Merrell Pharmaceuticals, Inc.

Merrell Dow Pharmaceuticals

Aventis Pharmaceuticals Inc.

Eli Lilly and Company

Hoechst Marion Roussel

Aventis Pharma Limited

Joseph P Burkhart

Norton P Peet

Michael R Angelastro

Shujaath Mehdi

J O'Neal Johnston

Philip M Weintraub

Cynthia A Gates

Matthew Joseph Fisher

Timothy Paul Burkholder

Yanping Xu

Daniel G Schirlin

Eugene L Giroux

Shawn Christopher Miller

Karin Briner

Jeffrey Thomas Mullaney

Thomas R Blohm

Bernhard Neises

William Harlan Gritton

H Michael Kolb

Fritz E Gerhart, Deceased

J O'neal Johnston

Leonard Larry Winneroski, Jr

Yao-Chang Xu

Matthew Robert Reinhard

Gene W Holbert

Brian Eugene Cunningham

Michel J Jung

William A Metz

Gary A Flynn

Douglas Wade Beight

Alan M Warshawsky

Meena V Patel

Cynthia Darshini Jesudason

Robert J Broersma

Dennis C Thompson

Daniel Timothy Kohlman

Sidney Xi Liang

Michael John Janusz

Freddie Craig Stevens

Ramalinga M Dharanipragada

Roger Ryan Rothhaar

William Arthur Metz, Jr

Timothy Thomas Curran

Joseph T Tsay

Michael J Jung

J Anthony Malikayl

Jian Shen

Steven L Gallion

William A Metz Jr

J O Johnston

Timothy T Curran

J Antony Malikayl

Jiu-Tsair Tsay

The present invention provides serotonergic aminoalkylbenzofurans of Formula (I): where R, R, R, R, R, R', R, R&#x2032;, and Rare as described in the specification. 

Aminoalkylbenzofurans as serotonin (5-HT(2c)) agonists

The present invention provides serotonergic benzofurylpiperazines of Formula I:where:

Benzofurylpiperazines and benzofurylhomopiperazines: serotonin agonists

The present invention relates to certain novel 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.

3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase

The present invention provides serotonergic benzofurans of Formula (I): where A, R, R, R, R, and Rare as described in the specification.

Serotonergic benzofurans

This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P moiety is substituted with various nitrogen-containing heterocyclic groups. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient afflicted with a neutrophil associated inflammatory disease.

Elastase inhibitors

The invention relates to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20&xgr;-fluoropregna-5,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C lyase, 5&agr;-reductase and C -hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide. The compounds of the invention have the following general formulae:

20-fluoro-17(20)-vinyl steroids

The present invention is directed to a method of using a certain compounds which are 2,19-methyleneoxy or 2,19 methylenethio bridged steroids, and related steroidal compounds as inhibitors of the enzyme steroid aromatase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.

2,19-methyleneoxy and 2,19-methylenethio bridged steroids as aromatase, 19-hydroxylase inhibitors and methods of their use in the treatment of estrogen mediated disorders

This invention relates to novel morpholinourea and related derivatives of pentafluoroethyl peptides which are orally active elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases and emphysema.

Orally-active elastase inhibitors

This invention relates to acylated enol derivatives of &agr;-ketoesters and &agr;-ketoamides. The compounds of this invention are either prodrugs of known elastase inhibitors or are elastase inhibitors in their own right and are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema.

Acylated enol derivative of &agr;-ketoesters and &agr;-ketoamides

This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Peptidase inhibitors

This invention relates to polyfluoroalkyl tryptophan tripeptides and to compositions containing them. The compounds are highly selective thrombin inhibitors which provide anticoagulant effects useful in the treatment of thrombin conditions and in preventing the coagulation of stored whole blood and blood products.

Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors

Perfluoroalkyl ketone inhibitors of elastase and processes for making

The present invention relates to methods and compositions using .DELTA..sup.16 unsaturated steroids which are useful as steroid C.sub.17-20 lyase inhibitors.

Methods and compositions using .DELTA..sup.16 unsaturated C.sub.17

This invention relates to acylated enol derivatives of known elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema or as prodrugs of compounds which are useful in the treatment of said diseases.

Acylated enol derivatives as prodrugs of elastase inhibitors

The present invention relates to .DELTA..sup.16 unsaturated steroids which are useful as steroid C.sub.17-20 lyase inhibitors.

.increment..sup.16 unsaturated C.sub.17 heterocyclic steroids useful as

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West Chester, OH, United States of America

Joseph P Burkhart