Kristin S Marron

US Patent:

6444688, Sep 3, 2002

Filed:

Jun 7, 1995

Appl. No.:

08/476288

Inventors:

Jeffrey A. Dodge - Indianapolis IN
Charles D. Jones - Indianapolis IN
Kristin Marron - San Diego CA
James P. Sluka - Greenwood IN
Mark G. Stocksdale - South Bend IN

Assignee:

Eli Lilly and Company - Indianapolis IN

International Classification:

A61K 31445

US Classification:

514324, 514277, 514319, 514320, 514337, 514422, 514428, 546196, 546202, 546205, 546269, 546274, 546340, 546342, 548525, 548527, 548575, 548576

Abstract:

The instant invention provides compounds of formula I wherein R is OH, OâC(O)â(C -C alkyl), OâC(O)âO(C -C alkyl), OâC(O)âAr, or OâC(O)âOâAr; R is H, OH, O(C -C alkyl), OâC(O)â(C -C alkyl), OâC(O)âO(C -C alkyl), OâC(O)âAr, OâC(O)âOâAr, OâSO â(C -C alkyl), chloro, fluoro, or bromo; V is S, O, or CH CH ; W is CHOH, C(O), or CH ; X is (CH ) ; R and R each, independently, are H, C -C alkyl, C(O)â(C -C alkyl), C(O)âNHâ(C -C alkyl), C(O)âAr, or together with the nitrogen to which they are attached form a 5- or 6-membered imide or cyclic amide; n is 1, 2, or 3; and Ar is optionally substituted phenyl; povided that at least one of R and R contains a carbonyl functional group, and their use in the treatment of estrogen deficiency pathologies.

US Patent:

59624752, Oct 5, 1999

Filed:

Oct 23, 1997

Appl. No.:

8/956802

Inventors:

Christopher Randall Schmid - Indianapolis IN
James Patrick Sluka - Greenwood IN
Kristin Sue Marron - San Diego CA

Assignee:

Eli Lilly and Company - Indianapolis IN

International Classification:

A61K 31445
C07D40904
C07D41704
C07D33356

US Classification:

514324

Abstract:

The present invention provides compounds with nitrogen, sulfur or carbon linked basic side chains of formula ##STR1## where R. sup. 1 and R. sup. 2 are independently hydrogen, halo, hydroxy, alkoxy, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy, arylcarbonyloxy, aryloxycarbonyloxy, or alkylsulfonyloxy; 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 --, --NH--, --NMe--, --S--, --SO. sub. 2 --; and R. sup. 3 and R. sup. 4 are independently hydrogen, alkyl, alkylcarbonyl, alkylamino-carbonyl, or arylcarbonyl, or together with the nitrogen to which they are attached form 1-pyrrolidinyl, 1-piperidinyl, or a 5- or 6-membered imide or cyclic amide ring. The present invention also provides pharmaceutical compositions containing the compounds optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for treating osteoporosis, aortal smooth muscle cell proliferation, (particularly restenosis), and estrogen-dependent cancer (particularly breast cancer).