Abstract: 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.

Abstract: 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, R1 is 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, R2, R3 and 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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, R1 is 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, R2, R3 and 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.

Abstract: The present invention relates to the use of iminosydnone compounds in processes for the preparation of conjugates of two compounds of interest. The invention further relates to the use of said iminosydnone compounds in a process for releasing a compound of interest. The invention finally relates to novel iminosydnone compounds.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: The present invention relates to the use of iminosydnone compounds in processes for the preparation of conjugates of two compounds of interest. The invention further relates to the use of said iminosydnone compounds in a process for releasing a compound of interest. The invention finally relates to novel iminosydnone compounds.

Abstract: The present invention relates to a process for the preparation of a first compound of interest C1 functionalized with a sydnone compound and to the corresponding functionalized C1 compound of interest. The present invention also relates to a process for the preparation of a conjugate of two compounds of interest C1 and C2 implying a sydnone compound and to the obtained conjugate. The present invention also relates to a process for preparing a compound of interest C2 comprising a strained alkyne moiety functionalized with a sydnone and to the corresponding functionalized compound of interest C2. It also relates to novel sydnone compounds substituted in position 4, which may be used in the above processes.

Abstract: 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.

Abstract: 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.

Abstract: 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 of length. Pharmaceutical compositions and therapeutic uses thereof are also provided.

Abstract: 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.

Abstract: 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.