Centre National De La Recherche Scientifique

Universitéde Strasbourg

Other

Université Louis Pasteur

Novalyst Discovery

Rhodia Chimie

Ucb S.a.

Aventis Cropscience S.a.

Rhone-poulenc Agro

Centre International De Recherche Aux Frontieres De La Chimie

Inoviem Scientific

Centre International De Recherche Aux Frontieres De La Chime

Syndivia

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

Université Louis Pasteur Strasbourg I

Alain Wagner

Charles Mioskowski

Oleksandr Koniev

Sergii Kolodych

Rachel Decor

Cédric Catala

Marc Schmutz

Virginie Pevere

Luc Quere

Patrice Talaga

Andrew David Griffiths

Jean-Philippe Starck

Sylvain Ursuegui

Matteo Zanda

Anne-Sophie Korganow

Rachid Baati

Frédéric Taran

Pierre Eftekhari

Michael Ryckelynck

Ketty Pernod

Igor Dovgan

Laure Dehuyser

Alexandre Varnek

Christopher Mueller

Sandra De Lamo Marin

Cedric Catala

Evelyne Schaeffer

Jean-Michel Becht

Michel Guyaux

Chimmanamada U Dinesh

Michio Ishibashi

Catherine Sylvain

Frank Hoonakker

Corinne Baehr

Arnaud Gissot

Jean Roger Desmurs

Michaël Ryckelynck

Disclosed is a process for preparation of heterogeneous monodisperse mixtures of protein conjugates with a defined degree of conjugation (1-8) obtained by using a tri-functional reagent allowing affinity concentration followed by subsequent simultaneous release-functionalization.

Bioconjugates with a controlled degree of conjugation, their process of preparation, and the reagents for their preparation

This invention pertains to protein-drug conjugates that may be used in the treatment of cancers and to pharmaceutical compositions containing the same. The protein-drug conjugate has the following formula (I), wherein: L is a cysteine-containing protein residue linked through one or more of the cysteine groups of the protein, Ris selected from the group consisting of arylene, arylene-heteroarylene, heteroarylene-arylene and heteroarylene, n is an integer from 0 to 5, p and q are independently 0 or 1, R, Rand Z are spacers, u is 0 or 1 and T is a cleavable unit sensitive to hydrolases, k is 1 or 2 and D is a cytotoxic drug residue selected from dolastatin residues, which may be identical to or different from each other when k is 2, m is the mean payload-to-protein ratio (PPR) of the conjugate, which ranges from 0.1 to 16. 

Protein-drug conjugates and their use in the treatment of cancers

The present invention relates to a method for capturing a molecular target present in the aqueous phase of a water-in-oil emulsion, said method being based on the use of a binding system comprising (a) a surfactant bearing a functional moiety on its hydrophilic head group and (b) a chemoprobe that acts as a molecular staple between the functionalized surfactant and the molecular target and comprises at least two distinct domains namely (i) at least one capture moiety which is able to specifically bind the molecular target and (ii) at least one binding domain which is able to interact with the functional group of the surfactant through covalent or non-covalent interactions, directly or through a binding intermediary.

Intra-droplet surface engineering to capture a molecular target

The present invention relates to hydroxychloroquine analogues having an activity superior to that of hydroxychloroquine but free from retinal cytotoxicity of formula (I), their pharmaceutically acceptable salts, solvates or hydrates: their method of preparation and their use in the treatment of lupus erythematosus.

Analogues of hydroxychloroquine (HCQ) without retinal toxicity

The present invention relates to a process for labeling compounds comprising thiol moieties with 3-arylpropiolonitrile compounds, to 3-arylpropiolonitrile compounds substituted with tag moieties and to specific 3-arylpropiolonitrile linkers.

3-aryl propiolonitrile compounds for thiol labeling

The present invention relates to new anti-infectious compounds consisting of (i) a polar head having from one to three mannose, dimannose or trimannose moieties, which is coupled through an appropriate linker to (ii) a single lipid chain of at least 17 carbon atoms in length. Pharmaceutical compositions and therapeutic uses thereof are also provided.

Mannosylated compounds useful for the prevention and the treatment of infectious diseases

A computer-based method for identifying at least one pair of similar chemical reactions between a plurality of reactions each related to preparation of at least one product from at least one reagent may include generating for each reaction a structural representation involving dynamic and conventional bonds and, based on the this structural representation, generating for each reaction a set of fragment descriptors of a predetermined length comprising the dynamical bonds and a corresponding descriptor vector. The method may further include calculating similarity indices between descriptor vectors of the plurality of reactions and comparing the similarity indices to identify at least one pair of similar reactions.

Methods for similarity searching of chemical reactions

A method for selecting at least one catalyst from a catalyst library on the basis of the reactivity thereof in a chemical conversion process includes: (a) testing the catalytic activity of a first catalyst from said catalyst library with respect to a reaction medium containing, as the compounds to be converted, at least one reactivity probe having a labeling system and including at least one reaction unit capable of reacting in said chemical conversion; (b) analyzing the reaction medium after said catalytic test for the purpose of qualitatively and/or qualitatively characterizing the resulting compounds; (c) repeating steps (a) and (b) for at least one other catalyst in said library; and (d) comparing the analysis results for each catalyst in order to characterize at least one catalyst having the required reactivity in said chemical conversion.

Method of use for characterizing the catalytic reactivity of catalyst(s)

The invention concerns a method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof of general formula (I), characterized in that it consists in reducing an isoxazole derivative of formula (II) in conditions directly resulting in the derivatives of formula (I), or in obtaining at least a lactone of structure (III) in racemic form(s), or a enantiomerically enriched mixture, followed by opening, in basic conditions, in an aprotic or protic solvent, the desired lactone(s) and, optionally, separating the desired form. The invention is useful for preparing in particular (2S, 3R, 4S)-4-hydroxyisoleucine.

Method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof

The invention concerns quinuclidine derivatives of formula I or II wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention show high affinities for m3 and/or m2 muscarinic receptors and are particularly suited for treating urinary incontinence.

Quinuclidine derivatives processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors

The invention relates to a method for the synthesis of two isomers, at function OH, alone or in mixtures, of amino acids &#x3b1; or the derivatives thereof, having general formula (B), wherein: linkage C&#x2014;O of the 4-position carbon (represented by symbol) denotes one or other of isomers III or IV, or mixtures thereof. Moreover, Rand Rrepresent: a hydrogen atom; or either Ror Rrepresents a hydrogen atom and the other substituent is a radical R, an acyl group &#x2014;COR, such as acetyl, or a functional group &#x2014;COOR, &#x2014;SOR, &#x2014;N (R, R), Rand R, which are identical or different, representing a C1-C12 linear or branched alkyl radical, optionally substituted, an aryl group with one or more aromatic rings and heterocycles, comprising between 5 and 8C, optionally substituted, or aralkyl, the alkyl substituent and the aryl group being as defined above; or Rand Rboth represent a substituent as defined above. Rrepresents a hydrogen atom or Rand Rhas the significance of R. The invention is characterised in that it comprises: the isomerisation of a compound having formula (I), wherein R, R, R, Rand Rare as defined above, such as to produce a compound having formula (II); and the reduction of the carbonyl function thereof which, depending on the catalytic system employed and the formula (I) compound used, produces one of the isomers having general formula (III) or (IV) or a mixture thereof having formula (B). The invention can be used for the synthesis of (2S, 3R, 4S)-4-hydroxyisoleucine.

Method for the synthesis of 4-hydroxyisoleucine and the derivatives thereof

Drugs for preventing and/or treating progressive lesions after organ damage without inhibiting the function of the organ or the regeneration function thereof, by selectively regulating the induction of cytotoxic effecter macrophages which are induced into damaged organ tissues in response to chemokines or cytokines expressed depending on the type of the damaged organ tissues.

Selective preventives/remedies for progressive lesions after organ damage

The invention concerns a method for orthometalation of a carbocyclic aromatic derivative bearing at least an electron donor group, characterised in that it consists in reacting said carbocyclic aromatic derivative with an efficient amount of at least one alkaline metal in the presence of a compound of formula (I): RX, wherein: R represents a hydrocarbon radical having 1 to 20 carbon atoms which can be a saturated or unsaturated, linear or branched, acyclic aliphatic radical; a saturated or unsaturated, monocyclic or polycyclic cycloaliphatic radical; a saturated or unsaturated, linear or branched aliphatic radical bearing a cyclic substituent; and X represents a bromine or chlorine atom.

Method for orthometalation of a carbocyclic aromatic derivative bearing at least an electron donor group

The present invention relates to a method of transforming cells in which an appropriate quantity of nucleic acid fragments is introduced into the cells. The nucleic acid fragments are introduced in the form of a nucleic acid composition comprising a nitrogen-containing silicone, useful for compacting the nucleic acid fragments; the compositions comprise aggregates of nucleic acid fragments and silicones according to the invention.

Nitrogen-containing silicone useful for compacting nucleic acid sequences and use for transforming cells

Growing community of inventors

Strasbourg, France

Alain Wagner