1-(OMEGA-CARBOXYALKYL)-3-3 OR 4-(1-PHENYLALKOXY OR 1-PHENOXYALKYL)BENZOYLINDOLE DERIVATIVES HAVING STEROID 5ALPHA-REDUCTASE INHIBITORY ACTIVITY AND MEDICAMENTS

摘要

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X is O, NH, N(C1-C4 alkyl), C1-C4 alkylene, C2-C4 alkenylene or C2-C4 alkynylene, said alkylene, alkenylene and alkynylene groups being optionally substituted by C1-C4 alkyl or aryl; Y is C1-C6 alkylene optionally substituted by C1-C6 alkyl; R is H, OH, halo, C1-C4 alkyl or C1-C4 alkoxy; R1, R2, R3 and R4 are each independently selected from H, C1-C4 alkyl, C1-C4 alkoxy, OH, halo and CF3; one of R6, R7 and R8 is C1-C15 alkyl or a group of the formula -Z(C1-C15 alkyl), -Z(aryl) or -Z(C3-C7 cycloalkyl), said alkyl group being optionally interrupted by O, S(O)q, NH or N(C1-C6 alkyl), and said alkyl group and the alkyl group of said -Z(C1-C15 alkyl) group being optionally substituted by C1-C10 alkoxy, aryl, C3-C7 cycloalkyl or a group of the formula -Z(aryl), and the remainder of R6, R7 and R8 and R5 and R9 are each independently selected from H, C1-C4 alkyl, C1-C4 alkoxy, halo and halo(C1-C4 alkyl); R10 is COOH, COOR11 or CONR12R13; R11 is a biolabile ester-forming group; R12 and R13 are each independently selected from H and C1-C4 alkyl; Z is O, S(O)q, NH or N(C1-C6 alkyl); q is 0, 1 or 2; and ''aryl'' used in the definitions of X, R6, R7 and R8, means phenyl optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, OH, halo, CF3, halo(C1-C6 alkyl), nitro, amino, C2-C6 alkanamido, C2-C6 alkanoyl or phenyl: together with pharmaceutical compositions containing, processes for the preparation of and uses of, such compounds.