Carboxylic acid amides, the preparation thereof and their...

Details Carboxylic acid amides, the preparation thereof and their... Carboxylic acid amides, the preparation thereof and their...

C - Chemistry, Metallurgy

07

C

C07C 257/18 (2006.01) A61K 31/40 (2006.01) A61K 31/4164 (2006.01) A61P 7/02 (2006.01) C07C 311/21 (2006.01) C07C 311/46 (2006.01) C07D 207/12 (2006.01) C07D 233/54 (2006.01) C07D 295/12 (2006.01) C07D 295/135 (2006.01) C07D 295/18 (2006.01) C07D 295/185 (2006.01) C07D 295/192 (2006.01)

Patent

CA 2380986

The present invention relates to carboxylic acid amides of general formula (see formula I) wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof, the prodrugs and the salts thereof which have valuable properties. The compounds of the above general formula I wherein R5 denotes a cyano group are valuable intermediate products for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein R5 denotes one of the amidino groups mentioned in claim 1 have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.

L'invention concerne des amides d'acide carboxylique de formule générale (I), dans laquelle R1 à R5, Ar, m et n sont définis dans la revendication 1, leurs tautomères, leurs stéréo-isomères, leurs mélanges, leurs promédicaments et leurs sels, qui présentent des propriétés précieuses. Les composés de la formule (I) mentionnée ci-dessus, dans laquelle R5 représente un groupe cyano, constituent des intermédiaires précieux pour la production des autres composés de la formule (I). Les composés de ladite formule (I), dans laquelle R5 représente un des groupes amidino mentionnés dans la revendication 1, présentent des propriétés pharmacologiques précieuses, notamment un effet antithrombique et un effet inhibiteur du facteur Xa.

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