Farnesyl transferase inhibiting 2-quinolone derivatives

Details Farnesyl transferase inhibiting 2-quinolone derivatives Farnesyl transferase inhibiting 2-quinolone derivatives

C - Chemistry, Metallurgy

07

D

C07D 401/06 (2006.01) A61K 31/47 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2231143

The present invention is concerned with compounds of formula (I), the stereoisomeric forms thereof and the pharmaceutically acceptable acid or base addition salts thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 is hydrogen, C1-12alkyl, Ar1, Ar2C1-6alkyl, quinolinylC1-6alkyl, pyridylC1- 6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di (C1-6alkyl)-aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula -Alk1- C(=O)-R9, -Alk1-S(O)-R9 or -Alk1-S(O)2-R9; R2 and R3 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxy-C1-6alkyloxy, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar1, Ar2C1-6alkyl, Ar2oxy, Ar2C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; or when on adjacent positions R2 and R3 taken together may form a bivalent radical; R4 and R5 each independently are hydrogen, Ar1, C1-6alkyl, C1-6alkyloxy-C1- 6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1-6alkylS(O)2-C1-6alkyl; R6 and R7 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy or Ar2oxy; R8 is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1- 6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl, cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, hydroxycarbonyl-C1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono-or di(C1-6alkyl)aminoC1-6alkyl, haloC1-6alkyl, C1-6alkyloxy-C1-6alkyl, aminocarbonylC1-6alkyl, Ar1, Ar2C1- 6alkyloxyC1-6alkyl, C1-6alkylthioC1-6alkyl; R10 is hydrogen C1-6alkyl or halo; R11 is hydrogen or C1-6alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

La présente invention concerne des composés de la formule (I), des formes stéréo-isomères de ceux-ci, ainsi que des sels d'addition de base ou d'acide de ceux-ci, acceptables sur le plan pharmacologique. Dans cette formule, les lignes en pointillé représentent une liaison facultative, X représente oxygène ou soufre, R<1> représente hydrogène, alkyle C1-12, Ar<1>, Ar<2>alkyle C1-6, quinolinyl-alkyle C1-6, pyridyl-alkyle C1-6, hydroxy-alkyle C1-6, alkyloxy C1-6-alkyle C1-6, mono ou di(alkyle C1-6)-amino-alkyle C1-6, amino-alkyle C1-6, ou un radical de la formule -Alk<1>-C(=O)-R<9>, -Alk<1>-S(O)-R<9>, ou -Alk<1>-S(O)2-R<9>, R<2> et R<3> représentent chacun indépendamment hydrogène, hydroxy, halo, cyano, alkyle C1-6, alkyloxy C1-6, hydroxy-alkyloxy C1-6, alkyloxy C1-6-alkyloxy C1-6, amino-alkyloxy C1-6, mono ou di(alkyle C1-6)amino-alkyloxy C1-6, Ar<1>, Ar<2>alkyle C1-6, Ar<2>oxy, Ar<2>alkyloxy C1-6, hydroxycarbonyle, alkyloxycarbonyle C1-6, trihalométhyle, trihalométhoxy, alcényle C2-6, ou bien lorsque R<2> et R<3> sont dans des positions adjacentes, pris ensemble, ils peuvent former un radical bivalent, R<4> et R<5> représentent chacun indépendamment hydrogène, Ar<1>, alkyle C1-6, alkyloxyC1-6-alkyle C1-6, alkyloxy C1-6, alkylthio C1-6, amino, hydroxycarbonyle, alkyloxy C1-6-carbonyle, alkyle C1-6S(O)alkyle C1-6 ou alkyle C1-6S(O)2-alkyle C1-6, R<6> et R<7> représentent chacun indépendamment hydrogène, halo, cyano, alkyle C1-6, alkyloxy C1-6 ou Ar<2>oxy, R<8> représente hydrogène, alkyle C1-6, cyano, hydroxycarbonyle, alkyloxycarbonyle C1-6, alkyle C1-6-carbonyl-alkyle C1-6,cyano-alkyle C1-6, alkyloxy C1-6-carbonyl-alkyle C1-6, hydroxycarbonyl-alkyle C1-6, hydroxy-alkyle C1-6, amino-alkyle C1-6, mono ou di(alkyle C1-6)amino-alkyle C1-6, halo-alkyle C1-6, alkyloxy C1-6-alkyle C1-6, aminocarbonyle-alkyle C1-6, Ar<1>, Ar<2>alkyloxy C1-6-alkyle C1-6, alkylthio C1-6-alkyle C1-6, R<10> représente hydrogène, alkyle C1-6 ou halo, R<11> représente hydrogène ou alkyle C1-6. Ces composés possèdent une activité inhibitrice de la farnésyle transférase. On décrit également la préparation de ces composés, des compositions les contenant ainsi que leur utilisation en tant que médicament.

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