Hoffmann-La Roche Inc.

Encysive Pharmaceuticals, Inc.

Texas Biotechnology Corporation

George W Holland

Perry Rosen

Jane L Jernow

Hans Maag

Chengde Wu

Jamal M Kassir

Ramakanth Sarabu

Robert Francis Kester

Nancy-Ellen Haynes

Ronald J Biediger

Wendy Lea Corbett

Robert V Market

Ian Leslie Scott

Fred Thomas Bizzarro

Joseph Francis Grippo

Wen Li

Paige Erin Mahaney

Ka-kong Chan

David L Coffen

Frederick Wong

E Radford Decker

Timothy P Kogan

Bore G Raju

William J Zally

Brian Dupre

Vanessa O Grabbe

Shuqun Lin

John R Vermeulen

W Harry Mandeville

Jian Li

Qi Chen

Karin M Keller

Natalie Blok

Hugo E Gallo-Torres

Daxin Gao

Ferdinand K Lee

Huong Bui

Linda K Hamaker

Antonio Focella

Noel Nguyen

Junmei Wang

C Eric Anderson

Radford E Decker

A method for the inhibition of the binding of &#x3b1;&#x3b2;integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and to the use of such compounds either a above, or in formulations for the control or prevention of diseases states in which &#x3b1;&#x3b2;is involved.

Carboxylic acid derivatives that inhibit the binding of integrins to their receptors

The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.

Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists

2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Heteroaromatic glucokinase activators

Propanoic acid derivatives that inhibit the binding of integrins to their receptors

Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides, N-(isoxazolyl)pyrrolylsulfonamides and N-(isoxazolyl)phenylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or pharmaceutically acceptable derivatives thereof that inhibit the activity of endothelin are also provided.

Sulfonamides and derivatives thereof that modulate the activity of endothelin

Urea derivatives

2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

A method for the inhibition of the binding of &agr;,&bgr;,integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions thereof; and the use of the compounds either as above, or in formulations for the control or prevention of diseases states in which &agr;,&bgr;,is involved.

Compounds that inhibit the binding of integrins to their receptors

A method for the inhibition of the binding of &agr;,&bgr;,integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which &agr;,&bgr;,is involved.

N, N-disubstituted amides that inhibit the binding of integrins to their receptors

Compounds of the formula: ##STR1## wherein the substituents are as defined herein, and enantiomers, diastereomers, racemates and salts with pharmaceutically acceptable bases, antagonize LTD.sub.4 action and thus, are useful in treating bronchial asthma, pulmonary anaphylaxis, cystic fibrosis, chronic bronchitis, bronchiectasis, respiratory distress syndrome and pulmonary oedema.

Cycloalkylthiazoles

Compounds of the formula: ##STR1## wherein the substituents are as described in the specification, antagonize LTD.sub.4 action and thus, are useful in treating bronchial asthma, pulmonary anaphylaxis, cystic fibrosis, chronic bronchitis, bronchiectasis, respiratory distress syndrome and pulmonary oedema.

New optically active intermediates and processes thereto are provided for use in synthesizing therapeutically active prostaglandins of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; from a compound of the formula: ##STR2## wherein R.sup.1 is as above and R.sup.2 is hydrogen or a carboxy blocking group convertible to an acid by hydrolysis.

Prostaglandin intermediates

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North Caldwell, NJ, United States of America

George W Holland