Centre National De La Recherche Scientifique

Universitè De Montpellier

Sanofi

University of Montpellier II

Societe Nationale Des Poudres Et Explosifs

Zentaris Gmbh

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

Institut National De La Sante Et De La Recherche Medicale

Societe De Conseils De Recherches Et D'applications Scientifiques (s.c.r.a.s.)

Uniwersytet Jagiellonski

Université Montpellier 2 Sciences Et Techniques

Aeterna Zentaris Gmbh

Ecole Nationale Superieure De Chimie De Montpellier

Centre National De La Recherche Scientifique-cnrs

Centre Hospitalier Universitaire De Montpellier

Jean Martinez

Gilles Subra

Bertrand Castro

Henri Demarne

Anne-Marie Pinel

Jean-Alain Fehrentz

Jean-Pierre Bali

Frédéric Lamaty

Jean-Pierre G Senet

Gerard Sennyey

Gerard Barcelo

Richard Magous

Luc Demange

Maciej Pawlowski

Mahmoud Jaouadi

Daniel Perrissoud

Aline Moulin

Damien Boeglin

Pascal Verdie

Pascaline Dubs

Pawel Zajdel

Michel Hocquaux

Matthias Gerlach

Christophe Thurieau

Dino Nisato

Michael Teifel

Klaus Paulini

Eric Ferrandis

Peter Schmidt

Ahmad Mehdi

Marcel Garcia

Gilbert Mueller

Babette Aicher

Marie Maynadier

Lars Blumenstein

Anna Wesolowska

Grzegorz Satala

Anne-Laure Blayo

José-Antonio Camara Y Ferrer

Andrzej J Bojarski

Christian Jorgensen

Anna Partyka

Guillaume Laconde

Muriel Amblard-Caussil

Florence Apparailly-Sechan

Piotr Popik

Georges Dewynter

Tomasz Kos

Daniel Farran

Cyril Dreyfus

David Pignol

Pascal Arnoux

Evelina Colacino

Florine Cavelier

Isabelle Duroux-Richard

Xavier Bantreil

Manuel Larrouy

Mathieu Bibian

Muriel Caussil-Amblard

Julien Tailhades

Muriel Amblard

Valérie Declerck

Benjamin Gallard

Katarzyna Grychowska

Lubomir Vezenkov

Yves Yeboue

Saïd Jebors

Nicolas Le Moigne

Jean-Francois Hernandez

Thomas-Xavier Metro

Jean-françois Hernandez

Cécile Echalier

Sonia Cantel

Michèle Cristau

Wesolowska Anna

Gilbert MÜLLER

Olivier Besnard

A continuous, solvent-free and non-enzymatic method for synthesizing a compound of formula (I): Ra-POLYPEP-Rc (I) wherein: POLYPEP is a poly-amino acid compound, Ra and Rc are as specified, the method including the steps of: a) feeding an extrusion reactor with (1) a compound of formula (II) Ra-PEPNt-Rg (II) wherein; PEPNt is a mono- or a poly-amino acid compound, Ra and Rg are as specified, and (2) a compound of formula (III) H-PEPCt-Rc (III) wherein: PEPCt is a mono- or a poly-amino acid compound, and Rc is as defined in the absence of any solvent, so that the compound of formula (II) and the compound of formula (III) react together for generating a compound of formula (I), and b) collecting the compound of formula (I) from the extrusion reactor.

Continuous, solvent-free and non-enzymatic peptide synthesis by reactive extrusion

The present invention relates to peptidomimetic macrocycles comprising at least one macrocycle-forming linker and an amino acid sequence chosen from the group consisting of: i) an amino acid sequence with at least about 50%, 60%, 70%, 80%, 90%, or 95% sequence identity to a human sequence IRAK2 54-71 (SEQ ID No1) and 100% identity with the amino acids in the positions 5-6, 9-11, 14-15 or ii) an amino acid sequence with at least about 50%, 60%, 70, 80%, 90%, or 95% sequence identity to a human sequence IRAKM 66-83 (SEQ ID No2) and 100% identity with the amino acids in the positions 5-6, 9-11, 13-14, wherein the peptidomimetic macrocycle comprises an a-helix and at least two natural or two non-natural amino acids crosslinked by a macrocycle-forming linker. It also concerns method of preparation of said peptidomimetic macrocycles and uses thereof, pharmaceutical composition and uses thereof, in particular as inhibitors of inflammatory pathways.

Stapled peptides and uses thereof

The present invention relates to new biopolymer, i.e. bioorganic nylons incorporating peptidic blocks obtained by a process of polymerization of amino peptidic blocks. The process of the invention comprises the steps of mixing amino peptidic blocks with or without a diaminoalcane and reacting the mixture according to polycondensation with a diacyl chloride in homogeneous or heterogeneous media.

Process for preparation of bioorganic nylon polymers and their use as antibacterial material

This invention concerns pyrroloquinoline derivatives as antagonists of 5-HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in schizophrenia, anxiety, depression, maniac depression, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, panic attacks, attention deficit hyperactivity disorder, attention deficit disorder, Parkinson's disease, Huntington's disease, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, obesity and type-2 diabetes, functional bowel disorder, Irritable Bowel Syndrome. The compounds have the general formula (XIV), wherein the symbols have the meanings given in the description.

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The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O&#x2014;N acyl shift enabling to obtain the corresponding peptide alcohols.

Solid phase peptide synthesis of peptide alcohols

The invention relates to the use of oligomers having constrained dipeptide or tripeptide motifs as agents for the vectorization of active ingredients.

Use of constrained peptide mimic oligomers as vectorization agents

The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and/or long term regulation of energy balance; short-, medium- and/or long term regulation (stimulation and/or inhibition) of food intake; adipogenesis, adiposity and/or obesity; body weight gain and/or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).

Triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors

The disclosure relates to a method for the synthesis of a compound of the following formula (I) in which: R1 and R2 are independently an N-protective group; R3 is a hydrogen atom, a C-Calkyl group, a C-Carylalkyl group, a C-Calkenyl group, or a alkoxycarbonylalkyl group; Y is a &#x2014;C(HR4)- group in which R4 is a hydrogen atom, a C-Calkyl group, an aryl group, a C-Carylalkyl group, or a C-Calkenyl group; or an orthophenylene group.

Transannular rearrangement of activated lactams

The invention relates to a nicotianamine derivative and to a process for chemical or enzymatic synthesis thereof. The nicotianamine derivative has the following formula (I). The invention finds use in the pharmacy field in particular. 

Nicotianamine-derived metallophore and processes for producing same

The present invention relates to a pipecolic linker and its use as a solid-phase linker in organic synthesis. Said pipecolic solid-phase linker may be used for coupling functional groups chosen between primary amines, secondary amines, aromatic amines, alcohols, phenols and thiols. In particular, said pipecolic solid-phase linker may be used for peptide or pseudopeptide synthesis, such as the reverse N to C peptide synthesis or the retro-inverso peptide synthesis, or for the synthesis of small organic molecules.

Pipecolic linker and its use for chemistry on solid support

The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular alcohol disorder, drug abuse, growth retardation, cachexia, short-, medium-, and/or long term regulation of energy balance, short-, medium-, and/or long term regulation (stimulation and/or inhibition) of food intake, intake of rewarding food, adipogenesis, adiposity and/or obesity, body weight gain and/or reduction, diabetes, diabetes type I, diabetes type II, tumor cell proliferation, inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).

Triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors

The invention relates to a dipeptide conjugate having general formula I, AA2-AA1-NH, wherein A represent the radical corresponding to a monocarboxylic acid with general formula II, HOOC&#x2014;R, in which: R represents a linear or branched aliphatic radical at C-C, which is optionally substituted by a hydroxyl group and which can comprise one or more unsaturations, preferably between 1 and 6 unsaturations, and/or which can comprise a phenyl group or lipoic acid or the reduced form thereof, dihydrolipoic acid or N-lipoyllysine; and AA1 and AA2 represent identical or different amino acids which are selected from the group containing Ala, Asn, Cys, Gln, Gly, Ile, Leu, Met, Phe, Pro, Ser, Thr, Trp, Tyr, Val, Asp, Glu, Arg, His, Lys, Orn, Dap, Dab, the corresponding homo-amino acids and the corresponding beta-amino acids in the form of enantiomers or diastereoisomers and mixtures thereof, including racemic mixtures.

&#x3b1;-MSH-antagonist dipeptide conjugates

The invention relates to a tripeptide conjugate having general formula I, A-AA1-AA2-AA3-NH, wherein A represents the radical corresponding to a monocarboxylic acid with general formula II, HOOC&#x2014;R, in which: R represents a linear or branched aliphatic radical at C-C, which is optionally substituted by a hydroxyl group and which can comprise one or more unsaturations, preferably between 1 and 6 unsaturations, lipoic acid or the reduced form thereof, dihydrolipoic acid, N-lipoyllysine, or phenylbutyric acid; and AA1, AA2 and AA3, which may be identical or different, represent independently of each other an amino acid selected from His, Phe, Ala, Arg, Lys, Orn, Trp, Nap, Tpi and Tic, on the condition that at least one of AA1, AA2 or AA3 represent Phe, preferably Dphe in the form of enantiomers or diastereoisomers and mixtures thereof, including racemic mixtures.

MSH-agonist tripeptide conjugates

The disclosure relates to a method for the synthesis of a compound of the formula (I) in which: n is an integer higher than or equal to 1; Rb and each Rn are independently a hydrogen atom, a C-Carylalkyl group or a C-Calkyl group substituted or not by an aryl group, &#x2014;COOH, C-C, &#x2014;COO-(alkyl), &#x2014;CONH, &#x2014;SH, heteroaryl, &#x2014;NH, &#x2014;NHC(NH)(NH), C-C-s-(alkyl), &#x2014;OH or phenol; Ra is a N-protective group; Rc is a ORd group in which Rd is a C-Calkyl group or a NReRf group in which Re and Rf Re independently an N-protective group.

Method for the synthesis of peptides without solvent

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Caux, France

Jean Martinez