Societe Civile Bioprojet

Institut National De La Sante Et De La Recherche Medicale

Bioprojet

Societe Civile Bioproject

Other

Thierry Monteil

Denis Danvy

Jean-Charles Schwartz

Jeanne-Marie Lecomte

Pierre Duhamel

Lucette Duhamel

Jean-Christophe Plaquevent

Claude Gros

Nadine Noel

Olivier Chamard

Serge Piettre

Helene Greciet

Christophe Lusson

Nadine Noel-Lefebvre

The invention relates to compounds which constitute a class of medicaments which have an anti-inflammatory activity and which act by inhibiting leukotriene A(LTA), and enzyme which is responsible for the biosynthesis of leukotriene LTB, a major proinflammatory mediator. The invention also relates to therapeutic anti-inflammatory, applications of these compounds as well as for methods of preparing these compounds.

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The invention concerns compounds inhibiting LTAhydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.

LTA4 hydrolase inhibitors

Process for synthesizing N-(mercaptoacyl) amino acid derivatives from alpha-substituted acrylic acids

The invention concerns LTA hydrolase inhibiting compositions of formula (1) as set forth below. It also concerns their therapeutic, in particular anti-inflammatory, applications.

Process for the asymmetric synthesis of S-acyl derivatives of

Process for the synthesis of .alpha.-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II). ##STR1##

Process for the synthesis of .alpha.-substituted acrylic acids and their

Amino acid derivatives of formula (Ia) and (Ib) and pro-drugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.

Amino acids derivatives, the process for their preparation and their

Process for the synthesis of a-substituted acrylic acids and their application. Process for the synthesis of a-substituted acrylic acids of general formula (I) and their application to the synthesis of N- (mercaptoacyl) aminoacid derivatives of formula (II). ##STR1##

Amino acid derivatives having both enkephalinase and ACE inhibiting properties corresponding to the formula: ##STR1##

Amino acid derivatives, the process for their preparation and their

New amino acid derivatives, processes for their preparation, and their therapeutic application are described. These amino acid derivatives correspond to the general formulae ##STR1## These derivatives may be used as medicaments which exhibit an enkephalinase-inhibitory activity.

Amino acid derivatives, processes for their preparation and their

New amino acid derivatives, processes for their preparation and their therapeutic application. Amino acid derivatives corresponding to the general formulae ##STR1## These derivatives may be used as medicaments which exhibit an enkephalinase-inhibitory activity.

Amino acid, derivatives, processes for their preparation and their

Amino acid derivatives of formula (Ia) and (Ib) and prodrugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.

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Saint Georges sur Fontaine, France

Thierry Monteil