Solvay (societe Anonyme)

Solvay Sa

Solvay

Alba Therapeutics Corporation

Peptisyntha

Corden Pharma Brussels Pc

Georges Blondeel

Roland Callens

Frank Becu

Marc Anteunis

Thierry Delplanche

Laurent Jeannin

Cyrille Pousset

Ronan Gire

A process for the manufacture of peptide Omiganan in solution phase. Novel intermediates in the process for the manufacture of Omiganan and processes for the manufacture of these intermediates.

Peptide manufacturing process

The invention provides crystalline forms of the peptide Gly-Gly-Val-Leu-Val-Gln-Pro-Gly (SEQ ID NO 1), and salts of the peptide, which may further have associated water molecules. These salts and hydrated salts of the peptide and compositions comprising these materials have advantageous pharmaceutical properties.

Larazotide acetate compositions

Process for the manufacture of an enantiopure compound comprising at least one functional group capable of reacting with an activated carboxyl group, starting from a mixture of enantiomers of the said compound, in which process: (a) a reaction medium comprising the mixture of enantiomers and a reagent based on an enantiopure amino acid, in which reagent at least one amino group of the amino acid is protected by a protective group and in which reagent at least one carboxyl group of the amino acid is activated, is subjected to conditions appropriate for bringing about the reaction of the functional group capable of reacting with the activated carboxyl group with the activated carboxyl group, so as to form a carbonyl bond; (b) the mixture of diastereomers obtained is subjected to a separation operation, so as to obtain at least one fraction composed essentially of a diastereomer, (c) at least a portion of the said fraction is subjected to a stage of cleavage of the carbonyl bond under conditions under which the protective group is essentially stable; and (d) the enantiopure compound and an enantiopure derivative of the amino acid in which at least one amino group is protected by the protective group are recovered.

Process for the manufacture of an enantiopure compound

Ureins are obtained by reaction, in basic medium, between an N-(aryloxycarbonyl)diamino acid and a compound containing a free amino group. The chirality of the compounds is outstandingly well preserved.

Ureins derived from &#x3b1;, &#x3c9;, diamino acids and process for their preparation

Ureins are obtained by reaction, in basic medium, between an N,-(aryloxycarbonyl)diamino acid and a compound containing a free amino group. The chirality of the compounds is outstandingly well preserved.

Ureins derived from &agr;, &ohgr;-diamino acids and process for their preparation

Ureins are obtained by reaction, in basic medium, between an N.sup..omega. -(aryloxycarbonyl)diamino acid and a compound containing a free amino group. The chirality of the compounds is outstandingly well preserved.

Ureins derived from alpha, omega-diamono acids and process for their

Compounds having the general formula: ##STR1## in which R3 represents an aryl group which is unsubstituted or substituted by one or more alkyl groups containing 1 to 4 carbon atoms; R4 represents a hydrogen atom, a group for protecting the amino functional group, an amino acid or a peptide some of whose functional groups are optionally substituted by a protecting group or by an activating group; R5 represents a hydroxy group, a halogen atom, a group for protecting the carboxyl functional group, an activating group, an amino group, an amino acid or a peptide some of whose functional groups are optionally substituted by a protecting group or by an activating group; and n is an integer from 1 to 10.

N-aryloxycarbonyl amino acids and peptides and their derivatives

An .alpha.-amino acid amide is prepared by reaction of an N.sup..alpha. -aryloxycarbonylamino acid with a compound containing a free amino group. This process makes it possible readily to prepare peptides, by direct reaction between the carboxyl group of the N.sup..alpha. -aryloxycarbonyl derivative of an amino acid and the free amino group of a second amino acid or of a peptide fragment, without requiring protection of the carboxyl function of the second amino acid or of the peptide fragment, nor a coupling agent nor a deprotection step.

Growing community of inventors

Aalst, Belgium

Georges Blondeel