Merrell Pharmaceuticals, Inc.

Merrell Dow Pharmaceuticals

Aventis Pharmaceuticals Inc.

Sanofi-a Ventis Deutschland Gmbh

Hoechst Marion Roussel

Sanofi

Genzyme Corporation

Scios Nova, Inc.

Aventis Pharma Limited

Philippe Bey

Michael Angelastro

Shujaath Mehdi

Marion Merrell Dow Canada Inc.

Gestion De La Sante Marion Merrell Dow Canada Inc.-marion Merrell Dow Canada Health Management Inc.

Michael R Angelastro

Norton P Peet

Joseph P Burkhart

Philip M Weintraub

Cynthia A Gates

Timothy Thomas Curran

Thomas R Blohm

Chi-Hsin Richard King

Gary A Flynn

Theresa Kuntzweiler

Haifeng Eishingdrelo

Hans-Jochen Lang

Anne Minnich

Kenneth J Bordeau

Barbara Cordell

Bradford Hirth

Viviane Van Dorsselaer

Hwa-Ok Kim

Daniel G Schirlin

J O'Neal Johnston

Michael John Janusz

Niall S Doherty

Sukanthini Thurairatnam

William Arthur Metz, Jr

Kwon Yon Musick

Heng-Keang Lim

Gregory Shutske

Elina Makino

Joseph T Klein

Guyan Liang

Stanly John

Mary A Cromwell

Robert H Barker, Jr

Sungtaek Lim

Timothy T Curran

Jeffrey N Higaki

Keith John Harris

Julie Bick

Jinqi Lu

Matthew D Linnik

Gary Alan Flynn

John Jiang

Steven L Gallion

Sachin Maniar

Mark Munson

Yong-Mi Choi

James Pribish

Adedayo Adedoyin

Jennifer Caims

Yongqing Huang

Catherine Bomont

Ann Minnich

Stephan Henke

William A Metz Jr

Daniel Schirlin

Keith J Harris

Described herein is a compound of Formula (I), and pharmaceutically acceptable salts thereof. Also described herein are compositions and the use of such compositions in methods of treating a variety of diseases and conditions, in particular Krabbe's Disease (KD) and Metachromatic leukodystrophy (MLD).

UDP glycosyltransferase inhibitors and methods of use

The present invention provides methods for determining the stability of methyleneamine, methyleneamine-like compounds or compounds containing a methyleneamine moiety in the presence of semicarbazide-sensitive amine oxidase (SSAO) or a biological sample containing SSAO activity. The disclosed methods may be configured in an assay format for high throughput screening applications.

Method for determining the stability of organic methyleneamines in the presence of semicarbazide-sensitive amine oxidase

The present invention provides compounds of formula I: a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R, R, R, R, X and n are defined as defined herein. Additionally, a method for treating dopamine-related neurological disorders selected form the group consisting of neurological, psychological, cardiovascular, cognitive or attention disorders, substance abuse and addictive behavior, or a combination thereof, comprising administering to a patient in need of such treatment a therapeutically effective amount of compounds of formula I.

3-piperidinylisochroman-5-ols as dopamine agonists

Host cells expressing HM74 were used to obtain furosemide-like molecules with agonist activity having the following structure formula: 

Furosemide modulators of HM74

Host cells expressing HM74 were used to obtain oxydecalin-like molecules with agonist activity having the following structure: 

Oxydecahydronaphthalene modulators of HM74

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

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

Perfluoroalkyl ketone inhibitors of elastase and processes for making

The present invention provides 4-nitro-.DELTA..sup.4 -3-ketosteroids, their use as steroid C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and to a novel process for preparing a compound of the formula: ##STR1## comprising sequentially: a) reacting a starting compound of the formula ##STR2## with an effective amount of a strong base at an elevated or suitable temperature for a time sufficient to create the corresponding thermodynamic dienolate, followed by addition of a neutral nitrating agent to produce the 4-nitrosteroid; and then;

Process for the preparation of 4-amino-.DELTA.4-3-ketosteroids via

Inhibitors of .beta.-amyloid protein production

The invention discloses 3-ketosteroids of the following formula used to inhibit steroid C.sub.17-20 lyase: ##STR1## wherein R is OH, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkanol, COCH.sub.2 OH, CO.sub.2 H, CONR.sub.7 R.sub.8, cyclopropyloxy, cyclopropylamino, acetylthioalkane, 2,2-dimethyldioxolan4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkylthiol;

Process for the preparation of 4-amino-.DELTA..sup.4 -3-ketosteroids via

The invention discloses 3-ketosteroids of the following formula used to inhibit steroid 5.alpha.-reductase: ##STR1## wherein R is OH, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkanol, COCH.sub.2 OH, CO.sub.2 H, CONR.sub.7 R.sub.8, cyclopropoxy, acetylthioalkane, cyclopylamino, 2-2-dimethyldioxolan-4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkanethiol;

Certain 3-ketosteroids used to inhibit steroid 5.alpha.-reductase

Process for the preparation of 4-amino- 4-3-ketosteroids via 4-nitro-

This invention relates to analogs of peptidase substrates in which the nitrogen atom of the scissile amide group of the substrate peptide has been replaced by H, an aldehyde, a substituted carbonyl or a substituted malonyl 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

Growing community of inventors

Mason, OH, United States of America

Michael R Angelastro