Sanofi

Syntex Pharmaceuticals, Ltd.

Sanofi-aventis

Synthelabo

Gary Mccort

Michel Tabart

Frank Halley

Laurent Schio

Youssef El-Ahmad

Bruno Filoche-Romme

Fabienne Thompson

Maurice Brollo

Corinne Terrier

Victor Certal

Jean-Claude G Pascal

Monsif Bouaboula

Hans Matter

Olivier Duclos

Henning Steinhagen

Bodo Scheiper

Antoine Alam

Gilbert Lassalle

Francoise Bono

Guillaume Begis

Sandrine Biscarrat

Dominique Blondet

Patrice Bellevergue

Klaus Wirth

Hans Ulrich Stilz

Christian Hoornaert

Werngard Czechtizky

Olaf Ritzeler

John Weston

Pierre Savi

Volker Kraft

Petra Arndt

Nils Rackelmann

Heinz Goegelein

Françoise Bono

Michel Aletru

Isabelle Blanc

Valerie Martin

Michael Podeschwa

Cécile Volle-Challier

Valérie Martin

Francoise Gellibert

Francedillaoise Gellibert

Pascale Goberville

Genevieve Dellac

Berangere Thiers

Oliver Duclos

Philippe Beauverger

Patrick Grailhe

Youssef El-ahmad

Bérangère Thiers

Bruno Filoche-RommÉ

Stephen O'CONNOR

Guillaume Bègis

Substituted 6,7-dihydro-5H-benzo[7]annulene compounds, processes for their preparation and therapeutic uses thereof

The present disclosure relates to novel substituted N-(3-fluoropropyl)-pyrrolidine compounds of formula (I-A), wherein R1 and R2 represent independently a hydrogen atom or a deuterium atom; A represents an oxygen or nitrogen atom; and SERM-F represents a selective estrogen receptor modulator fragment comprising an aryl or heteroaryl group linked to the adjacent 'A' group. The disclosure also relates to the preparation and to the therapeutic uses of the compounds of formula (I-A) as inhibitors and degraders of estrogen receptors. 

Substituted N-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof

Compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a &#x2014;COOH, a &#x2014;OH or a &#x2014;OPO(OH)group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a &#x2014;OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a &#x2014;COOH, &#x2014;OH or &#x2014;OPO(OH)group, then R5 represents a hydrogen atom; when R5 represents a &#x2014;OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group;and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.

The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives having Formula (I) as defined herein, their preparation and their therapeutic use.

5 oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives as CaMKII kinase inhibitors for treating cardiovascular diseases

The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Substituted 2-(chroman-6-yloxy)-thiazoles and their use as pharmaceuticals

The present invention relates to derivatives of pyridino-pyridinones, and to their preparation and use thereof, having activity as inhibitors of kinase activity of receptors for PDGF (platelet derived growth factors) ligands and optionally of receptors for the FLT3 (fms-like tyrosine kinase receptor) ligand receptors, said derivatives comprising compounds of formula (I): wherein the various substituent groups are more specifically defined herein. The compounds are suitable as therapeutics for the treatment of various proliferative diseases.

Pyridino-pyridinone derivatives, preparation and therapeutic use thereof

The disclosure relates to method of treating a disease in which VEGFR-3 is involved, comprising administering a therapeutically effective amount of a compound of the formula wherein R, R, R, and Rare as defined in the disclosure, to compositions containing them, to processes for preparing them, and to their use in therapeutics.

Derivatives of 7 alkynyl-1,8 naphthyridones, preparation method thereof and use of same in therapeutics

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 disclosure relates to 7-alkynyl-1,8-naphthyridones of formula (I): wherein R, R, R, and Rare as defined in the disclosure, to compositions containing them, to processes for preparing them, and to their use in therapeutics.

Derivatives of 7-alkynyl-1,8-naphthyridones, preparation method thereof and use of same in therapeutics

The present invention relates to pyridopyridone derivatives of formula (I): in which the variables are as defined herein, to their preparation and to their therapeutic use as inhibitors of the kinase activity of PDGF (platelet-derived growth factor) ligand receptors and possibly of FLT3 (fms-like tyrosine kinase receptor) ligand receptors.

Pyridinopyridinone derivatives, preparation thereof and therapeutic use thereof

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 disclosure relates to compounds of formula (I): wherein R, R, R, and Rare as defined in the disclosure, to compositions containing them, to processes for preparing them, and to their use in therapeutics.

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

Quinolein-2 (1H)-one derivatives as serotonin antagonists

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Paris, France

Gary Mccort