Sex steroid activity inhibitors
AssigneeEndorecherche, Inc.
InventorsFernand Labrie, Yves Merand
Life of this patent
Estimating the term…
Abstract
Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.
Claims13
A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a therapeutically effective amount of an estrogen activity inhibitor of the following formula:
- ##STR157## wherein the dotted line is optional double bond;
- wherein R.sub.5 and R.sub.6 are independently hydrogen, hydroxyl or a moiety which is converted to hydroxyl in vivo, but are not simultaneously hydrogen and are not simultaneously at positions 3 and 12;
- wherein Z is a bivalent ring closing moiety;
- wherein R.sup.100 is a bivalent moiety which distances L from the B-ring by 4-10 intervening atoms;
- wherein L is a bivalent or trivalent polar moiety selected from the group consisting of --CO--, --SO--, --CON<, --N<
- and --SON<;
- wherein G.sup.1 is either absent or selected from the group consisting of hydrogen, a C.sub.1 to C.sub.5 hydrocarbon, a saturated or unsaturated C.sub.5 to C.sub.7 cycloalkyl, a bivalent moiety which joins G.sup.2 and L to form a 5- to 7-membered heterocyclic ring, and halo-substituted derivatives of the foregoing;
- wherein G.sup.2 is either absent or selected from the group consisting ft hydrogen, a C.sub.1 to C.sub.5 hydrocarbon, a substituted or unsubstituted C.sub.5 to C.sub.7 cycloalkyl, a bivalent moiety which joins G.sup.1 and L to form a 5- to 7-membered heterocyclic ring and halo-substituted derivatives of the foregoing;
- and
- wherein G.sup.3 is a lower hydrocarbon.
A compound having the following molecular structure:
- ##STR158## wherein the dotted line is an optional double bond;
- wherein R.sub.5 and R.sub.6 are independently hydrogen, hydroxyl or a moiety which is converted to hydroxyl in vivo, but are not simultaneously hydrogen and are not simultaneously at positions 3 and 12;
- wherein Z is a bivalent ring closing moiety;
- wherein R.sup.100 is a bivalent moiety which distances L from the B-ring by 4-10 intervening atoms;
- wherein L is a bivalent or trivalent polar moiety selected from the group consisting of --CO--, --O--, --SON<, --N<
- and --SON<;
- wherein G.sup.1 is either absent or selected from the group consisting of hydrogen, a C.sub.1 to C.sub.5 hydrocarbon, a saturated or unsaturated C.sub.5 to C.sub.7 cycloalkyl, a bivalent moiety which joins G.sup.2 and L to form a 5- to 7-membered heterocyclic ring, and halo-substituted derivatives or the foregoing;
- wherein G.sup.2 is either absent or selected from the group consisting of hydrogen, a C.sub.1 to C.sub.5 hydrocarbon, a substituted or unsubstituted C.sub.5 to C.sub.7 cycloalkyl, a bivalent moiety which joins G.sup.1 and L to form a 5- to 7-membered heterocyclic ring and halo-substituted derivatives of the foregoing;
- and
- wherein G.sup.3 is a lower hydrocarbon.
A compound having the molecular structure:
- ##STR159## wherein R.sup.6 is methyl, ethyl, propyl, ethenyl or ethynyl;
- and wherein the two hydroxyl groups are not simultaneously at positions 3 and 12.
Dependencies are inferred from the claim text.