| abstract |
Tricyclic amide and urea derivatives useful in inhibiting G-protein function and treating proliferative diseases are pharmaceutical compositions containing the compounds. In the general formula of tricyclic amide and urea derivatives and their pharmaceutically acceptable salts and gravels (1.0), a, b, c and d are one of the nitrogen atoms or NR9, of which R9 is -OQ, methyl or other (- CH2) nCOOH, n1, 2 or 3, or CR2; or a, b, c and d are each CR1 or CR2; R1 and R2 are hydrogen, fish gene, trifluoromethyl, -OR10, -COR10, -SR10 or -S (O) tR11, a - of which t is 0, 1 or 2, - thiocyanate, -N (R10 ) 2, -NR10R11, nitro, -OC (O) R10, -CO2R10, -OCO2R11, cyano, -NHC (O) R10, -NHSO2R10, -CONHR10, (2-hydroxyethyl) carbamoyl, - NR10COOR11, a tube of formula (a), -SR11C (O) OR11, -SR11N (R75) 2 - of which R75 is hydrogen and -C (O) OR11-, benztriazol-1-yl-oxy-tube, optionally substituted 5-tetrazolyl. -piperine, alkynyl, optionally substituted alkenyl or alkyl; R3 and R4 are hydrogen or any of the substituents defined in R1 and R2, or R3 and R4 together form a coded ring; R5, R6, R7 and R8 are hydrogen, trifluoromethyl, -COR10, optionally substituted, or one of R5, R6, R7 and R8, together with R40 as defined in R, is optionally substituted - (CH2) r-. a value of 1, 2, 3 or 4, - or R5 and R6 together form an oxo or teak tube and / or R7 and R8 together form an ox or tube tube; R10 is hydrogen, alkyl, aryl or aralkyl; R11 is alkyl or aryl; X is a nitrogen atom, a methylpiper or a carbon atom attached to carbon 11 by a double bond; My fish gene A and B, nitro, -R10, -OR11, -OCO2R11 or -OC (O) R10, if there is a double bond between carbon atoms 5 and 6, or A and B have two hydrogen atoms, two - (OR11) 2, one hydrogen and one fish gene, two fish gene, one alkyl tube and one hydrogen gene, two alkyl tubes, one hydrogen gene and one -OC (O) R10, single hydrogen and one -OR a tube or -O- (CH2) pO-, of which p is 2, 3 or 4, when the 5 to 6 carbon atoms represent a single bond; R is as defined herein; R40, R42, R44 or R54 and Z means oxygen or sulfur. ŕ |