Sanofi

Aventis Pharma S.a.

Ucbbiopharma Srl

Sanofi-Aventis

Hoechst Marion Roussel

Ucb Biopharma Sprl

Lead Pharma Holding B.v.

Lead Pharma B.v.

Laurent Schio

Bruno Filoche-Romme

Frank Halley

Fabienne Thompson

Maurice Brollo

Patrick Fauveau

Victor Certal

Jean-Christophe Carry

Michel Tabart

Youssef El-Ahmad

Gary Mccort

Corinne Terrier

Daniel Christopher Brookings

Martin Clive Hutchings

James Andrew Johnson

Matthew Duncan Selby

Jag Paul Heer

Astrid Markus

Francois Clerc

Joanna Rachel Quincey

Mark Daniel Calmiano

Michel Klich

Teresa De Haro Garcia

Jean Keyaerts

Zhaoning Zhu

Baptiste Ronan

Fabrice Viviani

Michel Cheve

Hervé Minoux

Gilbert Marciniak

Youssef El Ahmad

Bertrand Vivet

Branislav Musicki

Serge Mignani

Malcolm Maccoss

Eric Bacque

David Machnik

Gilles Doerflinger

Jacques Mauger

Eric Didier

Karl Andreas Karlsson

Monsif Bouaboula

Olivier Courtin

Dominique Melon Manguer

Michael Alan Shaw

Yann Foricher

Michael Deligny

Cecile Combeau

Jean-Marc Michel

Mengyang Xuan

Sophie Jadot

Dominique Louis Leon Swinnen

Yves Evrard

Odile Angouillant-Boniface

Patrick Laurin

Annie Clauss

Malcolm Mac Coss

Stephen Hawser

Sylvie Gontier

Gilles Lebourg

Alain Krick

Sylvette Lachaud

Andre Zimmermann

Anil Nair

Alain Corbier

Joseph Maria Gerardus Barbara Cals

Jean-Francois Sabuco

Sander Bernardus Nabuurs

Marie-Pierre Cherrier

Kirsten Bjergarde

Cécile Combeau

François Clerc

Stéphanie Deprets

Dominique Louis Léon Swinnen

Nathalie Pietre-Dischamp

Pascale Vicat

Arlette Dussarat

Fabienne Chatreaux

Eric Parmantier

Georges Delettre

Nina Ma

Youssef El-ahmad

Dominique Louis Swinnen

Joseph Maria Cals

Bruno Filoche-RommÉ

André Zimmermann

A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6, 7-dihydro-7, 14-methanobenzimidazo[1, 2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.

Fused pentacyclic imidazole derivatives

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

A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs 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.

Novel compounds according to Formula I Meta or para or a pharmaceutically acceptable salt thereof wherein:A-Aare N or CR, CR, CR, CR, respectively, with the proviso that no more than two of the four positions A in A-Acan be simultaneously N; A, A, A, A, Aare N or CR, CR, CR, CR, CR, respectively, with the proviso that at least one but no more than two of the five positions A in A, A, A, A, Ais N; Ris C(2-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, (di)C(3-6)cycloalkylamino or (di)(C(3-6)cycloalkylC(1-3)alkyl)amino; Ris H, hydroxyethyl, methoxyethyl, C(1-6)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl; the sulfonyl group with Ris represented by one of R, Ror R; Ris H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkyl-C(1-3)alkyl; and Ris C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkyl-C(1-3)alkyl.

ROR gamma (ROR&#x3b3;) modulators

The invention relates to a compound of formula (I), more specifically in the levorotatory form (1a) thereof, in particular the form having a rotatory power [&#x3b1;]D=&#x2212;38.6+0.7 at a concentration of 0.698 mg/ml in methanol. The compound may be in the form of a base or an acid addition salt, in particular a pharmaceutically acceptable acid. The compound is a selective Aurora A and B kinase inhibitor and can be used as an anticancer drug.

Anti-cancer compound and pharmaceutical composition containing the same

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 a compound of formula (I), more specifically in the levorotatory form (1a) thereof, in particular the form having a rotatory power [&#x3b1;]D=&#x2212;38.6+0.7 at a concentration of 0.698 mg/ml in methanol. The compound may be in the form of a base or an acid addition salt, in particular a pharmaceutically acceptable acid. The compound is a selective Aurora A and B kinase inhibitor and can be used as an anticancer drug. 

The invention relates to the novel materials of formula (I), wherein each of the substituents R, R1, R2, R3, R4 and R5 is as defined herein. The materials are useful as inhibitors of AKT(PKB) phosphorylation.

(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives, preparation thereof and pharmaceutical use thereof as AKT(PKB) phosphorylation inhibitors

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

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Paris, France

Laurent Schio