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1,8-CYCLED N- OR C-BOUND IMIDAZOLE SUBSTITUTED DERIVATIVES OF QUINOLYNONE INHIBITING FARNESIL TRANSFERASE

机译:1,8循环的N或C键咪唑取代的喹诺酮类抑制芳烃转移酶衍生物

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.
机译:本发明涉及下式的化合物:药学上可接受的酸加成盐及其立体化学异构形式,其中虚线代表任选的键; X是氧或硫; -A-是式的二价基团; R 1和R 2各自独立地是氢,羟基,卤素,氰基,C 1-6烷基,三卤甲基,三卤甲氧基,C 2-6烯基,C 1-6烷氧基,羟基C 1-6烷氧基,C 1-6烷氧基C 1-6烷氧基,C 1-6烷氧基羰基,氨基C 1-6烷氧基,单-或二(C 1-6烷基)氨基C 1-6烷氧基,Ar,Ar-C 1-6烷基,Ar氧基,Ar-C 1-6烷氧基;或或者当在相邻的位置R1和R2上一起形成二价基团时; R 3和R 4各自独立地是氢,卤素,氰基,C 1-6烷基,C 1-6烷氧基,芳氧基,C 1-6烷硫基,二(C 1-6烷基)氨基,三卤代甲基,三卤代甲氧基,或者当在相邻位置R 3和R 4一起时可能形成二价基团; R5是被氢或C1-6烷基取代的咪唑基; R6为氢,羟基,卤素,氰基,任选取代的C1-6烷基,C1-6烷氧羰基或Ar;或式-O-R7,-S-R8,-N-R8R9的基团; Ar是任选取代的苯基;具有法呢基转移酶抑制活性;它们的制剂,含有它们的组合物及其作为药物的用途。

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