C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/06 (2006.01) A61K 31/47 (2006.01) C07D 455/04 (2006.01) C07D 498/06 (2006.01)
Patent
CA 2283587
This invention concerns compounds of formula (I), the pharmaceutically acceptable acid additions salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; -A- is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1- 6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar-C1-6alkyl, Ar-oxy, Ar-C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar- oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy; or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyl; R6 hydrogen, hydroxy, halo cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar; or a radical of formula -O-R7, -S-R8, -N-R8R9; and Ar is optionally substituted phenyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
L'invention concerne des composés de formule (I), leurs sels d'addition acides pharmaceutiquement acceptables et leurs formes stéréo-isomères, où la ligne en pointillé représente une liaison facultative; X désigne oxygène ou soufre; -A- est un radical bivalent de formule; R<1> et R<2> sont chacun indépendamment hydrogène, hydroxy, halo, cyano, alkyle C1-6, trihalométhyle, trihalométhoxy, alcényle C2-6, alkyloxy C1-6, hydroxyalkyloxy C1-6, alkyloxyC1-6alkyloxy C1-6, alkyloxycarbonyle C1-6, aminoalkyloxy C1-6, mono ou di(alkyle C1-6)amino alkyloxy C1-6, Ar, Ar-alkyle C1-6, Ar-oxy, Ar-alkyloxy C1-6; ou R1-R2, lorsqu'ils sont adjacents et pris ensemble, peuvent former un radical bivalent; R3 et R4 désignent chacun indépendamment hydrogène, halo, cyano, alkyle C1-6, alkyloxy C1-6, Ar-oxy, alkylthio C1-6, di(C1-6alkyl)amino, trihalométhyle, trihalométhoxy; ou R<3> et R<4>, lorsqu'ils sont adjacents et pris ensemble, peuvent former un radical bivalent; R<5> est un imidazolyle substitué par un hydrogène ou alkyle C1-6; R<6> désigne hydrogène, hydroxy, halo, cyano, éventuellement alkyle C1-6 substitué, alkyloxycarbonyle C1-6 ou Ar; ou un radical de la formule -O-R<7>, -S-R<8>, -N-R<8>R<9>; et Ar désigne éventuellement phényle substitué. Lesdits composés ont une activité inhibant la transférase farnésyle. L'invention concerne aussi leur préparation, les compositions les contenant et leur utilisation en tant que médicament.
Angibaud Patrick Rene
Ligny Yannick Aime Eddy
Poncelet Virginie Sophie
Sanz Gerard Charles
Venet Marc Gaston
Gowling Lafleur Henderson Llp
Janssen Pharmaceutica N.v.
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