Sanofi

Sanofi-Aventis

Bayer Aktiengesellschaft

Henning Steinhagen

Volkmar Wehner

Uwe Heinelt

Matthias Herrmann

Karl Schoenafinger

Bodo Scheiper

Hans Matter

Thomas Krahn

Markus Follmann

Joachim Schuhmacher

Erwin Bischoff

Gary Mccort

Holger Paulsen

Wolfgang Thielemann

Karl-Heinz Schlemmer

Herman Schreuder

Jochen Goerlitzer

Barbara Albrecht

Michael Gerisch

Felix Oehme

Axel Jensen

Stephan-Nicholas Müller

Kurt Ritter

Jörg Keldenich

Joachim Mittendorf

Reinhard Kirsch

Hans Ulrich Stilz

Anthony C Scotese

Kent W Neuenschwander

Marcel Patek

Jacques Mauger

Martin Smrcina

Martin Lorenz

Pavel Safar

Joachim H&uuml;tter

Kirsten Bjergarde

Jan Jänichen

Michael H&auml;rter

Hauke Szillat

Gabriele Handke

Guillaume Begis

Stephan Lensky

Stephan-Nicholas M&uuml;ller

Werner Nickl

Pascale Goberville

Gabriele Handke-Ergüden

Linli Wei

Bernard Pirard

Jochen Huber

Bérangère Thiers

Gary McCort

Jozsef Zsolt Bocskei

Berangere Thiers

Karl Schoenafinager

Volkmar Herrmann

Guillaume Bègis

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 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 present invention relates to cyclic azaindole-3-carboxamides of the formula I, wherein A, R, R, R, R, R, Y, Y, Y, Y, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Cyclic azaindole-3-carboxamides, their preparation and their use as pharmaceuticals

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 cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib, wherein R, R, R, R, R, R, Y, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae Ia and Ib, their use and pharmaceutical compositions comprising them.

Cyclic (aza)indolizinecarboxamides, their preparation and their use as pharmaceuticals

The invention relates to the compounds of formula I having antithrombotic activity which especially inhibits blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.

Tartrate derivatives for use as coagulation factor IXa inhibitors

The present invention relates to cyclic indole-3-carboxamides of the formula I, wherein A, R, R, R, R, R, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Cyclic indole-3-carboxamides, their preparation and their use as pharmaceuticals

Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).

Aryl-  and heteroaryl-ethyl-acylguanidine derivatives, their preparation and their application in therapeutics

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 invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.

Isoserine derivatives for use as coagulation factor IXa inhibitors

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Sulzbach, Germany

Henning Steinhagen