BENZOTHIOPHENE COMPOUND SUBSTITUTED WITH HETEROCYCLIC RING AND COMPOSITION CONTAINING THE COMPOUND

摘要

PROBLEM TO BE SOLVED: To obtain a compound having biological activity and useful for the treatment of osteoporosis, cardiovascular disorder, hormone-dependent cancer relating to postmenopausal syndrome, fibroid uterus and endometritis, especially the suppression of the cell proliferation of human aortic smooth muscle such as restenosis. SOLUTION: This compound is expressed by formula I [R1 is H, hydroxy, a 1-4C alkoxy, OC(O)O(1-6C alkyl), etc.; R2 is H, chloro, bromo, hydroxy, a 1-4C alkoxy, etc.; R3 and R4 are each a 1-4C alkyl or together with N form piperidino ring, etc.; X is a group of formula II, etc.; Y is CO, CHOH or CH2 ] or its salt, e.g. [2-(4-hydroxyphenyl)-6-hydroxybenzo [b]thien-3-yl] [2-[2-(1- piperidinyl)ethoxy]pyridin-5-yl]methanone. The compound of formula I can be produced by protecting a benzo [b]thiophene having 6-hydroxyl group and 2-(4-hydroxyphenyl) group, acylating the product and deprotecting the acylated compound.