Aventis Pharma Deutschland, Gmbh

Hoechst Aktiengesellschaft

Sanofi-a Ventis Deutschland Gmbh

Ajinomoto Co., Ltd.

Cassella Aktiengesellschaft

Sanofi

Sanofi-aventis

Hoechst Marion Roussel

Cassella Aktiengessellschaft

Otmar Klingler

Gerhard Zoller

Melitta Just

Hans Matter

Jochen Knolle

Bernd Jablonka

Gerhard Breipohl

Elisabeth Defossa

Wolfgang Konig

Manfred Schudok

Armin Walser

Fahad A Al-Obeidi

Uwe Heinelt

Herman Schreuder

Hans-Peter Nestler

Peter Wildgoose

Hans Ulrich Stilz

Naoyuki Fukuchi

James A Ostrem

Hans-Ulrich Stilz

Kuniya Sakurai

Volkmar Wehner

Reinhard Kirsch

Werngard Czechtizky

Joerg Habermann

Pavel Safar

Klaus-ulrich Weithmann

Christian Engel

Joerg Czech

Horst Blum

Andreas Lindenschmidt

Tilo Weiss

Hauke Szillat

Bernard Pirard

Wolfgang K Onig

The present invention relates to compounds of the Formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb), and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them. 

Cyclic peptides, their preparation and their use as inhibitors of the platelet adhesion

The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Pyrrole derivatives as P2Y12 antagonists

The present invention relates to compounds of the formula I, in which R1, R2, A, B, D, E, n, m or o have the meanings indicated below. The compounds of the formula I are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb). They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of atherothrombotic diseases.

Inhibitors of the GPIb-vWF interaction, their preparation and use

The present invention relates to compounds of the formula I, in which R1, R2, A, B, D, F, n, m and o have the meanings indicated herein. The compounds of the formula I are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb). They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of atherothrombotic diseases 

Inhibitors of the GPIb&#x2014;vWF interaction, their preparation and use

Pyrimidine-4,6-dicarboxylic acid diamides of the formula I are suitable for selectively inhibiting collagenase (MMP 13). The pyrimidine-4,6-dicarboxylic acid diamides can therefore be used for treating degenerative joint diseases.

Pyrimidine-4,6-dicarboxylic acid diamides for selectively inhibiting collagenases

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

Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them

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

Urea derivatives with antiproteolytic activity

N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them

Factor VIIa inhibitors

Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them

The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R , R , R R , R , R , R and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I) in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and/or auxiliary substances.

Indole derivatives as inhibitors or factor Xa

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Rodgau, Germany

Otmar Klingler