Estrogen agonists/antagonists

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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Details

514345, 546144, 546290, C07D21700, A61K 3147, A61K 3144

Patent

active

061536229

ABSTRACT:
Compounds of this formula ##STR1## are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.

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Lednicer, Daniel, et al., J. Med. Chem. 10 78 (1967) "Mammalian Antifertility Agents. IV. Basic, 3,4-Dihydronaphthalenes and 1,2,3,4-Tetrahydro-1-naphthols".
Bencze, W.L., et al., J. Med. Chem. 10 139 (1967) "Synthetic Estrogens, Implantation Inhibitors, and Hypocholesterolemic Agents. I. Tetrahydronaphthalene Series".
Lednicer, Daniel, et al., J. Med. Chem. 12 881 (1969) "Mammalian Antifertility Agents. VII. A Novel Sequence for the Preparation of 1,2-Disubstituted 3,4-Dihydronaphthalenes".
Jones, Robert C., Acta Endocrinologica (Copenh) 1987, 114:379-382 The Effect of a Luteinizing Hormone-Releasing Hormone Antagonist on Experimental Endometriosis in the Rat.
OsteoporosisConference, CRIP No. 1812/13 Apr. 16th/20th 1993. p. 29-30.
Jones, Charles D., et al., J. Med. Chem. (1984) 27, 1057-1066 "Antiestrogens. 2. Structure-Activity Studies in a Series of 3-Aroyl-2-arylbenzo[b]thiophene Derivatives Leading to [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)etho xy]-phenyl]methanone Hydrochloride (LY156758), a Remarkably Effective Estrogen Antagonist with Only Minimal Intrinsic Estrogenicity".
Chemical Abstract, vol. 64, pp. 15811-15814, 1966.

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