发明名称 TRIAZOLES AS FARNESYL TRANSFERASE INHIBITORS
摘要 Formula (I) a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric from thereof, wherein L1 and L2 are R1-Y-wherein each (R1-Y)- substituent is defined independently of the other; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocylce; =Z 1- 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 substitut ed or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1- 16alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1- 6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydrox y, 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 C 3- 7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are ea ch 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 CA2389280(A1) 申请公布日期 2001.05.25
申请号 CA20002389280 申请日期 2000.11.15
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 BRESLIN, HENRY JOSEPH;LIU, LI;DE CORTE, BART LIEVEN DANIEL;END, DAVID WILLIAM;SAHA, ASHIS KUMAR
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;(IPC1-7):C07D249/08;C07D409/12;C07D409/14;C07D417/14;A61K31/419;A61K31/443;A61K31/470 主分类号 A61K31/4196
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