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Abstract

The invention provides novel benzothiophenes of the formula: ##STR1## wherein R.sub.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --O--CO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl, or --OCOAr where Ar is optionally substituted phenyl; R.sub.2 is --H, --OH, --Cl, --Br, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl, or --OCOAr where Ar is optionally substituted phenyl; R.sub.3 is --H, --F, --Cl, --(C.sub.1 -C.sub.4 alkyl), --CN, or --O(C.sub.1 -C.sub.3 alkyl); R.sub.4 is --H, --F, --Cl, --(C.sub.1 -C.sub.4 alkyl), --CN or --O(C.sub.1 -C.sub.3 alkyl); R.sub.5 is --H, --F, --Cl, --(C.sub.1 -C.sub.4 alkyl), or --O(C.sub.1 -C.sub.3 alkyl); and R.sub.6 is --H, --F, --Cl, --(C.sub.1 -C.sub.4 alkyl), or --O(C.sub.1 -C.sub.3 alkyl); with the provisos that R.sub.3, R.sub.4, R.sub.5 and R.sub.6 can not all be hydrogen, and that when one of R.sub.3, R.sub.4, R.sub.5 or R.sub.6 is C.sub.1 -C.sub.4 alkyl, no more than two of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 can be hydrogen; Y is --CO--, --CHOH--, or --CH.sub.2 --; R.sub.7 and R.sub.8 are independently C.sub.1 -C.sub.4 alkyl or combine to form, with the nitrogen to which they are attached, 1-piperidinyl, 1-pyrrolidinyl, 1-hexamethyleneimino, or morpholino; or a pharmaceutically acceptable salt thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, optionally containing estrogen opr progestin, and the use of such compounds alone, or in combination with estrogen or progestin or alleviating the symptoms of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer.

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First Claim