发明名称 Farnesyltransferase-inhiberende 1,8-annelerte kinolinonderivater substituert med N- eller C-bundede imidazoler
摘要 This invention concerns compounds of formulathe pharmaceutically acceptable acid addition 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.
申请公布号 NO313143(B1) 申请公布日期 2002.08.19
申请号 NO19990004268 申请日期 1999.09.02
申请人 JANSSEN PHARMACEUTICA NV 发明人 VENET, MARC GASTON;ANGIBAUD, PATRICK RENE;LIGNY, YANNICK AIME EDDY;PONCELET, VIRGINIE SOPHIE;SANZ, GERARD CHARLES
分类号 C07D215/06;A61K31/47;A61K31/4704;A61K31/4709;A61K31/4741;A61K31/4745;A61K31/5383;A61P35/00;C07D401/10;C07D401/14;C07D455/04;C07D471/04;C07D471/06;C07D491/048;C07D491/052;C07D498/04;C07D498/06 主分类号 C07D215/06
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