Arylalkanoyl derivatives, processes for their preparation,...

C - Chemistry – Metallurgy – 07 – C

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Details

C07C 279/14 (2006.01) A61K 31/16 (2006.01) A61P 7/02 (2006.01) C07C 257/16 (2006.01) C07D 211/26 (2006.01) C07D 213/56 (2006.01)

Patent

CA 2358581

The present invention relates to new compounds for the inhibition of blood clotting proteins, and more particularly, to arylalkanoyl derivatives of formula (I), wherein R(1), R(2), R(3), R(4), R(5), R(6a) and R(6b) have the meanings indicated in the claims. The compounds of formula (1) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula (I) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, to and the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I) in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and auxiliary substances.

L'invention porte sur de nouveaux composés inhibiteurs des protéines de coagulation du sang et plus particulièrement de dérivés d'arylalkanoyl de formule (I), dans laquelle R(1), R(2), R(3), R(4), R(5), R(6a) et R(6b) ont la signification indiquée dans les revendications, lesdits composés étant des inhibiteurs du facteur Xa de l'enzyme de coagulation. L'invention porte également sur le procédé de préparation des composés de formule (I), sur des méthodes d'inhibition de l'activité du facteur Xa et de la coagulation et sur l'utilisation desdits composés pour le traitement et la prophylaxie de maladies pouvant être traitées ou prévenues par l'inhibition de l'activité du facteur Xa telles que les maladies thromboemboliques, et sur l'utilisation desdits composés pour la préparation de médicaments s'appliquant à ces maladies. L'invention porte en outre sur des compositions contenant le composé de formule (I) mélangé ou associé à un excipient inerte, et en particulier sur des préparations pharmaceutiques contenant le composé de formule (I), des substances pharmacocompatibles et des substances auxiliaires.

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