Sanofi

Continental Pharma Incorporated

Romeo Roncucci

Henri Demarne

Joseph Diaz

Paul-Henry Schmelck

Paolo Carminati

Dino Nisato

Sergio Boveri

Alberto Bianchetti

Claude L Gillet

Georges E Lambelin

Joseph L Roba

Paul J Niebes

William R Van Dorsser

Jacqueline Lansen

Alexis H Cordi

Mark A Martens

A process for the synthesis, in liquid phase and by fragments, of hGRF 1-44 and hGRF 1-40. This process consists in coupling, one after the other and in the order of the sequence of the GRF,

Synthesis of hGRF (Somatocrinin) in liquid phase and intermediate

Synthesis of hGRF (somatocrinin) in liquid phase and intermediate

The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising: coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group; selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.

Synthesis of hpGRF(Somatocrinin) in liquid phase and intermediate

A glycinamide derivative of the general formula I: ##STR1## wherein: R is a linear or ramified alkyl group C.sub.5 -C.sub.18, a linear or ramified alkenyl group C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9, C.sub.10, C.sub.11, C.sub.12, C.sub.13, C.sub.14, C.sub.15, C.sub.16, C.sub.17 or C.sub.18, a linear or ramified alkynyl group C.sub.4 -C.sub.10, a linear or ramified acyl group C.sub.4 -C.sub.18, a linear or ramified alkyl group C.sub.1 -C.sub.10, substituted by a phenoxy group, by a hydroxy radical, by an acetoxy radical, by a carboxy radical, by a linear or ramified alkoxycarbonyl group C.sub.1 -C.sub.4, by a carbonyl radical, by a carboxaldehyde group, by an acetal or cetal group, by one or more phenyl groups, by one or more phenyl groups substituted by a halogen atom such as fluorine, chlorine or bromine,

Derivatives of glycinamide, their preparation and their use

The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising:--coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group;--selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and--eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.

Synthesis of hpGRF (Somatocrinin) in liquid phase and intermediate

Amides acting as histamine H.sub.2 receptors antagonists, of formula ##STR1## wherein X represents a N.fwdarw.O or C-NH-A-B group in which A is CO or SO.sub.2 and B is alkyl, phenyl, pyridyl, pyridyl 1-oxide, pyrazinyl or thienyl; their salts; process for their preparation by reacting 2-(2-guanidinothiazol-4-ylmethylthio)ethylamine with a derivative of formula ##STR2## and optional salification; and pharmaceutical compositions containing same.

Certain amide derivatives of 2-guanidino-thiazoles and compositions

Amidobenzamides acting as histamine H.sub.2 receptors blocking agents, of formula ##STR1## wherein A is CO or SO.sub.2 and B is alkyl, phenyl, pyridyl, pyridyl-1-oxyde, pyrazinyl or thienyl; their salts; process for their preparation by reaching 2-(5-dimethyl-aminomethylfuran-2-ylmethylthio)ethylamine with a derivative of formula ##STR2## and optional salification and pharmaceutical compositions containing same.

Amidobenzamides, their salts and pharmaceutical compositions containing

A process and an apparatus for determining malondialdehyde content of blood platelets. A platelet-enriched plasma is prepared from a determined amount of blood, the counting of the platelets is carried out, the platelets are sedimented, an aggregation agent is added, segmented samples are prepared, said samples are submitted to a dialysis in order to eliminate the proteins and the malondialdehyde content is determined by colorimetry. The samples are segmented with a gas. The process is particularly suitable for evaluating the platelet regeneration.

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Paris, France

Romeo Roncucci