and the peripheral vessel, and hence, are useful as medicines in the prophylaxis or treatment of various ischemic diseases.

La présente invention concerne un dérivé de carbostyryle de formule (1), dans laquelle A est un alkylène inférieur, R est H, halogène ou un alcoxy inférieur, R<1> et R<2> sont chacun un alkyle inférieur, éventuellement substitué par OH, un alcoxy inférieur, un phényle-alcoxy inférieur ou un alcanoyloxy inférieur; le cycloalkyle est facultativement substitué par OH, un hydroxy-alcoxy inférieur ou un alcanoyloxy inférieur; ou l'amino est facultativement substitué par un alkyle inférieur ou un cycloalkyle; R<3> est H, un alkyle inférieur, un alkényle inférieur ou un hydroxy-alkyle inférieur, et la liaison entre les positions 3 et 4 du noyau de carbostyryle est simple ou double, à condition que, quand R et R<3> sont H, R<1> et R<2> ne soient pas soit un alkyle inférieur non substitué, soit un cycloalkyle non substitué ou un sel d'un de ces composés. Le dérivé selon l'invention manifeste des propriétés antithrombotiques, inhibitrices de l'épaississement de l'intima, de dissociation des amas de plaquettes et d'accroissement du débit sanguin dans le cerveau et dans les vaisseaux périphériques. Par conséquent, il est utile comme médicament dans la prophylaxie ou le traitement de diverses affections ischémiques.

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