Patent number: 6624157
Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas
and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof wherein:
r, s and t are 0 or 1;
m=0, 1, 2;
p is 0, 1 or 2;
X is selected from the group consisting of oxygen, hydrogen or R1, R2, R3;
Y is selected from the group consisting of CHR9, SO2, CO, CO2, O, NR10, SO2NR11 and CONR12;
R6, R7, R9, R10, R11, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, and R28 are selected from the group consisting of hydrogen, lower alkyl or substituted alkyl;
R4, R5 are selected from the group consisting of hydrogen, halo, nitro, cyano and U-R13;
R12 is selected from the group consisting of hydrogen, lower alkyl, aryl, substituted alkyl or aryl;
U is selected from the group consisting of sulfur, oxygen, NR14, CO, SO, SO2, CO2, NR15CO2, NR16CONR17, NR19SO2, NR19SO2NR20, SO2NR2
Type:
Grant
Filed:
January 26, 2001
Date of Patent:
September 23, 2003
Assignee:
Bristol-Myers Squibb Company
Inventor:
Charles Z. Ding