Other

Genentech, Inc.

Syntex (u.s.a.) Inc.

Sarcode Bioscience Inc.

Hoechst Aktiengesellschaft

Aventis Pharma S.a.

Hoechst Marion Roussel

Novartis Ag

Sanofi-a Ventis Deutschland Gmbh

Aventis Pharma Deutschland, Gmbh

Novartis Pharmaceuticals Corporation

Aventis Pharma S.a. Deutschland Gmbh Genentech, Inc.

Thomas Gadek

Robert S McDowell

Jochen Knolle

Denis Carniato

Jean-Francois Gourvest

Anuschirwan Peyman

Sarah Catherine Bodary

Volkmar Wehner

Jean-Marie Ruxer

John P Burnier

Hans Ulrich Stilz

Philip L Felgner

Gordon H Jones

Deborah A Eppstein

Richard B Roman

Jean-Michel Lefrancois

Karl-Heinz Scheunemann

David William Will

Brent K Blackburn

Anurschirwan Peyman

Rob Webb

Lawrence R McGee

Robert Maurice Pitti

Peter L Barker

Karlheinz Scheunemann

Robert Andrew Cuthbertson

Frederic Naud

Kirk D Robarge

Todd C Somers

Hans-Ulrich Stilz

Jean-Georges Teutsch

Gerhard Breipohl

David A Oare

Mark E Reynolds

Mark S Stanley

Daniel J Burdick

Kazuyuki Kitamura

Mizuho Inazu

Osamu Komiyama

James C Marsters

Amuschirwan Peyman

Serge Bernard

Roland Baron

Kenneth Jay Barr

Wang Shen

Min Zhong

Johan D Oslob

Francois Goubet

Theodor Andreas Wollmann

Charles Semba

Anuschirvan Peyman

Napoleane Ferrara

Jean Francois Gourvest

Gerhard Brejpohl

Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention. 

Crystalline pharmaceutical and methods of preparation and use thereof

The present invention provides compounds and methods for the treatment of diabetic retinopathy. In particular, LFA-1 antagonists are described herein to be used in the treatment of diabetic retinopathy. One aspect of the invention provides for diagnosis of diabetic retinopathy and administration of a LFA-1 antagonist, after the patient is diagnosed with diabetic retinopathy.

Compositions and methods for treatment of diabetic retinopathy

The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

Compositions and methods for treatment

Compositions and methods for treatment of eye disorders

There are described cycloalkyl derivatives of the formula (I)R&#x2014;Y-A-B-D-E-F-G&#x2003;&#x2003;(I)in which R, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists

The present invention relates to acylguanidino derivatives of formula (I), in which R, R, R, A, B, X, Y and n have the meanings indicated in claim, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical compositions comprising them 

Guanidino derivatives as inhibitors of cell adhesion

The invention relates to novel compounds having formula (I)wherein Cy, X, Y, L and Rare as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.

LFA-1 antagonist compounds

(2S)-2-(Adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its use The present invention relates to (2S)-2-(adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester of the formula Iand its physiologically tolerable salts, their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them. The compound of the formula I and its physiologically tolerable salts are valuable pharmacologically active compounds which can be used, for example, in the treatment or prophylaxis of diseases which can be influenced by inhibiting the vitronectin receptor, for example of bone diseases such as osteoporosis.

(2S)-2-(adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrhydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its use

The present invention relates to compounds of the formula IA&#x2014;B&#x2014;D&#x2014;E&#x2014;F&#x2014;G&#x2003;&#x2003;(I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Vitronectin receptor antagonists, their preparation and their use

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Oakland, CA, United States of America

Thomas Gadek