Eniricerche S.p.a.

Sclavo Spa

Enichem S.p.a

Eni-ente Nazionale Idrocarburi

Polifarma S.p.a.

Italfarmaco Spa

Anic S.p.a.

Enichem Elastomeri S.p.a.

Scalvo Spa

Sclano S.p.a.

Ente Nazionale Idrocarburi

Antonio S Verdini

Antonello Pessi

Alessandro Sisto

Fabio Bonelli

Massimo Pinori

Adriano Bernardi

Antonino Virdia

Vincenzo Politi

Giovanna De Luca

Giovanni Di Stazio

Valerio Caciagli

Carlo A Nuzzolo

Romano Di Trapani

Laura Gazerro

Flavio Leoni

Felice Centini

Luciano Nencioni

Silvana Cappelletti

Luigi Villa

Sabina Mariotti

Giuseppe C Viscomi

Franco Cardinali

Diana Boraschi

Antonio Virdia

Stefano Censini

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

An ELISA method with competitive inhibition is described for determining antisporozoite antibodies of P. Falciparum in human blood samples and in mosquito extract, which uses a single plate pretreated with only the synthetic antigen (NANP).sub.20 using, as total competitive inhibitor for the formation of the complex between the synthetic antigen adsorbed on the plate and the antibody contained in the sample, the (NANP).sub.20 synthetic peptide in a weight ratio of at least 20:1 with respect to the adsorbed antigen. Because of its high specificity, sensitivity and speed, the method is particularly suitable for epidemiological studies on malaria.

Immunoenzymatic single-plate ELISA method with competitive inhibition

Polypeptide useful for the preparation of antimalarial vaccines and of diagnostic kits for the detection of antisporozoite antibodies in clinical samples of malariated persons, constituted by: a synthetic peptide, which repeates the region I of P. falciparum and by a variable number of repetitive tetrapeptide units of CS protein of P. falciparum linked to each other by an amidic bond between the tail proline of I region and the head asparagine of the first tetrapeptide.

Polypeptide useful for the preparation of antimalarial vaccines and 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

Synthetic polypeptides constituted by at least two consecutive repeating units of (Asn-Asn-Pro) sequence are powerful immunogens in test animals. The formed antibodies recognize both the synthetic polypeptides and the immuno-dominant epitope of the circumsporozoitic protein of Plasmodium falciparum. Said polypeptides, which can be obtained in pure form, are particularly useful for the preparation of antimalarial vaccines and of diagnostic kits for the determination of malarial affections.

Sequential polypeptides endowed with immunological activity

New analogues of thymopentin (TP5) and of its tetrapeptide fragment (TP5.sup.1-4) containing two non-contiguous retro-inverted bonds in the peptide chain are described which are of the general formula (I) ##STR1## where R is hydrogen or an acyl radical, and R.sup.1 is an --OR.sup.2 group or an ##STR2## group where R.sup.2 is a hydrogen atom or a hydrocarbon radical, and R.sup.3 is a hydrogen atom or a hydroxyl group, and the corresponding pharmaceutically acceptable salts of acid or basic addition, possess immunomodulating activity.

Retro-inverso analogues of thymopentin and the method for their synthesis

An immunoenzymatic method for the detection of anti-Plasmodium falciparum-sporozoite antibodies in a sample of human blood, which operates, in homogeneous phase, and under suitable conditions, with a synthetic polypeptidic antigen (P), a synthetic antigen-enzyme (P-E) conjugate, wherein said antigen is capable of specifically reacting with the anti-Plasmodium falciparum-sporozoite antibodies (Ab) possibly present in the sample, and an inert substance capable of quantitatively precipitating the antibody-synthetic antigen-enzyme complex (Ab-P-E). The method, due to its specificity, sensitivity, reproducibility and rapidity, is particularly useful in the epidemiological investigations into malaria and in the evaluation of the efficacy of an antimalarial vaccine.

Immunoenzymatic method in homogeneous phase for the determination of

New retro-inverso analogs of thymopentin (TP5) and of its tripeptide fragment (TP5.sup.1-3) of general formula (I) ##STR1## are described wherein R is hydrogen or an acyl radical, and R.sup.1 is --OR.sup.2 or ##STR2## wherein R.sup.2 is hydrogen or a hydrocarbyl radical, and the corresponding pharmaceutically acceptable acid- or base-addition salts. A process of preparing the tripeptide fragment of formula I is also described. The new compounds are enzyme-resistant immunomodulatory peptides.

Process for preparing new thymopentin retro-inverso analogs and

An improvement is described in the synthesis method for N.sup..alpha. -trityl-N.sup.G -trityl arginine within a process for preparing N.sup..alpha. -fluorenylmethoxycarbonyl-N.sup.G -trityl-arginine from arginine, comprising:

Process for the synthesis of N.sup..alpha.

Immunologically active polypeptide composition constituted by polypeptides having the formula:

Polypeptidic composition useful for the preparation of antimalarial

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

Synthetic peptides constituted by at least two repeating, consecutive units of asparaginyl-proline (Asn-Pro).sub.n sequence, are described. The peptides are powerful immunogens, capable of inducing in laboratory animals the formation of a high concentration of antibodies capable of reacting both with the (Asn-Pro).sub.n peptides, and with the immunodominant epitope of the circumsporozoite protein of Plasmodium falciparum. The peptides, which can be obtained in a pure form by chemical synthesis, are particularly useful for preparing antimalarial vaccines and diagnostic kits for the determination of malaria in man.

Synthetic, immunologically active peptides useful for the preparation of

New analogues of thymopentin (TP5) and of its tetrapeptide fragment (TP5.sup.1-4) containing two non-contiguous retro-inverted bonds in the peptide chain are described. The new compounds, of general formula (I) ##STR1## where R is hydrogen or an acyl radical, and

Retro-inverso analogues of thymopentin, and their use in the preparation

An improvement is described in the synthesis method for N.sup..alpha. -trityl-N.sup.G -trityl arginine within a process for preparing N.sup..alpha. -fluorenyl-methoxycarbonyl-N.sup.G -trityl-arginine from arginine, comprising:

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Monterotondo, Italy

Antonio S Verdini