Substituted benzo(B)thiophene compounds having activity as selec

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514442, 514443, 514146, 546202, 548525, 549 51, A61K 31445, C07D40904, C07D41704, C07D33356

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active

059624752

ABSTRACT:
The present invention provides compounds with nitrogen, sulfur or carbon linked basic side chains of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen, halo, hydroxy, alkoxy, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy, arylcarbonyloxy, aryloxycarbonyloxy, or alkylsulfonyloxy; O--SO.sub.2 --(C.sub.4 -C.sub.6 alkyl), chloro, fluoro, or bromo; W is CHOH, C(O), or CH.sub.2 ; Y is --CH.sub.2 --, --NH--, --NMe--, --S--, --SO.sub.2 --; and R.sup.3 and R.sup.4 are independently hydrogen, alkyl, alkylcarbonyl, alkylamino-carbonyl, or arylcarbonyl, or together with the nitrogen to which they are attached form 1-pyrrolidinyl, 1-piperidinyl, or a 5- or 6-membered imide or cyclic amide ring.
The present invention also provides pharmaceutical compositions containing the compounds optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for treating osteoporosis, aortal smooth muscle cell proliferation, (particularly restenosis), and estrogen-dependent cancer (particularly breast cancer).

REFERENCES:
patent: 5589482 (1996-12-01), Thompson
patent: 5643896 (1997-07-01), Cullinan
Ruenitz, P.C. Drugs for Osteoporosis Prevention: Mechanisms of Bone Maintenance Current Medicinal Chemistry 1995 2.791-802 vol. 2, No. 4, pp.
Black, L.J.-Biological Actions and Binding Properties of a New Estrogen Antagonist, LY1107018 Hormone Antagonists,Editor M.K. Agarwal, pp. 129-145 (1982).

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