UNSATURATED 17β-SUBSTITUTED 3-CARBOXY STEROIDS

摘要

The present invention concerns steroidic 5α-reductase inhibitors having formula (I), wherein Y is oxygen or sulphur; R is a group: a) -OR4, wherein R4 is hydrogen or a C1-C6 alkyl group; b) (1), wherein each of R5 and R6, independently, is hydrogen or a C1-C6 alkyl group; c) (2), wherein R7 is hydrogen or a C1-C6 alkyl group and W is a group: (i) (3), wherein R8 is a C1-C6 alkyl group, a C5-C6 cycloalkyl group, a C6-C9 cycloalkylalkyl group, a phenyl group or a benzyl group; or (ii) (4), wherein R9 is a C1-C6 alkyl group or a C5-C6 cycloalkyl group; or (iii) (5), wherein R5 and R6 are as defined above; (d) (6), wherein each of R10 and R11 is, independently, hydrogen or a C1-C6 alkyl group or taken together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen, and n is an integer of 2 to 4; R1 is hydrogen, a C1-C6 alkyl group, a C5-C6 cycloalkyl group, a C6-C9 cycloalkylalkyl group or an aryl group; each of R2 and R3 is, independently, selected from the group consisting of hydrogen, C1-C6 alkyl, C5-C6 cycloalkyl, C6-C9 cycloalkylalkyl and aryl or R2 and R3, taken together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen; and the symbol (----) represents a single or a double bond provided that when it is a double bond the hydrogen in the 5α position does not exist and the pharmaceutically acceptable salts thereof. In view of their 5α-reductase inhibiting activity the compounds of the invention can be useful for the treatment of androgen dependent conditions.