Therapeutic antiestrogens
AssigneeEndorecherche, Inc.
InventorsFernand Labrie, Yves Merand
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Abstract
Novel antiestrogenic compounds are disclosed for use in therapeutic preparations for treatment of estrogen-dependent diseases. The compounds are specified diphenylethane and diphenylethylene analogs which show strong affinity for estrogen receptors but substantially lack the capacity to activate such receptors or otherwise act as agonists.
Claims4
A pharmaceutical composition comprising a pharmaceutically acceptable diluent or carrier and a therapeutically effective amount of an antiestrogen of the formula:
- ##STR15## wherein R.sup.6 is methyl or ethyl;
- where the dotted line represents an optional double bond of configuration;
- wherein A.sup.1 and A.sup.11 are the same or different and are either absent or selected from the group consisting of straight-chain alkylene and branched-chain alkylene, A.sup.1 and A.sup.11 together having a total of from 3 to 20 carbon atoms;
- wherein Y is phenylene;
- wherein R.sub.21 is selected from the group consisting of hydrogen, straight or branched-chain lower alkyl, lower alkenyl, and lower alkynyl,
- wherein X is CONR.sub.23, R.sub.23 being hydrogen or lower alkyl;
- and wherein .mu. is an integer from 0 to 5.
A pharmaceutical composition comprising a pharmaceutically acceptable diluent or carrier and a therapeutically effective amount of an antiestrogen having the molecular formula:
- ##STR16##
An antiestrogenic compound having the molecular formula:
- ##STR17## wherein R.sup.6 is methyl or ethyl;
- where the dotted line represents an optional double bond of configuration;
- wherein A.sup.1 and A.sup.11 are the same or different and are either absent or selected from the group consisting of a straight- or branched-chain alkylene, A.sup.1 and A.sup.11 together having a total of from 3 to 20 carbon atoms;
- wherein Y is phenylene;
- wherein R.sub.21 is selected from the group consisting of hydrogen, straight or branched-chain lower alkyl, lower alkenyl, and lower alkynyl
- wherein X is --CONR.sub.23 --, R.sub.23 being hydrogen or lower alkyl;
- and wherein .mu. is an integer from 0 to 5.
An antiestrogenic compound having the molecular formula:
- ##STR18##
Dependencies are inferred from the claim text.