Eli Lilly and Company

Kyowa Hakko Kogyo Co., Ltd.

Ligand Pharmaceuticals, Inc.

Timothy A Grese

Henry U Bryant

Mitchell I Steinberg

David Andrew Neel

Prabhakar Kondaji Jadhav

Andrew L Glasebrook

Douglas Linn Gernert

David L Phillips

Marcus F Boehm

Yutaka Kanda

Donald Paul Matthews

Shiro Akinaga

Michael Gregory Bell

Pierre-Yves Michellys

Kevin Matthew Gardinier

Mitsunobu Hara

Peter Ambrose Lander

Jonathan Edward Green

Shinji Nara

Michael Joseph Coghlan

Kevin Robert Fales

Christopher M Mapes

Jun Eishima

Matthew Lee Brown

Rieko Nakatsu

Stephen Sung Cho

Lewis Dale Pennington

Stephen Sung Yong Cho

The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula I, including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula I.

Tricyclic steroid hormone nuclear receptor modulators

The present invention is directed to compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof: (I). The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof.

Retinoid X receptor modulators

The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation, particularly congestive heart failure, comprising administering to a patient in need thereof an effective amount of a compound of the formula: I or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula I, including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula I 

Dihydroindol-2-one derivatives as steroid hormone nuclear receptor modulators

This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as pharmaceuticals such as an antitumor agent.

Piperidine derivatives

Methods of inhibiting CNS problems in post-menopausal women

The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;

Pentacyclic compounds, intermediates, processes, compositions, and

The invention provides benzo[b]thiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pathologies.

Benzo [B] thiophene compounds, and compositions for treating bone loss,

The present invention relates to compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);

Benzothiophene compounds

The present invention provides compounds of formula I: ##STR1## wherein X is --O-- or --S--,

A method of inhibiting one or more CNS disorders in a post-menopausal woman comprising administering to a female human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

The instant invention provides methods for inhibiting bone loss comprising adminstering to a mammal in need of treatment a compound as provided in formula I.

Methods of inhibiting bone loss

A method of lowering serum cholesterol levels comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R is hydrogen; hydroxy; C.sub.1 -C.sub.6 alkoxy; a group of the formula --O--C(O)--R.sup.a, wherein R.sup.a is hydrogen, C.sub.1 -C.sub.6 alkyl optionally substituted with amino, halo, carbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.7 alkanoyloxy, carbamoyl and/or aryl; or R.sup.a is C.sub.1 -C.sub.6 alkenyl optionally substituted with aryl; or R.sup.a is a C.sub.3 -C.sub.7 cycloalkyl; or R.sup.a is aryl optionally substituted with hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, and/or halo; or R.sup.a is --O-aryl;

Methods for lowering serum cholesterol

A method of lowering serum cholesterol levels is disclosed comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R is herein defined; R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.7 alkyl substituted with C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 cycloalkyl, or substituted or unsubstituted C.sub.3 -C.sub.7 cycloalkenyl;

Method for lowering serum cholesterol

A method of lowering serum cholesterol levels comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R is as herein defined;

Growing community of inventors

Indianapolis, IN, United States of America

Timothy A Grese