发明名称 Triazoles as farnesyl transferase inhibitors
摘要 A prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1-Y- wherein each (R1-Y)- substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(-O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; =Z1-Z2=Z3- represents a radical of formula -N-N-CH- (a-1), -N-CH-N- (a-2), -CH-N-N- (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(-O), C(-S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, -NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.
申请公布号 AU2506301(A) 申请公布日期 2001.05.30
申请号 AU20010025063 申请日期 2000.11.15
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 ASHIS KUMAR SAHA;DAVID WILLIAM END;BART LIEVEN DANIEL DE CORTE;HENRY JOSEPH BRESLIN;LI LIU
分类号 A61K31/4196;A61K31/4439;A61K31/4709;A61K31/506;A61P1/00;A61P1/18;A61P11/00;A61P13/10;A61P13/12;A61P17/00;A61P31/12;A61P35/00;A61P35/02;A61P43/00;C07D249/08;C07D401/06;C07D401/12;C07D401/14;C07D403/12;C07D405/12;C07D405/14 主分类号 A61K31/4196
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