Compounds and compositions with nitrogen-containing non-basic side chains
AssigneeEli Lilly and Company
InventorJeffrey A. Dodge
Life of this patent
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Abstract
The present invention provides compounds and pharmaceutical compositions, optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for inhibiting the symptoms of postmenopausal symptoms, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer. The present invention further provides the use of the compounds of the present invention for inhibiting uterine fibroid disease and endometriosis in women, and aortal smooth muscle cell proliferation, particularly restenosis, in humans.
Claims11
A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need of such treatment an effective amount of a compound of formula II ##STR38## wherein R.sup.1 and R.sup.2, independently, are H, OH, O(C.sub.1 -C.sub.6 alkyl), O--C(O)--(C.sub.1 -C.sub.6 alkyl), O--C(O)--O(C.sub.1 -C.sub.6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, 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).sub.n, or CH(C.sub.1 -C.sub.4 alkyl);
- V is S, O, or CH.sub.2 CH.sub.2 ;
- n is 1, 2, or 3;
- and
- Ar is optionally substituted phenyl;
- or a pharmaceutically acceptable salt or solvate thereof.
A method for alleviating endometriosis comprising administering to a woman in need of such treatment an effective amount of a compound of formula II ##STR39## wherein R.sup.1 and R.sup.2, independently, are H, OH, O(C.sub.1 -C.sub.6 alkyl), O--C(O)--(C.sub.1 -C.sub.6 alkyl), O--C(O)--O(C.sub.1 -C.sub.6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, 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).sub.n, or CH(C.sub.1 -C.sub.4 alkyl);
- V is S, O, or CH.sub.2 CH.sub.2 ;
- n is 1, 2, or 3;
- and
- Ar is optionally substituted phenyl;
- or a pharmaceutically acceptable salt or solvate thereof.
A method for alleviating aortal smooth muscle cell proliferation comprising administering to a person in need of such treatment an effective amount of a compound of formula II ##STR40## wherein R.sup.1 and R.sup.2, independently, are H, OH, O(C.sub.1 -C.sub.6 alkyl), O--C(O)--(C.sub.1 -C.sub.6 alkyl), O--C(O)--O(C.sub.1 -C.sub.6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, 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).sub.n, or CH(C.sub.1 -C.sub.4 alkyl);
- V is S, O, or CH.sub.2 CH.sub.2 ;
- n is 1, 2, or 3;
- and
- Ar is optionally substituted phenyl;
- or a pharmaceutically acceptable salt or solvate thereof.
A method for alleviating restenosis comprising administering to a person in need of such treatment an effective amount of a compound of formula II ##STR41## wherein R.sup.1 and R.sup.2, independently, are H, OH, O(C.sub.1 -C.sub.6 alkyl), O--C(O)--(C.sub.1 -C.sub.6 alkyl), O--C(O)--O(C.sub.1 -C.sub.6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, 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).sub.n, or CH(C.sub.1 -C.sub.4 alkyl);
- V is S, O, or CH.sub.2 CH.sub.2 ;
- n is 1, 2, or 3;
- and
- Ar is optionally substituted phenyl;
- or a pharmaceutically acceptable salt or solvate thereof.
Dependencies are inferred from the claim text.