Aventis Pharma Deutschland, Gmbh

Sanofi

Sanofi-a Ventis Deutschland Gmbh

Other

Hoechst Aktiengesellschaft

Sanofi-aventis

Genentech, Inc.

Aventis Pharma S.a.

Hoechst Schering Agrevo Gmbh

Hoechst Marion Roussel

Ucb Biopharma Sprl

Hoechst Marion Roussel Deutschland Gmbh

Hoechst Aktiengesellschaft Ag

Volkmar Wehner

Hans Ulrich Stilz

Robert S McDowell

Thomas Gadek

Jochen Knolle

Denis Carniato

Uwe Heinelt

Hans Matter

Dirk Seiffge

Marc Nazare

Anuschirwan Peyman

Jean-Francois Gourvest

Henning Steinhagen

Jean-Marie Ruxer

Jean-Michel Lefrancois

Matthias Herrmann

Karl Schoenafinger

Wolfgang Schmidt

David William Will

Matthias Urmann

Sarah Catherine Bodary

Robert Maurice Pitti

Kurt Ritter

Michael Wagner

Reinhard Kirsch

Armin Bauer

Hans-Ulrich Stilz

Markus Follmann

Werner Knauf

Manfred Kern

Burkhard Sachse

Werner Bonin

Anna Waltersdorfer

Harald Jakobi

Wolfgang Schaper

Adolf Heinz Linkies

Dieter Bernd Reuschling

Peter Braun

Olaf Ritzeler

Rainer Preuss

Bodo Scheiper

Peter Lummen

Friedemann Schmidt

Karlheinz Scheunemann

Dirk Gretzke

Zhaoning Zhu

Jean-Georges Teutsch

Rikki Peter Alexander

Gilbert Lassalle

Boris Kroeplien

Sven Ruf

Victoria Elizabeth Jackson

Jag Paul Heer

Jean-Michel Altenburger

Martin Lorenz

Kazuyuki Kitamura

Klaus-ulrich Weithmann

Mizuho Inazu

Mark Daniel Calmiano

Yogesh Anil Sabnis

Volker Laux

Michael Deligny

Jean-Pascal Herault

Osamu Komiyama

Horst Blum

Tom Gadek

Christoph Huels

Gerhard Zoller

Gerhard Breipohl

Holger Heitsch

Malcolm Maccoss

Anthony C Scotese

Manfred Schudok

Kent W Neuenschwander

Stefanie Flohr

Herman Schreuder

Julien Alistair Brown

Otmar Klingler

Herbert Kogler

Matthew Duncan Selby

Jacques Mauger

Pavel Safar

Christopher Kallus

Petra Lennig

Joanna Rachel Quincey

Gareth Neil Brace

Jean Keyaerts

Petra Stahl

Bernhard Neises

Hauke Szillat

Malcolm Mac Coss

Dominique Louis Leon Swinnen

Ellen Olivia Gallimore

Marc Nazaré

Christoph Huls

Hartmut R&uuml;tten

Prafulkumar Tulshibhai Chovatia

Frédéric Petit

Nathalie Van Houtvin

The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, Rto Rand Rare as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders

The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, Rto Rand Rare as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them. 

A series of fused tricyclic imidazole derivatives, in particular dihydro-1H-cyclopenta[4,5]imidazo[1,2-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNF&#x3b1; activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Fused tricyclic imidazole derivatives as modulators of TNF activity

A series of tricyclic benzimidazole derivatives, in particular dihydro-1H-imidazo [1,2-a]benzimidazole, dihydro-1H-pyrrolo [1,2-a]benzimidazole, dihydro-1H-pyrazino[1,2-a]benzimidazole, dihydro-1H-[1,4]oxazino[4,3-a]benzimidazole and dihydrothiazolo[3,4-a]benzimidazolem, and analogs thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Fused tricyclic benzimidazoles derivatives as modulators of TNF activity

The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.

Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments

The invention relates to novel compounds of formula I where X, A, Q1, Q2, Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.

Triazolium salts as PAR1 inhibitors, production thereof, and use as medicaments

The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are 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.

Chlorothiophene-isoxazoles as inhibitors of coagulation factors Xa and thrombin

The disclosure relates to compounds of formula I: wherein the groups R1, R2, R3, R4, R5 and X are as defined in the disclosure, having antithrombotic activity, which in particular inhibits the protease-activated receptor 1 (PAR1). The disclosure further relates to methods for producing the same and to the use thereof as a pharmaceutical product.

Pyridylvinylpyrazoloquinolines as PAR1 inhibitors

The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, R9, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.

Imidazopyridazines as PAR1 inhibitors, production thereof, and use as medicaments

The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.

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The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are 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.

Chlorothiophene-amides as inhibitors of coagulation factors Xa and thrombin

The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially 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. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Malonamide derivatives with antithrombotic activity

The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.

Heteroaryl-carboxylic acid (sulfamoyl alkyl) amide-derivatives as factor Xa inhibitors

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Sandberg, Germany

Volkmar Wehner