Sanofi-a Ventis Deutschland Gmbh

Sanofi

Sanofi-aventis

Detlef Kozian

Sylvain Ricard

Sandrine Mace

Jean-Francois Deleuze

Karl-Ernst Siegler

Matthias Herrmann

Andreas Evers

Marc Nazare

Werngard Czechtizky

Evi Kostenis

Stefan Schaefer

Bernward Schoelkens

Martina Jacobs

Martin Bossart

Joerg Czech

Marc Nazaré

Thomas Leeuw

Wilfried Renner

Winfried Maerz

The present invention relates to compounds of the formula (I), wherein the residues Rto R, V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 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 medicaments, and pharmaceutical compositions comprising them. 

Pyrazole derivatives and their use as LPAR5 antagonists

The present invention relates to compounds of the formula (I), wherein the residues Rto R, V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present, or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 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 medicaments, and pharmaceutical compositions comprising them. 

Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation

The present invention relates to compounds of the formula (I), wherein the residues A, Rto R, Zand Zhave the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 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 medicaments, and pharmaceutical compositions comprising them. 

Benzo[1,3]dioxine derivatives and their use as LPAR5 antagonists

The present invention is directed to a method identifying a risk for a thrombogenic disorder including, without limitation, atrial fibrillation, stroke, prolonged intermitted neurological deficit (PRIND), transitory ischemic attack (TIA), atherosclerotic cerebrovascular disease (CVD) and/or coronary heart disease, as well as to a method for selecting patients with a risk for a thrombogenic disorder, to a method for identifying a pharmaceutical for the therapy or prophylaxis of a thrombogenic disorder as well as to a method for producing a medicament and a diagnostic by employing the TAFI-Ile347 polymorphism.

Method for the identification of a risk for a thrombogenic disorder by determining the TAFI-Ile347 polymorphism

The present invention refers to human EGLN2 variants having at position 58 of the amino acid sequence a serine or a leucine and their use in the prevention or treatment of thromboembolic or coronary heart diseases, in particular stroke, prolonged reversible ischemic neurological deficit (PRIND), transitoric ischemic attack (TIA), myocardial infarction and/or early myocardial infarction.

EGLN2 variants and use thereof in preventing or treating thromboembolic disorders and coronary heart diseases

The present invention relates to a method of identifying an increase in risk for type II Diabetes mellitus, venous thrombosis, or pulmonary embolism in a subject, wherein the presence of an amino acid exchange at position 286 from valine (Val) to alanine (Ala) in the EDG5 protein in a biological sample taken from the subject.

Association of EDG5 polymorphism V286A with type II diabetes mellitus and venous thrombosis/pulmonary embolism and the use thereof

EGLN2 variants and use thereof in preventing or treating thromboembolic disorders and coronary heart disease

The use of the single nucleotide polymorphism (SNP) at position &#x2212;(97) of the GIP gene for the identification of a cardiovascular disease or of an increased risk for developing a cardiovascular disease in a biological sample taken from an individual to be examined.

Use of a GIP promoter polymorphism

The present invention refers to a method for the in vitro or in vivo diagnosis of cardiovascular diseases, in particular high blood pressure, stenosis, vessel occlusion and/or other thrombotic events, wherein the nucleotide at position 950 of a nucleic acid coding for the human ARK2 protein or the amino acid at position 298 of the human ARK2 protein of a sample of a person is determined as well as to the use of ARK2 for the development and/or production of a medicament for treating a cardiovascular disease.

Method for the diagnosis and treatment of cardiovascular diseases

The present invention is directed to a method identifying a risk for a thrombogenic disorder, to a method for selecting patients with a risk for a thrombogenic disorder, to a method for identifying a pharmaceutical for the therapy or prophylaxis of a thrombogenic disorder as well as to a method for producing a medicament and a diagnostic by employing the TAFI-Ile347 polymorphism.

Method for the identification of a risk for a thrombogenic disorder by determining the TAFI-lle347 polymorphism

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 present invention refers to a method of diagnosis of a predisposition to develop thrombotic disease, to test systems and their use for the diagnosis of a predisposition to develop thrombotic disease, to a PXpromoter variant and its use for screening for an anti-thrombotic agent, and to methods for identifying an individual that can be prophylactically or therapeutically treated with an anti-thrombotic agent, or for adapting a therapeutic or prophylactic dose of an anti-thrombotic agent.

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Frankfurt am Main, Germany

Detlef Kozian