US 7,511,061 B2
Triazoles as farnesyl transferase inhibitors
Ashis Kumar Saha, Harleysville, Pa. (US); David William End, Ambler, Pa. (US); Bart Lieven Daniel De Corte, Southampton, Pa. (US); Henry Joseph Breslin, Lansdale, Pa. (US); and Li Liu, Doylestown, Pa. (US)
Assigned to Janssen Pharmaceutica N.V., Beerse (Belgium)
Filed on Jun. 02, 2005, as Appl. No. 11/143,814.
Application 11/143814 is a division of application No. 10/130322, previously published as PCT/EP00/11393, filed on Nov. 15, 2000.
Claims priority of provisional application 60/165434, filed on Nov. 15, 1999.
Prior Publication US 2005/0234117 A1, Oct. 20, 2005
Int. Cl. A61K 31/4196 (2006.01); A61K 31/47 (2006.01); C07D 215/00 (2006.01); C07D 249/06 (2006.01)
U.S. Cl. 514—311  [546/112; 546/152; 546/169; 548/262.2; 548/267.6; 514/383] 12 Claims
 
1. A compound of formula

OG Complex Work Unit Drawing
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- is a radical of formula
═N—N═CH— (a-1),
═N—CH═N— (a-2), or
═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 a substituted or unsubstituted C1-14heterocycle, or C1-12alkyl substituted with one or more substituents independently selected from a substituted or unsubstituted C1-14heterocycle;
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; and
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.