Sanofi-a Ventis Deutschland Gmbh

Sanofi

Aventis Pharma Deutschland, Gmbh

Sanofi-aventis

Ucb Biopharma Sprl

Hoechst Aktiengesellschaft

Genzyme Corporation

Ucbbiopharma Srl

Uwe Heinelt

Hans-Jochen Lang

Klaus Wirth

Armin Hofmeister

Volkmar Wehner

Markus Bleich

Henning Steinhagen

Matthias Herrmann

Karl Schoenafinger

Elisabeth Defossa

Michael Gekle

Hans Matter

Gerhard Zoller

Otmar Klingler

John Weston

Bodo Scheiper

Victoria Elizabeth Jackson

Armin Walser

Hans-Willi Jansen

Olaf Ritzeler

Jag Paul Heer

Fahad A Al-Obeidi

Nils Rackelmann

Friedemann Schmidt

Peter Wildgoose

Thomas Licher

Dirk Gretzke

Zhaoning Zhu

Markus Follmann

Rikki Peter Alexander

Ulrich Gebert

Boris Kroeplien

Pavel Safar

Mark Daniel Calmiano

Laurent Bialy

John J Grome

Yogesh Anil Sabnis

Karl Rudolphi

Petra Arndt

Michael Deligny

Heinrich Englert

Heinz-Werner Kleemann

Jan-Robert Schwark

Wendelin Frick

Kurt Ritter

Malcolm Maccoss

Manfred Schudok

Julien Alistair Brown

Max Hropot

Matthew Duncan Selby

Jacques Mauger

Maria Mendez-Perez

Hiristo Anagnostopulos

Joanna Rachel Quincey

Joerg Czech

Gareth Neil Brace

Jean Keyaerts

Erhard Wolf

Hauke Szillat

Dominique Louis Leon Swinnen

Ellen Olivia Gallimore

Gernot Zech

Malcolm Mac Coss

Prafulkumar Tulshibhai Chovatia

Matthias Hermann

Dominique Louis Léon Swinnen

Sabine Defays

Nathalie Van Houtvin

Praful Tulshi Chovatia

Volkmar Herrmann

Karl Schoenafinager

Veronique Durieu

Martin Hug

Dominique Louis Swinnen

Volmar Wehner

Véronique Durieu

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 disclosure relates to isoxazolidines and their use as receptor-interacting protein kinase 1 inhibitors, for example in the treatment of diseases and disorders mediated by RIP kinase 1.

Isoxazolidines as RIPK1 inhibitors and use thereof

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 substituted fused tricyclic imidazo pyrazine derivatives and analoges thereof, represented by formula (I), 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 imidazo pyrazines as modulators of TNF activity

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 substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.

Substituted aminoindanes and analogs thereof, and the pharmaceutical use thereof

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

This disclosure relates to compounds of formula I: wherein R1, R2, R3, R4, X and Y have the meanings denoted in the disclosure. The compounds of formula I have antithrombotic activity and in particular inhibit the protease-activated receptor 1 (PAR1). The disclosure further relates to a method for producing the compound of formula I and to the use thereof as a pharmaceutical product.

Tricyclic pyridyl-vinyl pyrroles as PAR1 inhibitors

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 invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders. 

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 provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.

Process for synthesizing heterocyclic compounds

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

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Wiesbaden, Germany

Uwe Heinelt