Societe Civile Bioprojet

Institut National De La Sante Et De La Recherche Medicale

Other

Bioprojet

Societe Civile Bioproject

Claude Gros

Jean-Charles Schwartz

Jeanne-Marie Lecomte

Pierre Duhamel

Lucette Duhamel

Denis Danvy

Jean-Christophe Plaquevent

Thierry Monteil

Nadine Noel

Bruno Giros

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.

[object Object]

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

LTA4 hydrolase inhibitors

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

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.

The (R) or (S) isomer of acetorphan or N-/(acetylthiomethyl)-2-oxo-1-phenyl-3-propyl/(S) alanine methyl ester is prepared by splitting of racemic acetylthio-3-benzyl-2-propanoic acid by reaction with ephedrin, separation of the enantiomeric salt obtained, then freeing of the acid and coupling with the corresponding amino acid ester. The obtained preparations possess remarkable therapeutic activities and can notably be used as drugs.

Thioester enantiomeric compounds and their therapeutic uses

The (R) or (S) isomer of acetorphan or N-/2-acetylthiomethyl)-1-oxo-3-phenylpropyl/(S) alanine methyl ester is prepared by splitting of racemic acetylthio-2-benzylpropanoic acid by reaction with ephedrin, separation of the enantiomeric salt obtained, then freeing of the acid and coupling with the corresponding amino acid ester. The obtained preparations possess remarkable therapeutic activities and can notably be used as drugs.

The (R) or (S) isomer of acetorphan or N-12-acetylthiomethyl-1-oxo-3-phenyl propyl/(S) alanine methyl ester is prepared by splitting of racemic 3-acetylthio-2-benzyl propanoic acid by reaction with ephedrin, separation of the enantiomeric salt obtained, then freeing of the acid and coupling with the corresponding amino acid ester. The obtained preparations possess remarkable therapeutic activities and can notably be used as drugs.

Growing community of inventors

Paris, France

Claude Gros