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US5567828A Expired / Lapsed US ⏱️ 0.0 years remaining

Compounds and compositions with nitrogen-containing non-basic side

Assignee: Eli Lilly and Co
•
Filing: 1995-06-07
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Granted: 1996-10-22
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Expires: 2015-06-07
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Abstract

Abstract The present invention provides compounds with nitrogen-containing non-basic side chains of formula II ##STR1## wherein R 1 and R 2 , independently, are H, OH, O(C 1 -C 6 alkyl), O--C(O)--(C 1 -C 6 alkyl), O--C(O)--O(C 1 -C 6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO 2 --(C 4 -C 6 alkyl), chloro, fluoro, or bromo; W is CHOH, C(O), or CH 2 ; Y is (CH 2 ) n , or CH(C 1 -C 4 alkyl); V is S, 0, or CH 2 CH 2 ; n is 1, 2, or 3; and Ar is optionally substituted phenyl. The present invention also provides pharmaceutical compositions containing compounds of formula II, 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 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.

Inventors

  • 👤 Jeffrey A. Dodge

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-31 09:47
CPC Classifications
C; C07; C07D; C07D409/00; C07D409/02; C07D409/12; A; A61; A61P; A61P13/00; A61P13/02; A61P15/00; A61P19/00; A61P19/08; A61P19/10; A61P3/00; A61P35/00; A61P43/00; A61P9/00; C07C; C07C255/00; C07C255/01; C07C255/11; C07C255/13; C07D333/00; C07D333/50; C07D333/52; C07D333/54; C07D333/56

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 93 words
A compound with nitrogen-containing non-basic side chains of formula II ##STR39## wherein R 1 and R 2 , independently, are H, OH, O(C 1 -C 6 alkyl), O--C(O)--(C 1 -C 6 alkyl), O--C(O)--O(C 1 -C 6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO 2 -(C 4 -C 6 alkyl), chloro, fluoro, or bromo; W is CHOH, C(O), or CH 2 ; Y is (CH 2 ) n, or CH (C 1 -C 4 alkyl); V is S, O, or CH 2 CH 2 ; n is 1, 2, or 3; and Ar is optionally substituted phenyl.
Claim 2
Dependent Claim 93 words
A compound with nitrogen-containing non-basic side chains of formula II ##STR39## wherein R 1 and R 2 , independently, are H, OH, O(C 1 -C 6 alkyl), O--C(O)--(C 1 -C 6 alkyl), O--C(O)--O(C 1 -C 6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO 2 -(C 4 -C 6 alkyl), chloro, fluoro, or bromo; W is CHOH, C(O), or CH 2 ; Y is (CH 2 ) n, or CH (C 1 -C 4 alkyl); V is S, O, or CH 2 CH 2 ; n is 1, 2, or 3; and Ar is optionally substituted phenyl.
Claim 3
Dependent Claim 9 words
The compound of claim 1 wherein V is S.
Claim 4
Dependent Claim 9 words
The compound of claim 1 wherein W is C(O).
Claim 5
Dependent Claim 14 words
The compound of claim 1 wherein Y is CH 2 or CHCH 3 .
Claim 6
Dependent Claim 21 words
The compound of claim 1 wherein R 1 and R 2 , independently, are OH or O(C 1 -C 6 alkyl).
Claim 7
Dependent Claim 22 words
The compound of claim 1 wherein V is S, and W is C(O), and Y is CH 2 or CHCH 3 .
Claim 8
Dependent Claim 19 words
The compound of claim 6 wherein R 1 and R 2 , independently, are OH or OCH 3 .
Claim 9
Dependent Claim 11 words
The compound of claim 7 wherein Y is CH 2 .
Claim 10
Dependent Claim 11 words
The compound of claim 7 wherein Y is CHCH 3 .
Claim 11
Dependent Claim 29 words
A pharmaceutical composition comprising a compound according to claim 1, and optionally an effective amount of estrogen or progestin in combination with a pharmaceutically acceptable carrier, diluent, or excipient.
Claim 12
Dependent Claim 29 words
A pharmaceutical composition comprising a compound according to claim 6, and optionally an effective amount of estrogen or progestin in combination with a pharmaceutically acceptable carrier, diluent, or excipient.
Claim 13
Dependent Claim 29 words
A pharmaceutical composition comprising a compound according to claim 7, and optionally an effective amount of estrogen or progestin in combination with a pharmaceutically acceptable carrier, diluent, or excipient.
Claim 14
Dependent Claim 29 words
A pharmaceutical composition comprising a compound according to claim 8, and optionally an effective amount of estrogen or progestin in combination with a pharmaceutically acceptable carrier, diluent, or excipient.
Claim 15
Dependent Claim 29 words
A pharmaceutical composition comprising a compound according to claim 9, and optionally an effective amount of estrogen or progestin in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1999-10-22 2000-04-22 2000-10-22 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2003-10-22 2004-04-22 2004-10-22 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2007-10-22 2008-04-22 2008-10-22 $7700.00 Window Closed / Lapsed

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