Sigma-Tau Industrie Farmaceutiche Riunite S.p.a.

Other

Sigma-Tau Healthscience S.p.a.

Nazareno Scafetta

Maria Ornella Tinti

Claudio Cavazza

Domenico Misiti

Piero Foresta

Francesco De Angelis

Mose Santaniello

Vito Ulderico Ruggiero

Mos&egrave; Santaniello

Claudio Pisano

Fabio Giannessi

Mos&eacute; Santaniello

Andrea Pucci

Gian Carlo Gramiccioli

Maria Grazia Cima

Lucia Critelli

Ida Bernabei

Perfluorinated esters of alkanoyl L-carnitine for the preparation of cationic lipids for the intracellular delivery of pharmacologically active compounds

Non-hygrocopic salts of L-carnitine and of the lower alkanoyl L-carnitines with pamoic acid are described, which are used to prepare solid compositions suitable for oral administration. Solid compositions containing such salts are also described.

Solid compositions suitable for oral administration containing non-hydroscopic salts of L-carnitine and alkanoyl L-carnitines

Solid and non hygroscopic salts consisting of lower alkanoyl L-carnitine magnesium citrates are disclosed which are suitable for preparing solid composition useful as dietary/nutritional supplements for human use and as fodder supplement for veterinary purposes.

Solid compositions suitable for oral administration comprising an alkanoyl-l-carnitine magnesium citrate

Water-soluble dodecandioates wherein the cationic moiety is selected from the group comprising the cations of basic aminoacids (e.g. lysine) and choline and orally or parenterally administrable compositions containing same, are disclosed.

Water-soluble salts of dodecandioic acid and pharmaceutical and nutritional compositions containing same

Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, staight or branched alkanoyl having 2-26 carbon atoms, optionally &ohgr;-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.

Esters of acyl L-carnitines and pharmaceutical compositions containing same for treating endotoxic shock

Solid compositions suitable for oral administration comprising

Solid compositions suitable for oral administration comprising non

DL-, D- or L-carnitine esters of formula ##STR1## wherein R, Y and X.sup.- have the meaning shown in the specification which possess potent bactericidal, fungicidal and antiprozoal activity, processes for their preparation and compositions topically applicable for treating infections of the skin, outer ear and mucosa, are disclosed.

Bis alkanoyl esters of carnitine having bactericidal, fungicidal and

Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, straight or branched alkanoyl having 2-26 carbon atoms, optionally .omega.-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.

Esters of acyl L-carnitines and pharmaceutical compositons containing

The esters of acyl L-carnitines with gamma-hydroxybutyric acid in the form of pharmacologically acceptable salts of formula (I) ##STR1## wherein X.sup.- is the anion of a pharmacologically acceptable salt, e.g. chloride, bromide, orotate, acid aspartate, acid citrate, acid phosphate, acid fumarate, lactate, acid maleate, acid oxalate, acid sulfate and glucosephosphate or in the form of inner salts of formula (I') ##STR2## wherein R is a straight or branched acyl group having from 2 to 5 carbon atoms, such as e.g. acetyl, propionyl, n-butyryl, isobutyryl and isovaleryl, are active in inhibiting neuronal degeneration (as it occurs in Alzheimer's senile dementia and Parkinson's disease) and in the treatment of coma.

Esters of acyl l-carnitines with gamma-hydroxybutyric acid and

The esters of acyl L-carnitines with gamma-hydroxybutyric acid in the form of pharmacologically acceptable salts of formula (I) ##STR1## wherein X.sup.- is the anion of a pharmacologically acceptable salt, e.g. chloride, bromide, orotate, acid aspartate, acid citrate, acid phosphate, acid fumarate, lactate, acid maleate, acid oxalate, acid sulfate and glucosephosphate or in the form of inner salts of formula (I') ##STR2## wherein R is a straight or branched acyl group having from 2 to 5 carbon atoms, such as e.g. acetyl, propionyl, n,butyryl, isobutyryl and isovaleryl, are active in inhibiting neuronal degeneration (as it occurs in Alzheimer's senile dementia and Parkinson's disease) and in the treatment of coma.

Easters of acyl L-carnitines with gamma-hydroxybutyric acid and

L-(-)-carnitine is prepared from D-(+)-carnitinamide by (a) reacting D-(+)-carnitinamide in an acid medium with a straight or branched chain aliphatic alcohol thereby forming D-(+)-carnitine ester, (b) acylating the D-(+)-carnitine ester with an anhydride R.sub.2 O, thereby forming an acylated ester intermediate, (c) acid hydrolyzing the ester group of the acyl carnitine ester thereby obtaining acyl D-(+)-carnitine, (d) lactonizing the acyl D-(+)-carnitine to a lactone of L-(-)-carnitine, and (e) reacting the lactone with base thereby forming L-(-)-carnitine.

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Pavona di Albano, Italy

Nazareno Scafetta