Compounds and compositions with nitrogen-containing non-basic side chains
First Claim
1. 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 R1 and R2, independently, are H, OH, O(C1 -C6 alkyl), O--C(O)--(C1 -C6 alkyl), O--C(O)--O(C1 -C6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO2 --(C4 -C6 alkyl), chloro, fluoro, or bromo;
- W is CHOH, C(O), or CH2 ;
Y is (CH2)n, or CH(C1 -C4 alkyl);
V is S, O, or CH2 CH2 ;
n is 1, 2, or 3; and
Ar is optionally substituted phenyl;
or a pharmaceutically acceptable salt or solvate thereof.
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Accused Products
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.
17 Citations
11 Claims
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1. 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 R1 and R2, independently, are H, OH, O(C1 -C6 alkyl), O--C(O)--(C1 -C6 alkyl), O--C(O)--O(C1 -C6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO2 --(C4 -C6 alkyl), chloro, fluoro, or bromo;
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W is CHOH, C(O), or CH2 ; Y is (CH2)n, or CH(C1 -C4 alkyl); V is S, O, or CH2 CH2 ; n is 1, 2, or 3; and Ar is optionally substituted phenyl; or a pharmaceutically acceptable salt or solvate thereof. - View Dependent Claims (2, 3, 4, 5, 6, 10, 11)
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7. 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 R1 and R2, independently, are H, OH, O(C1 -C6 alkyl), O--C(O)--(C1 -C6 alkyl), O--C(O)--O(C1 -C6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO2 --(C4 -C6 alkyl), chloro, fluoro, or bromo;
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W is CHOH, C(O), or CH2 ; Y is (CH2)n, or CH(C1 -C4 alkyl); V is S, O, or CH2 CH2 ; n is 1, 2, or 3; and Ar is optionally substituted phenyl; or a pharmaceutically acceptable salt or solvate thereof.
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8. 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 R1 and R2, independently, are H, OH, O(C1 -C6 alkyl), O--C(O)--(C1 -C6 alkyl), O--C(O)--O(C1 -C6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO2 --(C4 -C6 alkyl), chloro, fluoro, or bromo;
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W is CHOH, C(O), or CH2 ; Y is (CH2)n, or CH(C1 -C4 alkyl); V is S, O, or CH2 CH2 ; n is 1, 2, or 3; and Ar is optionally substituted phenyl; or a pharmaceutically acceptable salt or solvate thereof.
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9. 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 R1 and R2, independently, are H, OH, O(C1 -C6 alkyl), O--C(O)--(C1 -C6 alkyl), O--C(O)--O(C1 -C6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO2 --(C4 -C6 alkyl), chloro, fluoro, or bromo;
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W is CHOH, C(O), or CH2 ; Y is (CH2)n, or CH(C1 -C4 alkyl); V is S, O, or CH2 CH2 ; n is 1, 2, or 3; and Ar is optionally substituted phenyl; or a pharmaceutically acceptable salt or solvate thereof.
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Specification
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- Resources
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Current AssigneeEli Lilly and Company
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Original AssigneeEli Lilly and Company
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InventorsDodge, Jeffrey A.
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Primary Examiner(s)Dees, Jos e G.
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Assistant Examiner(s)LAMBKIN, DEBORAH C
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Application NumberUS08/680,475Time in Patent Office309 DaysField of Search514/443, 514/469, 514/520, 514/177, 514/182US Class Current514/177CPC Class CodesA61P 13/02 of urine or of the urinary ...A61P 15/00 Drugs for genital or sexual...A61P 19/10 for osteoporosisA61P 3/00 Drugs for disorders of the ...A61P 35/00 Antineoplastic agentsA61P 43/00 Drugs for specific purposes...A61P 9/00 Drugs for disorders of the ...C07C 255/13 containing cyano groups and...C07D 333/56 Radicals substituted by oxy...C07D 409/12 linked by a chain containin...
