Benzothiophene compounds

The present invention relates to compounds of formula I wherein R is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C4-C6 alkyl); R is 1-naphthyl, 2-naphthyl, 1-thienyl, 2-thienyl, benzothienyl, or -CH2C6H5; any of which may be optionally substituted with 1-3 substituents independen...

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Bibliographic Details
Main Authors STEPHEN S. Y. CHO, HENRY U BRYANT, TIMOTHY A. GRESE
Format Patent
LanguageEnglish
Published 12.03.1997
Edition6
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The present invention relates to compounds of formula I wherein R is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C4-C6 alkyl); R is 1-naphthyl, 2-naphthyl, 1-thienyl, 2-thienyl, benzothienyl, or -CH2C6H5; any of which may be optionally substituted with 1-3 substituents independently selected from the group halo, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C4-C6 alkyl); X is -CH2-, -CO-, or -CH(OH)-; n is 2 or 3; and R is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl , 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical compositions containing compounds of formula I, optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for alleviating the symptoms of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, 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.
Bibliography:Application Number: AU19960067740