Estrogen nucleus derivatives for use in inhibition of sex steroid activity

摘要

Novel compounds for the inhibition of sex steroid activity for the treatment of both androgen-related and estrogen-related diseases include for example 15- and 16-halo substituted compounds such as: The compounds are characterized by an estrogenic nucleus substituted with a substituent of the formula -R1[B-R2-]xL-G wherein at least one of L and G is a polar moiety distanced from a ring carbon of the estrogenic nucleus by a least three intervening atoms: x is an integer from 0-6; R1 and R2 are independently either absent or selected from the group consisting of straight- or branched-chain alkylene, straight- or branched-chain alkynylene, straight- or branched-chain alkenylene, phenylene, and fluoro-substituted analogs of the foregoing; and B is either absent or selected from the group consisting of -O-, -Se-, -SO-, -SO2-, -NR3-, -SiR32, -CR3OR3-, NR3CO-, NR3CS-, -CONR3-, CSNR3-, -COO-, -COS-, -SCO-, -CSS-, -SCS-, -OCO- and phenylene (R3 being hydrogen or lower alkyl).