1,2-annelated quinoline derivatives

Details 1,2-annelated quinoline derivatives 1,2-annelated quinoline derivatives

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/4365 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01) C07D 221/00 (2006.01) C07D 235/00 (2006.01) C07D 239/00 (2006.01) C07D 249/00 (2006.01) C07D 257/00 (2006.01) C07D 401/06 (2006.01) C07D 403/06 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2355717

This invention concerns compounds of formula (I), the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein -X1-X2-X3- is a trivalent radical; >Y1-Y2- is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R1 and R2 are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-4alkyloxycarbonyl, aminoC1- 6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1- 6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl; or two R1 or R2 on adjacent positions form together a bivalent radical; R3 is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkylthio-C1- 6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxy- carbonylC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C1-6alkylcarbonylC1-6alkyl, C1-6alkyloxycarbonyl, aryl, arylC1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, or a radical of formula -O-R10, -S-R10 or -NR11R12; R4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

L'invention concerne des composés correspondant à la formule (I), des sels d'addition d'acide et formes isomères stéréochimiques de ceux-ci, acceptables sur le plan pharmacologique. Dans cette formule, =X?1¿-X?2¿-X?3¿- représente un radical trivalent; ~Y?1¿-Y?2¿- représente un radical trivalent; r et s valent chacun indépendamment 0, 1, 2, 3, 4 ou 5; t vaut 0, 1, 2 ou 3; chaque R?1¿ et R?2¿ représentent indépendamment hydroxy, halo, cyano, alkyle C¿1-6?, trihalométhyle, trihalométhoxy, alcényle C¿2-6?, alkyloxy C¿1-6?, hydroxy-alkyloxy C¿1-6?, alkylthio C¿1-6?, alkyloxy C¿1-6?-alkyloxyC¿1-6?, alkyloxycarbonyle C¿1-6?, amino-alkyloxy C¿1-6?, mono- or di(alkylC¿1-6?)amino, mono- or di(alkylC¿1-6?)amino-alkyloxy C¿1-6?, aryle, aryl-alkyle C¿1-6?, aryloxy or aryl-alkyloxy C¿1-6?, hydroxycarbonyle, alkyloxycarbonyle C¿1-6?; ou bien deux R?1¿ ou R?2¿ situés sur des positions adjacentes forment ensemble un radical bivalent; R?3¿ représente hydrogène, halo, alkyle C¿1-6?, cyano, halo-alkyle C¿1-6?, hydroxy-alkyle C¿1-6?, cyano-alkyle C¿1-6?, amino-alkyle C¿1-6?, alkyloxy C¿1-6?-alkyle C¿1-6?, alkylthio C¿1-6?-alkyle C¿1-6?, aminocarbonyl-alkyle C¿1-6?, hydroxycarbonyle, hydroxycarbonyl-alkyle C¿1-6?, alkyloxycarbonylC¿1-6?-alkyle C¿1-6?, alkylcarbonylC¿1-6?-alkyle C¿1-6?, alkyloxycarbonyle C¿1-6?, aryle, aryl-alkyloxy C¿1-6?-alkyle C¿1-6?, mono- or di(alkylC¿1-6?)amino-alkyle C¿1-6?, ou un radical correspondant à la formule -O-R?10¿, -S-R?10¿ ou -NR?11¿R?12¿; R?4¿ représente un imidazolyle, éventuellement substitué, aryle représente phényle ou naphtalényle, éventuellement substitué. Ces composés possèdent une activité inhibitrice de la farnésyle transférase et de la géranylgéranyle transférase. L'invention concerne encore la préparation de ces compositions, des compositions les contenant, ainsi que l'utilisation de ces composés en tant que médicament.

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