Sanofi

Sanofi-aventis

Emory University

Imperial College of Science, Technology and Medicine

Bodo Scheiper

Henning Steinhagen

Uwe Heinelt

Matthias Herrmann

Volkmar Wehner

Karl Schoenafinger

Hans Matter

Gary Mccort

Dennis C Liotta

Klaus Wirth

Josef Pernerstorfer

Hans Ulrich Stilz

James P Snyder

Christian Buning

Herman Schreuder

Sven Ruf

Jacques Mauger

Pavel Safar

Thorsten Sadowski

Anthony G M Barrett

Simak Ali

Thomas Olpp

Georg Horstick

Guillaume Begis

Ashutosh S Jogalekar

Karl Schoenafinager

Pascale Goberville

Berangere Thiers

Raoul Charles Dalmedo Stuart Coombes

Aleksandra Siwicka

Jan Brackow

Volkmar Herrmann

Bérangère Thiers

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 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 present invention relates to compounds of the formula I, wherein A, D, E, G, R, R, R, Rand Rhave the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, 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. 

Oxygen-substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals

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 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 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

This invention provides a class of compounds which are useful for specifically inhibiting cyclin-dependent kinases. This class of compounds finds use in treating diseases resulting from inappropriate activity of cyclin-dependent kinases, including cancer, viral infections (e.g., HIV) neurodegenerative disorders (e.g. Alzheimer's disease), and cardiovascular disorders (e.g. atherosclerosis). Moreover, certain members of this class are particularly useful for inhibiting cyclin-dependent kinase 7 and are especially useful for the treatment of breast cancer.

Selective inhibitors for cyclin-dependent kinases

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Frankfurt am Main, Germany

Bodo Scheiper