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Eni-ente Nazionale Idrocarburi

Ente Nazionale Idrocarburi

Massimo Pinori

Antonio S Verdini

Paolo Mascagni

Flavio Leoni

Silvana Cappelletti

Laura Gazerro

Felice Centini

Rocco Mazzaferro

Gianni Gromo

Romano Di Trapani

Barbara Vergani

Maria Lattanzio

Daniela Modena

Patrizia Caretto

Fabrizio Marcucci

Andrea Vitali

Non-selective somatostatin analogues

Alpha-amino acid derivatives with antiinflammatory activity

The present invention relates to novel compounds, of the general formula (I), the N-oxide forms thereof, the salts thereof with pharmaceutically acceptable acids and the stereochemical isomers thereof, which are useful as antifungal agents; to pharmaceutical compositions containing such compounds as the active ingredient; to methods for the production of said compounds and the associated pharmaceutical compositions. 

Azole derivative useful as antifungal agents with reduced interaction with metabolic cytochromes

A compound having formula (I) and a process for the preparation thereof are described.

Monohydrate hydrochloride of the 4-hydroxycarbamoyl-phenyl)-carbamic acid (6-diethylaminomethyl-naphtalen-2-yl) ester

Compounds of formula (I), inhibit TNF&#x3b1; production and may therefore be useful in the treatment of inflammation, of auto-immune diseases, and of pathological conditions which involve excessive production of that cytokine. The compounds of formula (I) are also inhibitors of the histone deacetylase enzyme and may therefore be useful in tumorous diseases, alone or in association with other anti-tumor active ingredients 

Hydroxamic acid derivatives having anti-inflammatory action

Oligopeptides derived from C-reactive protein fragments

A method for treating septic shock by administering a retroinverted tetrapeptides of formula I ##STR1## wherein R is a hydrogen atom or the side-chain of threonine; R.sub.1 is the side-chain of arginine, leucine or glutamine; and R.sub.2 is a hydrogen atom or a metabolically perishable acyl group; with the proviso that when R.sub.1 is the side-chain of arginine, R cannot be the side-chain of threonine; diastereo-isomeric forms and pharmacologically acceptable salts, esters and amides thereof.

Partially modified and retro-inverted tetrapeptides analogues of

This invention relates to new gem-diamino derivatives of general formula (I) ##STR1## where R is the side chain of an amino acid, of which any functional groups are suitably protected, and

Gem-diamino derivatives and their use in the synthesis of retro-inverso

A method of synthesis of a partially retro-inverso peptide incorporating at least one malonyl residue of formula (III) ##STR1## wherein R represents the side chain of an .alpha.-amino acid, is described which is characterized in that said malonyl residue is incorporated by condensing a 5-substituted-2,2-dimethyl-1,3-dioxane-4,6-dione of formula (IV) ##STR2## wherein R' is the side-chain R wherein the functional groups, if any, are suitably protected, with an amino acid, amino acid amide, peptide fragment, or pseudo-peptide fragment wherein the terminal carboxyl group, if present, and the possible side-chain functionalities are suitably protected and the reactive amino group is tri-alkyl-silylated. The new compounds of formula (VI) and a process for the preparation of a partially retro-inverso tuftsin analog which involves use of said method and said intermediate are also described and claimed.

Process for the preparation of retro-inverso peptides and new

A method of synthesis of a partially retro-inverso peptide incorporating at least one malonyl residue of formula (III) ##STR1## wherein R represents the side chain of an .alpha.-amino acid, is described which is characterized in that said malonyl residue is incorporated by condensing a 5-substituted-2,2-dimethyl-1,3-dioxane-4,6-dione of formula (VI) ##STR2## wherein R' is the side-chain R wherein the functional groups, if any, are suitably protected, with an amino acid, amino acid amide, peptide fragment, or pseudo-peptide fagment wherein the terminal carboxyl group, if present, and the possible side-chain functionalities are suitably protected and the reactive amino group is tri-alkyl-silylated. The new compounds of formula (VI) and a process for the preparation of a partially retro-inverso tuftsin analog which involves use of said method and said intermediate are also described and claimed.

Process for the preparation of retro-inverso peptides and

Synthesis of an analogue of the (5-14) decapeptide of equine angiotensinogen partially retro-inverted at the Phe-Phe bond, of formula: ##STR1## The retro-inverso analogue inhibits renin with high resistance to enzymatic degradation, and can be used in the treatment of renin-dependent hypertension.

Partially retro-inverted decapeptide as a specific renin inhibitor with

There is provided an analog of the (5-14) decapeptide of equine angiotensinogen which is partially inverted at the Phe-Val bond, and which has the formula ##STR1## This retro-inverso analog inhibits renin with high resistance to enzymatic degradation and it can be used in the treatment of renin-dependent hypertension.

Growing community of inventors

Paderno D'Adda, Italy

Massimo Pinori