Aventis Pharma Deutschland, Gmbh

Hoechst Aktiengesellschaft

Sanofi-a Ventis Deutschland Gmbh

Sanofi-aventis

Sanofi

Aventis Pharma Duetschland Gmbh

Manfred Schudok

Hans Matter

Wilfried Schwab

Werner Thorwart

Burkhard Haase

Gerhard Kretzschmar

Otmar Klingler

Armin Hofmeister

Herman Schreuder

Eckart Bartnik

Klaus-ulrich Weithmann

Hans-Peter Nestler

Gerhard Zoller

Ulrich Lerch

Susanne Grabley

Johannes Meiwes

Peter Hammann

Michael Wagner

Anna Kohlmann

Armin Bauer

Bernhard Neises

Frank B&uuml;ttner

Volkmar Wehner

Elisabeth Defossa

Uwe Heinelt

Reinhard Kirsch

Sven Ruf

Wolfgang Holla

Maxime Lampilas

Pavel Safar

Petra Lennig

Gerd Fulling

Petra Stahl

Hauke Szillat

Antonio Ugolini

Kristin Breitschopf

Gunter Billen

G&uuml;nter Billen

The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.

Spirocyclic nitriles as protease inhibitors

The present invention includes novel derivatives of bicyclic tetrahydrofuran imino acids of formula I, processes for their preparation, and uses thereof as medicaments. The compounds are suitable for use in the therapy and prophylaxis of diseases which are associated with an increased matrix metalloproteinase activity.

Tetrahydrofuran derivatives for use as inhibitors of matrix metalloproteinases

The present invention is directed to a compound of formula (I), wherein R, R, R, R, A, L and n are as defined herein, its pharmaceutical composition, preparation and uses as a MMP inhibitor.

Substituted tetrahydroisochinolines as MMP inhibitors, related production method and use as medicine

The invention relates to a bicycloazaheterocyclyl carboxylic acid sulfonamide derivative of formula I herein, pharmaceutical preparation comprising it, process for preparing it and method for its pharmaceutical use. 

Imino acid derivatives as inhibitors of matrix metalloproteinases

The invention is directed to a compound of the formula I wherein the variables are as defined herein, ora stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a salt thereof. Another aspect of the present invention is directed to a pharmaceutical composition comprising, a pharmaceutically effective amount of one or more compounds of formula I according to claimin admixture with a pharmaceutically acceptable carrier. The invention is also directed to a method for effecting the prophylaxis and therapy of degenerative joint diseases such as osteoarthroses, spondyloses, cartilage loss following joint trauma or a relatively long period of joint immobilization following meniscus or patella injuries or ligament ruptures, diseases of the connective tissue such as collagenoses, periodontal diseases, wound healing disturbances and chronic diseases of the locomotory apparatus such as inflammatory, immunological or metabolism-associated acute and chronic arthritides, arthropathies, myalgias and disturbances of bone metabolism, for the treatment of ulceration, atheroscleroses and stenoses, and for the treatment of inflammations, cancer diseases, tumor metastasis formation, cachexia, anorexia, cardiac insufficiency and septic shock or for the prophylaxis of myocardial and cerebral infarctions, in a patient in need thereof, comprising administering to the patient a pharmaceutically effective amount of the compound of formula I according to claim, or a pharmaceutically acceptable salt, solvate or prodrug thereof. Furthermore the invention is directed to a method for preparing a compound of formula I.

Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors

The present invention is directed to a compound of formula (I), or a stereoisomer or a mixture of stereoisomer thereof in any ratio, or its physiologically tolerable salt, which is useful as an inhibitor of matrix metalloproteinase. The present invention is also directed to a pharmaceutical preparation comprising a pharmaceutically effective amount of at least one compound of formula (I); processes for their preparation; the use of a compound of formula (I) having activity as an matrix metalloproteinase inhibitor; and for the prophylaxis and therapy of disease states that involve an increase in the activity of matrix metalloproteinase.

Bicyclic imino acid derivatives as inhibitors of matrix metalloproteinases

Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.

Sulfonylaminocarboxylic acids

Compounds of formula I, in which R, R, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use

Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids

Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use

Urea derivatives with antiproteolytic activity

Factor VIIa inhibitors

Sulfonylaminophosphinic and sulfonylaminophosphonic acid derivatives, methods for their preparation and use

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Eppstein, Germany

Manfred Schudok