Laboratori Baldacci S.p.a.

Laboratori Balducci S.p.a.

Other

Baldacci, Massimo

Massimo Baldacci

Luigi Fiume

Corrado Busi

Alessandro Mattioli

Giulio Caccia

Romano Danesi

Bruno Macchia

Aldo Balsamo

Mario Del Tacca

Marco Macchia

Marinella Roberti

Giuseppina Di Stefano

Guiseppina Di Stefano

Ugo Baldacci

Maria Beatrice Rondinelli

The object of the present invention is a product obtainable by spray-drying an aqueous solution comprising iron bis-glycinate chelate and alginic acid and/or water-soluble salts thereof, preferably sodium alginate, potassium alginate and/or magnesium alginate, the use of said product for the prevention and/or treatment of anaemia, preferably sideropenic anaemia, in humans, the pharmaceutical formulations containing it, and the use of said formulations for the prevention and/or treatment of anaemia, preferably sideropenic anaemia, in humans.

Product based on iron bis-glycinate chelate and alginic acid and/or water-soluble salts thereof, formulations thereof, and pharmaceutical uses thereof

The present invention relates to pyrrolidone carboxylic acid (PCA) and/or pharmaceutically acceptable salts or derivatives thereof for use in the treatment of ocular diseases and/or disorders. A further object of the present invention are compositions comprising pyrrolidone carboxylic acid (PCA) and/or pharmaceutically acceptable salts or derivatives thereof, at least one physiologically acceptable excipient, and optionally at least one additional active ingredient for use in the treatment of ocular diseases and/or disorders.

Pyrrolidone carboxylic acid (PCA) for ophthalmic use

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.

Process for the synthesis of aminaphtone

The present invention refers to conjugated compounds of antiviral drugs having hepatotropic activity, methods of making these compounds, and compositions thereof.

Hepatotropic conjugates of antiviral drugs carriers thereof and pharmaceutical compositions containing them

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.

Geranylgeranyl-derivatives, process for the preparation thereof and related pharmaceutical compositions

Hepatotropic conjugates of antiviral drugs carriers thereof and

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. There are also obtained pure alpha-hydosanes having a well defined molecular weight range capable of providing several pharmacological activities more particularly an activating effect of he anti-thrombine III, a potentiating effect of the tissutal activator and a fibrine depolymerizing effect have been found for some of them whereas for some others an effect on the factor Xa/PTT ratio has been revealed and lastly for still others a lipasemic and anti-coagulating activity has been found.

Complexable heterogenous oligosaccharides and alpha-hydosanes having

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.

Sulfonamido derivative inhibiting the aldose reductase enzyme system and

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.

Sulfonamido derivatives inhibiting the aldose reductase enzyme system

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.

Method for the preparation of conjugates of

A conjugate of 9-(2-hydroxyethoxymethyl)-guanine with lactosaminated human albumin is therapeutically more efficacious than the free drug in the treatment of chronical hepatitis induced from Virus B. For the preparation of the conjugate an aqueous solution of 9-(2-hydroxyethoxymethyl)-guanine in form of a derivative, particularly monophosphate, and an aqueous solution of lactosaminated human albumin are reacted in the presence of 1-ethyl-3-(dimethylaminopropyl)-carbodiimide, by adjusting the pH to the value of 7.5 and by maintaining the reaction mixture for 24 hours under stirring and in the dark.

Conjugate of 9-(2-hydroxyethoxymethyl)-guanine with lactosaminated human

The administration by oral route of a composition comprising arginine pyrrolidone carboxylate and lysine pyrrolidone carboxylate at a dose of 150 to 200 mg/kg of body weight has immunomodulating activity capable of restoring depressed immunodefenses.

Pharmaceutical composition having immunomodulating activity

The treatment of patients suffering from acute alcoholic intoxication with pyridoxine 5-oxo-2-pyrrolidon-carboxylate permits the symptomatology of the psychomotor excitation and aggression to be readily and essentially completely solved.

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Pisa, Italy

Massimo Baldacci