Aventis Pharma S.a.

Sanofi

Rhone-poulenc Rorer S.a.

Sanofi-aventis

Rhone-poulenc Sante

Sanofi-a Ventis Deutschland Gmbh

Novexel

Novexel Sa

Michel Tabart

Fabrice Viviani

Serge Mignani

Jean-Luc Malleron

Frank Halley

Eric Bacque

Baptiste Ronan

Catherine Souaille

Youssef El-Ahmad

Jean-Francois Peyronel

Daniel Achard

Fabienne Thompson

Jean-Christophe Carry

Antony Bigot

Claude Moutonnier

Michel Evers

Bruno Filoche-Romme

Serge Grisoni

Alain Truchon

Youssef El Ahmad

Laurent Schio

Marcel Patek

Gary Mccort

Pascal Desmazeau

Anil Nair

Maurice Brollo

Corinne Terrier

Victor Certal

Patrick Mailliet

Michel Cheve

Jacques Mauger

Marie-Christine Dubroeucq

Claude Guyon

Dominique Damour

Hervé Bouchard

Francois Clerc

Bernard Baudoin

Herve Bouchard

Arielle Genevois-Borella

Conception Nemecek

Martin Smrcina

Vincent Leroy

Eric Nicolai

Jean-Paul Martin

Bertrand Vivet

Kirsten Bjergarde

Monsif Bouaboula

Mark Dodson

Sylvie Wentzler

Laurence Gauzy-Lazo

Guy Pantel

Eric Bacqué

Guy Picaut

Philippe Girard

Jean-Philippe Letallec

Marie-Pierre Cherrier

Philippe Hubert

St&eacute;phane Mutti

Jean-Francedillaois Peyronel

Stephen Hanessian

Teresa Damiano

Pascal Billot

Odile Angouillant-Boniface

Antonio Ugolini

Eykmar Fett

Christophe Daubi&eacute;

Eric Bacqu&eacute;

Jean-Fran&ccedil;ois Desconclois

Pierre Yves Abecassis

Bruno Filoche-Rommé

Alain Le Brun

Cécile Combeau

Carole Neves

Michel Kryvenko

Bernd Janocha

Sylvaine Lafont

Christian Wehrey

Jacques Bourget

Marc Antoine Perrin

Eric Baque

Marc Pierre Lavergne

Martha Ackerman-Berrier

Evelyne James-Surcouf

Anne Morgat

Jean-Francedillaois Sabuco

Alain Rabion

Youssef El-ahmad

Sabine Boisnard

Bruno Filoche-RommÉ

Pierre-Yves Abecassis

Herein is provided a novel process for the preparation of methyl 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylate by a Suzuki coupling of compound (3), wherein LG represents a leaving group, with an organoboron reagent: Compound (3) is obtained by activation of compound (4) with a leaving group LG, and compound (4) is obtained by alpha-arylation of methyl 5-oxo-6,7,8,9-tetrahydro-5H-benzo[7]annulene-2-carboxylate with 1-LG'-2,4-dichlorobenzene, wherein LG′ represents a leaving group:

Process for the preparation of methyl 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylate

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 disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R, R, R, Ra, Rb, and Rare as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.

Substituted pyrazoles, compositions containing these, method of production and use

The invention relates to pyrazole derivatives of general formula (I): in which X represents chlorine or fluorine; to a process for preparing said derivatives, and to therapeutic uses of said derivatives.

Pyrazole derivatives, preparation thereof, and therapeutic use thereof

The disclosure relates to compounds of formula (I): which modulate the activity of proteins, particularly kinases, and to compositions containing the same, and to the use thereof as medicaments, in particular as anticancer agents.

7-substituted aza-indazoles, compositions containing same, production method and use thereof

The disclosure relates to substituted pyrazolo-pyridines, compositions containing them, methods for the production thereof, and to their use as medicaments, in particular, as anticancer agents.

Substituted pyrazolopyridines, compositions containing them, method for the production thereof, and their use

The invention relates to compounds of formula (I): wherein Ra, R1, Ar, L, A, W, Y, and Z are as defined in the disclosure; to compositions containing them; and to the preparation and use thereof, in particular as anticancer agents.

Substituted pyrrolopyridines, compositions containing them, manufacturing process therefor and use thereof

The disclosure concerns substituted pyrroles of formula (I): wherein A, L, Ar, R1, R2, R5, and Ra are as defined in the disclosure, compositions containing the same, methods for making the same and uses thereof, in particular as anti-cancer agents.

Substituted pyrroles, compositions containing same, method for making same and use thereof

Compounds of formula (I): wherein R1, R5, R6, R7, Ar, L, A, and Q are as defined in the description, and to salts thereof, to compositions containing them, to the process for preparing them, and to their use as medicinal products, in particular as anticancer agents.

Substituted indoles, compositions containing them, method for the production thereof and their use

The disclosure concerns substituted imidazoles and pyrroles, compositions containing the same, the preparation thereof, and the use thereof as medicaments, particularly as anti-cancer agents.

Substituted pyrroles and imidazoles, compositions containing same, manufacturing process therefor and use thereof

Growing community of inventors

La Norville, France

Michel Tabart