Sanofi-aventis

Sanofi

Sanofi-synthelabo

Commissariat &#xc0; L'&#xc9;nergie Atomique Et Aux &#xc9;nergies Alternatives

Commissariat a L'energie Atomique

Frank Marguet

Jacques Froissant

Frederic Puech

Benoit Marabout

Mireille Sevrin

Philippe Burnier

Frédéric Puech

Yannick Evanno

Elisabetta Bianchi

Olivier Duclos

Alessia Santoprete

Antoine Ravet

Stéphane Illiano

Paola Magotti

Christophe Pacaud

Beno&icirc;t Marabout

Jean-Francois Gibert

Laurent Dubois

Christian Hoornaert

Ahmed Abouabdellah

Antonio Almario Garcia

Sergio Mallart

Raffaele Ingenito

Claire Minoletti-Hochepied

Luc Even

Thomas Rooney

Benoît Marabout

Catherine Gille

Bertrand Tavitian

Jean Jeunesse

Sylvain Cote Des Combes

Badia Ferzaz

Jesus Benavides

Phikip Janiak

J&eacute;sus Benavides

Dorothee Cheuret

R&eacute;gine Bartsch

Anne Olivier-Bandini

Sylvain Cote-Des-Combes

Regine Bartsch

R&eacute;gine Bartsch-Li

Frédéric c/o Sanofi-Aventis Département Brevets Puech

Cyrille Thominiaux

Annelaure Damont

Frédéric Dolle

Hervé Boutin

Dorothée Cheuret

Régine Bartsch

Marie-Noelle Castel

Herve Boutin

Marie-Noëlle Castel

Provided is a biologically active single chain Relaxin peptide having the following formula (I):N-Ac-(E)-X-E-G-R-E-X-V-R-X-X-I-X-X-E-G-X-S-X-X-X-X-R-(X)-(X)-(K)-(X)-(gE)-X-C; or a salt or solvate thereof. Also provided is a pharmaceutical composition comprising at least one peptide of the invention, and the peptide or the pharmaceutical composition for its use as a medicament.

Modified lipidated Relaxin B chain peptides and their therapeutic use

Provided is a biologically active single chain Relaxin peptide having the following formula (I): N-X-(E)-X-E-G-R-E-X-V-R-X-X-I-X-X-E-G-X-S-X-X-X-X-R-(X)-(X)-(X)-NH-C. Also provided is a pharmaceutical composition comprising at least one peptide of the invention, or a pharmaceutically acceptable salt or a solvate thereof. Further provided is the peptide, a pharmaceutically acceptable salt or solvate thereof, or the pharmaceutical composition for use as a medicament.

Modified relaxin B chain peptides and their therapeutic use

Compounds corresponding to the general formula (I) wherein Rrepresents a group C-alkyl, C-cycloalkyl, C-cycloalkyl-C-alkyl, C-alkyl-C-cycloalkyl, C-cycloalkyl-C-cycloalkyl, C-alkylthio-C--alkyl, C-alkoxy-C-alkyl, hydroxy-C-alkyl, hydroxy-C-alkyl-C-cycloalkyl-C-alkyl, hydroxy-C-cycloalkyl, C-fluoroalkyl or C-fluorocycloalkyl; an optionally substituted heterocyclic group; a group C-alkyl substituted with an optionally substituted heterocyclic group; Xrepresents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C-alkyl, C-cycloalkyl, C-cycloalkyl-C-alkyl, C-fluoroalkyl or cyano; and Rrepresents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents,in the form of the base or of an acid-addition salt, and the therapeutic use thereof.

3,4-dihydropyrrolo[1,2-A]pyrazine-2,8(1H)-dicarboxamide derivatives, preparation thereof and therapeutic use thereof for diseases involving casein kinase 1 epsilon and/or casein kinase 1 delta

The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which:

Hexafluoroisopropyl carbamate derivatives, their preparation and their therapeutic application

Compounds corresponding to the general formula (I) 

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A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom;Rrepresents a hydrogen atom or a (C-C)alkyl group; Rand Reach represent, independently of one another, a hydrogen atom or a (C-C)alkyl group or else Rand Rform, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C-C) alkyl or (C-C) alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.

3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use

The invention concerns compounds of general formula (I): Wherein n, X, Y, Rand Rare as defined herein. The invention also concerns a method for preparing the compounds and their therapeutic use.

1H-pyrimido[4,5-b]indole derivatives, their preparation and therapeutic use

The invention discloses and claims therapeutic uses of compounds of general formula (I) Wherein X, R, Rand Rare as described herein. The invention further discloses processes for preparing them, and novel intermediates therefor.

3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b]indole-1-acetamide derivatives, their preparation and their application in therapeutics

A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; Rrepresents a hydrogen atom or a (C-C)alkyl group; Rand Reach represent, independently of one another, a hydrogen atom or a (C-C)alkyl group or else Rand Rform, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C-C)alkyl or (C-C)alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.

The invention provides compounds of general formula (I) in whichX represents a hydrogen or halogen atom; Rrepresents a hydrogen atom or a (C-C)alkyl group; Rand Reach independently of one another represent a hydrogen atom or a (C-C)alkyl group, or else Rand R, together with the nitrogen atom bearing them, form a pyrrolidinyl, piperidinyl, morpholinyl or 4-(C-C)alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type which may carry one or more halogen atoms and/or one or more (C-C)alkyl and/or (C-C)alkoxy groups; in the form of bases, addition salts with acids, solvates or hydrates; the pharmaceutical compositions comprising them, processes for preparing them, and synthesis intermediates.

3-heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b] indole-1-acetamide derivatives, preparation and use thereof in medicaments

The invention concerns compounds of general formula (I), wherein: X represents a hydrogen or halogen atom; Rrepresents a hydrogen atom or a (C&#x2013;C)alkyl group; Rand R, represent each, independently of each other, a hydrogen atom or a (C&#x2013;C)alkyl group, or Rand Rform, with the atom which bears them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl, pyridazinyl type, the heteroaromatic group may represent one or several halogen atoms and/or one or several (C&#x2013;C)alkyl, (C&#x2013;C)alkoxyl groups; in the form of bases, addition salts to acids, solvates or hydrates. The invention also concerns pharmaceutical compositions containing same, methods for preparing same and synthesis intermediates 

3-heteroaryl-3, 5-dihydro-4-oxo-4H-pyridazino[4, 5-b]indole-1-carboxamide derivatives their preparations and therapeutic use

4-Oxo-3,5-dihydro-4H-pyridazino&lsqb;4,5-b&rsqb;indole-1-carboxamide derivatives having affinity for the peripheral benzodiazepine receptors are useful for the prevention or treatment of peripheral neuropathies and for the treatment of central neurogenerative diseases.

4-oxo-3,5-dihydro-4H-pyridazino&lsqb;4,5-b&rsqb;indole-1-carboxamide derivatives, preparation and therapeutic use

Pyridazino&lsqb;4,5-b&rsqb;indole-1-acetamide derivatives for the prevention or treatment of diseases linked to the dysfunctioning of peripheral-type benzodiazepine receptors.

Use of pyridazino&lsqb;4,5-b&rsqb;indole-1-acetamide derivatives for preparing medicines for treating diseases related to the dysfunction of peripheral benzodiazepin receptors

4-Oxo-3,5-dihydro-4H-pyridazino&lsqb;4,5-b&rsqb;-indole-1-acetamide derivatives, their preparation and their application in therapy

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Verrieres le Buisson, France

Frank Marguet