Heterocyclic substituted benzothiophenes, compositions, and meth

Details Heterocyclic substituted benzothiophenes, compositions, and meth Heterocyclic substituted benzothiophenes, compositions, and meth

1997-02-07

1997-11-18

McKane, Joseph

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514255, 514272, 514324, 514333, 546194, 5462764, 5462811, 544224, 544333, 544405, A61K 3150, A61K 31505, C07D40914

Patent

active

056887965

ABSTRACT:
The present invention provides class of compounds of formula I ##STR1## and their pharmaceutically acceptable salts in which R.sup.1 is hydrogen, hydroxy, alkoxy, alkoxycarbonyloxy, alkylcarbonyloxy, arylcarbonyloxy; R.sup.2 is hydrogen, hydroxy, alkoxy, alkoxycarbonyloxy, alkylcarbonyloxy, alkylsulfonyloxy, arylcarbonyloxy, Cl or Br; R.sup.3 and R.sup.4 are independently C.sub.1 -C.sub.4 alkyl, or combine with the nitrogen atom to which they are attached to form a pyrrolidino, piperidino, or hexamethyleneimino ring; X is selected from ##STR2## and Y is --CO--, --CHOH--, or --CH.sub.2 --. The compounds and pharmaceutical compositions containing the compounds, either alone or in combination with either progestin or estrogen, are useful for alleviating the symptoms of osteoporosis, cardiovascular related pathological conditions such as hyperlipidemia, and estrogen-dependent cancer.
The compounds of the present invention also are useful for inhibiting uterine fibroid disease and endometriosis in women and aortal smooth muscle cell proliferation, particularly restenosis, in humans.

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