Aventis Pharma S.a.

Sanofi

Sanofi-aventis

Novexel

Youssef El-Ahmad

Michel Tabart

Bruno Filoche-Romme

Jean-Luc Malleron

Frank Halley

Conception Nemecek

Maurice Brollo

Serge Mignani

Baptiste Ronan

Augustin Hittinger

Victor Certal

Hartmut Strobel

Kurt Ritter

Laurent Schio

Dominique Lesuisse

Michel Evers

Sven Ruf

Fabrice Viviani

Gary Mccort

Fabienne Thompson

Corinne Terrier

Monsif Bouaboula

Gilbert Marciniak

Bertrand Vivet

Sylvie Wentzler

Guy Pantel

Corinne Venot

Jean-Christophe Carry

Herve Bouchard

Arielle Genevois-Borella

Jean Bouquerel

Marcel Patek

Gilles Doerflinger

Jacques Mauger

Fahad A Al-Obeidi

Anil Nair

Mark Gabriel Palermo

Jean-Francois Sabuco

Andrees Bohme

Jean-Philippe Letallec

Jean-Francois Peyronel

Philippe Hubert

Thomas Faitg

Gaetan Touyer

Greg Harlow

Corrine Terrier

Didier Bénard

Daniel Bond

Eric Bacque

Antony Bigot

Michel Cheve

Hervé Bouchard

Stefan Guessregen

Jean-Paul Martin

Catherine Souaille

Didier Benard

Eric Bacqué

Bruno Filoche-Rommé

Nicolas Muzet

Anne Olivier

Anne Dagallier

Anne Lebrun

Véronique Zerr

Eric Baque

Axel Ganzhorm

William A Metz

Fahad Al-Obeidi

Sylvie c/o Sanofi-Aventis Département Brevets Wentzler

Jean-François Peyronel

Mark Palermo

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 invention relates to novel pyrimidinone-based heterocyclic compounds which are parasite growth inhibitors, having the general formula (I) in which Y is a morpholine chosen from three bridged morpholines, L is a bond or a linker, n=0 or 1 and Ris a methyl group when n=0 and a hydrogen atom when n=1. Process for the preparation thereof and therapeutic use thereof. 

Pyrimidinone derivatives as antimalarial agents

The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH, ORc, SRc, SORa, SORa, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSORa, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF, CHF, CHF, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.

Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them

Novel compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R, R1, R2, R3, R4, R5, and R6 have the meanings given in the description, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibitors.

Pyrrolo(2,3-b) pyridine derivatives, the preparation and the pharmaceutical use thereof in the form of kinase inhibitors

Compounds of formula (I): wherein Ra, Rb, R, Xand Xare as defined in the disclosure, pharmaceutical compositions comprising said compounds, processes for making and methods of using the same are provided.

Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors

The present invention is related to a compound of formula (I) wherein R1, R2, R3, R4 and X are as defined herein, or an acid-addition salt thereof, its preparation and therapeutic use in the treatment or prevention of diseases involving the Nurr-1 nuclear receptors, also known as NR4A2, NOT, TINUR, RNR-1 and HZF3.

2-benzoylimidazopyridine derivatives, preparation and therapeutic use thereof

The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.

Cyclic urea compounds, preparation thereof and pharmaceutical use thereof as kinase inhibitors

Compounds of formula (I):  wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.

Bis-azaindole derivatives, preparation and pharmaceutical use thereof as kinase inhibitors

The invention relates to compounds of formula (I): in which R1, R2, L, X, R3, A, R4, R', R&#x2033;, R&#x2033;&#x2032;, R5, Y and Lare as herein defined, salts and prodrugs thereof, to their use as protein kinase inhibitors, and to methods of treating diseases comprising adminstration thereof.

The present invention is related to a compound of formula (I): wherein R, R, R, Rand X are as defined herein, or an addition salt with an acid thereof, its pharmaceutical composition or use for treating or preventing diseases involving Nurr-1 nuclear receptors, also known as NR4A2, NOT, TINUR, RNR-1 and HZF3.

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Creteil, France

Youssef El-Ahmad