Abstract: The present invention concerns a new process for the synthesis of aminaphtone, which makes use of non-toxic solvents and reagents, under mild reaction and temperature conditions. The aminaphtone obtained with the method of the present invention also has a purity of at least 98% in weight. The method comprises the following steps: a) epoxidating menadione 1 to provide epoxide 2, b) acidifying epoxide 2 to provide hydroxynaphthoquinone 3, c) esterifying between hydroxynaphthoquinone 3 and 4-aminobenzoyl chloride to obtain compound 4, and d) reducing compound 4 in the presence of a reducing agent in water to obtain aminaphtone.

Abstract: The present invention concerns a new process for the synthesis of aminaphtone, which makes use of non-toxic solvents and reagents, under mild reaction and temperature conditions. The aminaphtone obtained with the method of the present invention also has a purity of at least 98% in weight. The method comprises the following steps: a) epoxidating menadione 1 to provide epoxide 2, b) acidifying epoxide 2 to provide hydroxynaphthoquinone 3, c) esterifying between hydroxynaphthoquinone 3 and 4-aminobenzoyl chloride to obtain compound 4, and d) reducing compound 4 in the presence of a reducing agent in water to obtain aminaphtone.

Abstract: The use of metadoxine in the treatment of hepatic fibrosis is described. Metadoxine can be orally and/or parenterally administered at a dosage comprised between 50 and 1000 mg per dose, preferably between 300 and 600 mg per dose. In the in vitro study, metadoxine results effective at lower concentrations with respect to those that are obtained in the plasma after oral administration at the doses recommended for conventional pathology.

Abstract: The present invention relates to novel geranylgeranyl derivatives and the pharmaceutically acceptable salts thereof having antiproliferative activity in eukaryotic cells with respect to the inhibition of protein geranygeranylation. The invention also relates to the pharmaceutical compositions containing the novel derivatives and to the process of preparation thereof.

Abstract: A conjugate of an antiviral nucleoside with a lactosaminated human albumin (L-HSA) and its method of preparation is described. The method of preparation involves the reaction of an antiviral phosphorylated nucleoside in the form of an imidizolide with L-HSA at a pH above 7.5 and running the reaction until the desired molar ratio of drug to L-HSA is obtained.

Abstract: Complexable heterogeneous oligosaccharides and pure alpha-hydosanes, namely not contaminated from other macromolecules (mucopolysaccharides, proteins, nucleic acids, etc.) of a defined molecular weight are produced starting from a mixture of mucopolysaccharides obtained starting from bovine or swine mucosa through a process comprising a precipitation with organic solvents, a further purification by means of specific enzymes and chromatographic separation by gel filtration. Heterogeneous oligosaccharides are obtained which can be complexed with metals, being thus able to promote the pharmacological effect of the metal thanks to the geater permeability towards the complexes of the membrane of the cells of the absorbing mucosa and of the cells of the target tissue.

Abstract: The xanthosulfonamido and benzensulfonamido derivatives corresponding to the formula: ##STR1## wherein X represents hydrogen, alkyl, alkoxy or halogen, Y represents an alkyl, alkoxy or halogen and Z represents the group ##STR2## or Y and Z taken together form the group: ##STR3## wherein R.sub.1 in turn is a group selected among electron attracting groups, halogens and the group: ##STR4## itself, possess activity in inhibiting the aldose-reductase enzyme system and are thus useful in the treatment of the complications, at the eye and peripheral neuropathy levels, as induced by diabetes.

Abstract: The xanthosulfonamido and benzensulfonamido derivatives corresponding to the formula: ##STR1## wherein x represents hydrogen, alkyl, alkoxy or halogen, Y represents an alkyl, alkoxy or halogen and Z represents the group ##STR2## or Y and Z taken together form the group: ##STR3## wherein R.sub.1 in turn is a group selected among electron attracting groups, halogens and the group: ##STR4## itself, possess activity in inhibiting the aldose-reductase enzyme system and are thus useful in the treatment of the complications, at the eye and peripheral neuropathy levels, as induced by diabetes.

Abstract: For the preparation of conjugates of adenine-9-beta-D-arabinofuranoside 5'monophosphate (ara-AMP) with lactosaminated human albumin (L-HSA) aqueous solutions of the two components to be conjugated are brought into contact in the presence of 1-ethyl-3-(dimethylaminopropyl)-carbodiimide, by adjusting the pH in the range from slightly acidic to alkaline and by carrying out the conjugate separation. The resulting conjugate, wherein the molar ratio, as determined through spectrophotometric route, between ara-AMP and L-HSA does vary between 5 and 20, remains soluble after lyophilization even at room temperature and shows biological activity at least equivalent to that of the conjugate as prepared according to the known art.

Abstract: The 2-(.omega.-alkylaminoalkyl)- and 2-(.omega.-dialkylaminoalkyl)-3-(4-X-benzylidene)phthalimidines are useful as local anesthetics. For the preparation, the adduct is formed between the suitable 3-(4-X-benzylidene)phthalide and a substituted amino-alkylamine, the adduct being then reacted with acetic anhydride; the X substituent at the position 4 of the benzylidene group then can be suitably converted according to the requirements.