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1. (WO2001036395) TRIAZOLES AS FARNESYL TRANSFERASE INHIBITORS

Pub. No.:    WO/2001/036395    International Application No.:    PCT/EP2000/011393
Publication Date: Sat May 26 01:59:59 CEST 2001 International Filing Date: Thu Nov 16 00:59:59 CET 2000
IPC: C07D 249/08
C07D 401/12
C07D 401/14
C07D 403/12
C07D 405/12
C07D 405/14
Applicants: JANSSEN PHARMACEUTICA N.V.
SAHA, Ashis, Kumar
END, David, William
DE CORTE, Bart, Lieven, Daniel
BRESLIN, Henry, Joseph
LIU, Li
Inventors: SAHA, Ashis, Kumar
END, David, William
DE CORTE, Bart, Lieven, Daniel
BRESLIN, Henry, Joseph
LIU, Li
Title: TRIAZOLES AS FARNESYL TRANSFERASE INHIBITORS
Abstract:
Formula (I) a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric from thereof, wherein L?1 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 C¿1-14?heterocylce; =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 SO¿2?, (CH2)n wherein n is 1 to 4, C(=O), C(=S), or a direct bond; R?2¿ is aryl, C¿3-7?cycloalkyl, C3-7cycloalkyl, substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted 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 hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R?3¿ is aryl, -NR5R6, a substituted or unsubstituted C¿1-14?heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R?4¿ is hydrogen, aryl, C¿3-7?cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R?5 and R6¿ are each independently selected from hydrogen, a substituted or unsubstituted C¿1-14?heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl aryloxy or a substituted or unsubstituted C1-14heterocycle.