Substituted aryl and heteroaryl derivatives, the preparation...

Details Substituted aryl and heteroaryl derivatives, the preparation... Substituted aryl and heteroaryl derivatives, the preparation...

C - Chemistry, Metallurgy

07

D

C07D 207/24 (2006.01) A61K 31/165 (2006.01) A61K 31/40 (2006.01) C07C 233/88 (2006.01) C07C 235/68 (2006.01) C07C 257/18 (2006.01) C07C 311/37 (2006.01) C07D 207/20 (2006.01) C07D 295/192 (2006.01)

Patent

CA 2445571

The present invention relates to new substituted aryl and heteroaryl derivatives of general formula Image wherein A, Ar, n, X, Y1, Y2, Y3, Y4, R1 and R5 are defined as in claim 1, the prodrugs, the tautomers, stereoisomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable properties. Thus, the compounds of the above general formula I wherein R5 does not contain a cyano group have, in particular, an antithrombotic effect and a selective factor Xa-inhibiting effect with generally improved compatibility. The compounds of the above general formula I wherein R5 contains a cyano group are valuable intermediate products for preparing the antithrombotic compounds of general formula I.

La présente invention concerne de nouveaux dérivés aryle et hétéroaryle substitués de formule générale (I), dans laquelle A, Ar, n, X, Y1, Y2, Y3, Y4, R1 et R5 sont tels que définis dans la revendication 1, ainsi que des promédicaments, des tautomères, des stéréo-isomères, des mélanges et des sels de ces composés, en particulier des sels physiologiquement tolérables de ces composés contenant des acides ou des bases inorganiques ou organiques, lesdits composés possédant des propriétés utiles. Les composés de formule générale (I) dans lesquels R5 ne contient aucun groupe cyano possèdent en particulier une action antithrombotique et une action inhibitrice sélective sur le facteur Xa, avec une compatibilité généralement accrue. Les composés de formule générale (I) dans lesquels R5 contient un groupe cyano constituent des intermédiaires utiles pour produire des composés antithrombotiques de formule générale (I).

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