Sanofi-a Ventis Deutschland Gmbh

Sanofi-aventis

Sanofi

Behringwerke Aktiengesellschaft

Aventis Pharma Deutschland, Gmbh

Hoechst Marion Roussel Deutschland Gmbh

Joerg Czech

Klaus Bosslet

Martin Opper

Melitta Just

Eckart Bartnik

Tilo Weiss

Ekkehard Leberer

Andreas R Klatt

Thomas Leeuw

Sebastian Barradeau

Uwe Heinelt

Armin Hofmeister

Gerhard Hessler

Otmar Klingler

Marc Nazare

Werngard Czechtizky

Detlef Kozian

Dieter Hoffmann

Sylvain Ricard

Sandrine Mace

Jean-Francois Deleuze

Karl-Ernst Siegler

Gernot Zech

The present invention relates to compounds of the formula I, in which R; R; R; R; R; R; Z; A; B; E; X; Q; J; V; G and M 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.

Quinoline-carboxamide derivatives as P2Y12 antagonists

Provided herein are carbohydrate complement-modified bifunctional glycoproteins, and their use in tumor-selective therapy. The bifunctional glycoproteins comprise a first component that specifically binds to a tumor-specific antigen and a second component having enzymatic activity by means of which a non-toxic prodrug is cleaved into a cytotoxic drug. The carbohydrate complement comprises at least one exposed carbohydrate residue selected from the group consisting of mannose, galactose, N-acetylglucosamine, N-acetyllactose, glucose and fucose. The modified carbohydrate complement contributes to increased relative concentration of the glycoproteins at the site of the tumor, and enhanced clearance from the general circulation and non-tumor sites.

Bifunctional glycoproteins having a modified carbohydrate complement and their use in tumor-selective therapy

The invention refers to the use of a p21-activated kinase (PAK) inhibitor as a target protein for the discovery of a PAK inhibitor as a medicament for the treatment of a joint disease.

Use of PAK inhibitor for the treatment of a joint disease

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 invention relates to polynucleotide sequences comprising genetic variations of the PAR1 gene at positions 3090 and/or 3329. The occurrence of these variants in humans correlates with increased occurrence of particular cardiovascular disorders. The invention furthermore relates to methods for detecting said genetic variations for the purpose of patient diagnosis.

Analysis and use of PAR1 polymorphisms for evaluating the risk of cardiovascular disorders

The invention relates to compounds of the formula I having antithrombotic activity, which in particular inhibit the protease-activated receptor 1 (PAR1), processes for their preparation and use thereof as medicaments.

Imino-imidazo-pyridine derivatives having antithrombotic activity

The invention refers to the use of a p21-activated kinase (PAK) inhibitor for the treatment of a joint disease such as osteoarthritis or rheumatoid arthritis or for the treatment of a joint pain and the use of PAK as a target protein for the discovery of a PAK inhibitor as a medicament for the treatment of a joint disease.

The invention relates to the cytoplasmic expression of antibodies, antibody fragments and antibody fragment fusion molecules in. In particular, antibody fragment fusion molecules having an antibody moiety which is directed against tumors and an enzyme moiety which cleaves a nontoxic prodrug to give the toxic drug can be advantageously prepared in this way while retaining their respective functional properties.

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The invention relates to the cytoplasmic expression of antibodies, antibody fragments and antibody fragment fusion molecules in In particular, antibody fragment fusion molecules having an antibody moiety which is directed against tumors and an enzyme moiety which cleaves a nontoxic prodrug to give the toxic drug can be advantageously prepared in this way while retaining their respective functional properties.

Cytoplasmic expression of antibodies, antibody fragments and antibody fragment fusion proteins in E. coli

The invention relates to the cytoplasmic expression of antibodies, antibody fragments and antibody fragment fusion molecules in E. coli. In particular, antibody fragment fusion molecules having an antibody moiety which is directed against tumors and an enzyme moiety which cleaves a nontoxic prodrug to give the toxic drug can be advantageously prepared in this way while retaining their respective functional properties.

Growing community of inventors

Marburg, Germany

Joerg Czech