Use of an estrogen agonist/antagonist to treat conditions responsive to estrogen such as rheumatoid arthritis, colon cancer, tissue wounds and cataracts

摘要

A compound of formula (I) or an optical or geometric isomer thereof; or a nontoxic pharmacologically acceptable acid addition salt, N-oxide, ester, quaternary ammonium salt or prodrug thereof is used to treat a condition responsive to estrogen agonist/antagonist wherein: A is CH2 or NR; B, D and E are independently CH or N; Y is optionally substituted phenyl, naphthyl, cycloalkyl, cycloalkenyl, a five or six membered heterocycle containing up to two heteroatoms selected from -O-, -NR- and -S(O)n-, or a bicyclic ring system consisting of a five or six membered heterocyclic ring fused to a phenyl ring, said heterocyclic ring containing up to two heteroatoms selected from -O-, -NR- and -S(O)n-; Z1 is -(CH2)pW(CH2)q-; -O(CH2)pCR5R6-; -O(CH2)pW(CH2)q-; -OCHR2CHR3- or -SCHR2CHR3-; G is -NR7R8; an optionally substituted bicyclic amine containing five to twelve carbon atoms, either bridged or fused or Z and G in combination may be group of formula (II); W is -CH2-; -CH=CH-; -O-; -NR2-; -S(O)n-; -C(O)-; -CR2(OH)-; -CONR2-; -NR2CO-; a group of formula (III) or -C ºC-; R and R2 to R8 are as defined in the specification; e and n are independently 0, 1 or 2; m is 1, 2 or 3 and p and q are independently 0, 1, 2 or 3.