Novel farnesyl transferase inhibitors, preparation,...

C - Chemistry – Metallurgy – 07 – D

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C07D 495/08 (2006.01) A61K 31/40 (2006.01) C07D 209/00 (2006.01) C07D 209/44 (2006.01) C07D 333/00 (2006.01) C07D 403/04 (2006.01) C07D 409/04 (2006.01) C07D 471/08 (2006.01) C07D 487/08 (2006.01) C07D 491/08 (2006.01)

Patent

CA 2315144

The invention concerns novel products of general formula (I), their preparation, the pharmaceutical compositions containing them and their use for preparing medicines. (I) In the general formula (I): Het represents a monocyclic or polycyclic system, for which at least one of the cycles contain 1 to 4 heteroatoms; Ar represents an optionally substituted phenyl radical, a phenyl radical substituted for a heterocycle, a polycyclic or heterocyclic aromatic radical; R represents a -COOH, -COOR¿4?, -CON(R¿5?)(R¿6?) radical in which R¿4? = alkyl, R¿5? = H, alkyl, R¿6? = alkyl, hydrogen, hydroxy, amino optionally substituted, alkoxy; R¿1?, R¿2? = hydrogen, halogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl; R¿3? = hydrogen, alkyl, alkylthio; X = methylene, alken-1,1-diyl, cycloalkan-1,1-diyl; in racemic form or the optical isomers or mixtures of their optical isomers, and the salts of the product of general formula (I). The products of general formula (I) are farnesyl transferase inhibitors.

Nouveaux produits de formule générale (I), leur préparation, les compositions pharmaceutiques qui les contiennent et leur utilisation pour la préparation de médicaments. Dans la formule générale (I), Het représente un système mono- ou polycyclique, pour lequel au moins un des cycles contient 1 à 4 hétéroatomes; Ar représente un radical phényle éventuellement substitué, un radical phényle substitué à un hétérocycle, un radical aromatique polycyclique ou hétérocyclique; R représente un radical -COOH, -COOR4, -CON(R5)(R6) où R4 = alcoyle, R5 = H, alcoyle, R6 = alcoyle, hydrogène, hydroxy, amino éventuellement substitué, alcoxy; R1, R2 = hydrogène, halogène, alcoyle, alcoxy, alcoylthio, alcoxycarbonyle; R3 = hydrogène, alcoyle, alcoylthio; X = méthylène, alcèn-1,1-diyle, cycloalcan-1,1-diyle; sous forme racémique ou leurs isomères optiques ou les mélanges de leurs isomères optiques, ainsi que les sels du produit de formule générale (I). Les produits de formule générale (I) sont des inhibiteurs de farnésyle transférase.

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