Zambon S.p.a.

Zambon Group

Davide Della Bella

Dario Chiarino

Angelo Carenzi

Franco Pellacini

Mario Fantucci

Vittorio Ferrari

Giancarlo Grancini

Viviana Frigeni

Carlo Veneziani

Uberto Teotino

Mauro Napoletano

Alberto Sala

Giancarlo Jommi

Gian Carlo Grancini

Mario Portelli

Vittorio Ferrrari

Alberto Pilotto

Compounds of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and n have the meanings reported in the specification, processes for their preparation and pharmaceutical compositions containing them as active ingredient are described. The compounds of formula I are inhibitor of enzymatic systems and they are useful in pharmaceutical field.

Peptides with pharmaceutical activity

Compounds of formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and n have the meanings reported in the specification, processes for their preparation and pharmaceutical compositions containing them as active ingredient are described. The compounds of formula I are inhibitors of enzymatic systems and they are useful in pharmaceutical field.

Isoxazoles with nootropic activity

Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2, R.sub.3 and n have the meanings reported in the specification), their salts with pharmaceutically acceptable acids, process for their preparation and pharmaceutical compositions containing them are described. The compounds of formula I have a remarkable analgesic activity.

Pyrrolidone-2 compounds and their use for central analgesic activity

Compounds of the formula ##STR1## wherien R, R.sub.1, R.sub.2 and Y have the meanings mentioned in the description, processes for their preparation and their use in the pharmaceutical field are described. The compounds of formula I are endowed with antipyretic, anti-inflammatory, mucolitic and analgesic activity together with good gastric tolerability. In addition, the compounds of formula I are active in the treatment of ischemic or reperfusion syndromes.

Derivatives of thiazolidine-4-carboxylic acid having pharmacological

The compound N-[(1S,2R)-fluoromethyl-2-hydroxy-2-(4-methylsulphonyl-phenyl)-ethyl]-2-pr openamide and the derivatives thereof in which the hydroxy in 2 position is esterified by a mono or dicarboxylic acid or by an aminoacid are described. Such compounds have antibiotic activity and are useful in human and veterinary therapy.

Compositions with antibiotic activity and their use

Mono(2-ammonium-2-hydroxymethyl-1,3-propanediol)(2R-cis)-(3-methyloxiranyl) phosphonate endowed with therapeutic activity as broad-spectrum antibiotic, as well as a method for preparing same from bis(2-ammonium-2-hydroxymethyl-1,3-propanediol)(2R-cis)-(3-methyloxiranyl) phosphonate and a sulphonic acid. Pharmaceutical compositions containing the novel mono(2-ammonium-2-hydroxymethyl-1,3-propanediol)(2R-cis)-(3-methyloxiranyl ) phosphonate are disclosed.

Mono(2-ammonium-2-hydroxymethyl-1,3

Compounds of formula ##STR1## in which R, R.sub.1 and Y have the meanings shown in the description, their preparation by condensing an aldehyde or a ketone with cysteine or a derivative thereof and their use in the pharmaceutical field. The compounds of formula I possess antipyretic, anti-inflammatory, mucolytic and analgesic activity together with a low capacity to cause gastric injuries. The compounds of formula I, furthermore, are particularly useful in the treatment of ischemia and reperfusion syndromes.

Pharmaceutically useful derivatives of thiazolidine-4-carboxylic acid

A method for the treatment of ischemia and reperfusion syndromes, which consists in administering to a patient in need thereof a therapeutically effective amount of a compound of the formula: ##STR1## in which R is hydrogen or a C.sub.1 -C.sub.6 alkyl group, or of a salt thereof, when R=H, with a pharmaceutically acceptable base. New compounds and pharmaceutical compositions useful in the method of this invention.

Thioesters for the treatment of ischemia and reperfusion syndromes

A method for the treatment of ischemia and reperfusion syndromes, which consists in administering to a patient in need thereof a therapeutically effective amount of a compound of the formula: ##STR1## in which R is hydrogen or a C.sub.1 -C.sub.6 alkyl group, or of a salt thereof, when R.dbd.H, with a pharmaeutically acceptable base. New compounds and pharmaceutical compositions useful in the method of this invention.

Method for the treatment of ischemia and reperfusion syndromes

4-(isoxazolyl)-thiazole-2-oxamic acids and derivatives thereof

Use of 4-(isoxazolyl)-thiazole-2-oxamic acid derivatives

Dipeptide compounds having pharmaceutical activity and compositions

Bis-(2-ammonium-2-hydroxymethyl-1,3-propanediol)(2R-cis)-(3-methyloxiranyl) -phosphonate showing high bioavailability and tolerability is disclosed, as well as a method for preparing same from (2R-cis)-(3-methyloxiranyl)-phosphoric acid, or a salt thereof, and 2-amino-2-hydroxymethyl-1,3-propanediol, or a salt thereof. Pharmaceutical compositions containing the novel bis-phosphonate; useful for clinical forms of urinary and respiratory infections, are also disclosed.

Bis-(2-ammonium-2-hydroxymethyl-1,3-propaned

N-substituted derivatives of 1-(4'-alkylthiophenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof. The novel derivatives according to this invention are endowed with calcium antagonist activity and are useful as antiarrhythmic and vasodilating agents.

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Milan, Italy

Davide Della Bella