Sanofi

Aventis Pharma S.a.

Maurice Brollo

Bruno Filoche-Romme

Frank Halley

Laurent Schio

Youssef El-Ahmad

Baptiste Ronan

Victor Certal

Michel Tabart

Gary Mccort

Fabienne Thompson

Corinne Terrier

Gilbert Marciniak

Youssef El Ahmad

Bertrand Vivet

Monsif Bouaboula

Karl Andreas Karlsson

Jean-Philippe Letallec

Fabrice Viviani

Annie Clauss

Andre Zimmermann

Jean-Christophe Carry

Eric Bacque

Gilles Doerflinger

Eric Didier

Hervé Minoux

Marie-Pierre Cherrier

Odile Angouillant-Boniface

François Clerc

Jacques Clement

Jerome Arigon

Jean-Robert Labrosse

Florence Durand

Romain Combet

Eric Parmantier

Youssef El-ahmad

Jérome Arigon

Bruno Filoche-RommÉ

André Zimmermann

The invention relates to the novel products of formula (I): with p, q=0, 1 or 2; R1=phenyl, pyridyl; &#x2014;(CH)&#x2014;Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; &#x2014;SO&#x2014;Rb; &#x2014;CO&#x2014;Re; m=1 or 2; Ra=aryl, heteroaryl, &#x2014;CO-cycloalkyl, &#x2014;CO-heterocycloalkyl, &#x2014;CO&#x2014;Rb, &#x2014;C(Rb)&#x2550;N&#x2014;ORc, &#x2014;CORd, &#x2014;CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CHor CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is and the isomer of configuration R,R these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.

2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one and this 1,2,3,4-tetrahydropyrimido{1,2-a}pyrimidin-6-one derivatives comprising a substituted morpholine, preparation thereof and pharmaceutical use thereof

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 invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; &#x2014;(CH)&#x2014;Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; &#x2014;SO&#x2014;Rb; &#x2014;CO&#x2014;Re; m=1 or 2; Ra=aryl, heteroaryl, &#x2014;CO-cycloalkyl, &#x2014;CO-heterocycloalkyl, &#x2014;CO&#x2014;Rb, &#x2014;C(Rb)&#x2550;N&#x2014;ORc, &#x2014;CO 2 Rd, &#x2014;CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CHor CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments. 

2,3-dihydro-1H-imidazo{1,2-a}pyrimidin-5-one and this 1,2,3,4-tetrahydropyrimido{1,2-a}pyrimidin-6-one derivatives comprising a substituted morpholine, preparation thereof and pharmaceutical use thereof

The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.

Pyrimidine derivatives, preparation thereof, and pharmaceutical use thereof as akt(pkb) phosphorylation inhibitors

The disclosure relates to compounds of formula (I): wherein R, R, R, R, and Rare as defined in the disclosure, to the compositions containing them and to the use thereof as medicaments, in particular as anticancer agents. The disclosure also relates to the process for preparing the compounds of formula (I) and to reaction intermediates.

Pyrazolylbenzimidazole derivatives, compositions containing them and use thereof

The invention relates to compounds of the formula:  or their racemic, enantiomeric or diastereoisomeric isomers, or pharmaceutically acceptable salts of the compounds of formula I or the racemic, enantiomeric or diasteroisomeric isomers.

1,2,3,4-tetrahydro-pyrimido(1,2-a)pyrimidin-6-one derivatives, preparation thereof, and pharmaceutical use thereof

The invention relates to a product of formula (I) where R1, R2, R3, and R4 are as defined herein, the therapeutic use of the product, a process to make the product, and a pharmaceutical composition comprising the product.

2,3-dihydro-1H-imidazo(1,2-a)pyrimidin-5-one derivatives, preparation thereof, and pharmaceutical use thereof

The invention relates to novel products of formula (Ia) or (Ib): 

Pyrimidinone derivatives, preparation thereof and pharmaceutical use thereof

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Paris, France

Maurice Brollo