Mediolanum Farmaceutici, S.r.l.

Italfarmaco Spa

Mediolanum Farmaceutici

Piergiuseppe Pagella

Patrizia Terni

Stefano Maiorana

Giancarlo Sportoletti

Luigi De Ambrosi

Pietro Cremonesi

Antonio Papagni

Gianni Ferrari

Arnaldo Fravolini

Rinaldo Del Bono

A process for preparing pyrido-benzothiazine derivatives having the following general formula: ##STR1## in which R is H or a C.sub.1 -C.sub.6 alkyl or a C.sub.1 -C.sub.6 fluoroalkyl, and R.sub.1 is N-alkyl-3-pyrrolidinalkylamine with C.sub.1 to C.sub.6 alkyls or ##STR2## where R.sub.2 is a C.sub.1 -C.sub.6 alkyl or a C.sub.2 -C.sub.6 alkenyl or an arylalkyl group, possibly substituted by halogen, hydroxy or keto-groups, both in the racemic form and in the optically active form. The process for the preparation of derivatives of formula (I) starts with a first reaction cycle starting from 2,4-difluoro-3-chloronitrobenzene. Said derivatives possess a high antibacterial activity as well as a high bioavailability to tissues. The invention also refers to pharmaceutical compositions containing them as active components.

Process for preparing pyrido-benzothiazine derivatives having high

Pyrido-benzothiazine derivatives having the following general formula: ##STR1## in which R is H or a C.sub.1 -C.sub.6 alkyl or a C.sub.1 -C.sub.6 fluoroalkyl, and R.sub.1 is N-alkyl-3-pyrrolidinalkylamine with C.sub.1 to C.sub.6 alkyls or ##STR2## where R.sub.2 is a S.sub.1 -C.sub.6 alkyl or a C.sub.2 -C.sub.6 alkenyl or an arylalkyl group, possibly substituted by halogen, hydroxy or keto-groups, both in the racemic form and in the optically active form. The invention also comprises the process for the preparation of derivatives of formula (I) starting from 2.4-difluoro-3-chloronitrobenzene. Said derivatives possess a high antibacterial acitvity as well as a high bioavailability to tissues; the invention also refers to pharmaceutical compositions containing them as active components.

Pyrido-benzothiazine derivatives having high antibacterial activity and

The invention relates to antibacterially active pyrido-benzothiazine derivatives with long-term action, having the following general formula: ##STR1## in which R is ##STR2## Where R.sup.1 is H, C.sub.1 -C.sub.6 alkyl, p-fluorophenyl, m-fluorophenyl, o-fluorophenyl or 2-pyridyl; or ##STR3## where R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 are lower alkyls. The invention also comprises the process for preparing compounds of general formula (I). Said process consists of a synthesis cycle using 2,4-difluoro-3-chloronitrobenzene and thiolactic acid as starting substances. The inventiona also comprises pharmaceutical compositions containing at least one of the compounds of general formula (I) as active principle.

Antibacterially active pyrido-benzothiazine derivatives with long-term

A process for producing natural heparan sulphate and dermatan sulphate for mixtures of proteoglycans from the aorta, myocardium and particularly vascularized organs, based on a series of precipitation and purification steps which enable the protein part of the proteoglycan to be eliminated and the two products to be obtained in substantially pure form, without any chemical or enzymatic degradation. When administered orally or parenterally, the heparan sulphate obtained exerts activation effects on antithrombin III and on the fibrinolytic process. The dermatan sulphate obtained exerts an inhibiting effect on Factor Xa and also possesses the property of activating the fibrinolytic effect of heparan sulphate.

Process for producing natural heparan sulphate and dermatan sulphate in

Bio-available iron-protein derivatives having an iron content of from 2% to 20% by weight and a nitrogen content of from 12% to 16% by weight obtained by reacting acetylated globin with an iron compound selected from the group consisting of ferric chloride, iron fructate and iron saccharate, and pharmaceutical compositions for treating and preventing iron deficiency in animals and humans.

Bio-available iron-protein derivatives and process for their preparation

Pharmaceutical compositions are described which have antithrombotic activity suitable for the prevention and for the therapy of cardiac infarcts, cerebral infarcts and venous thrombosis. They contain as the active component a fraction of heparin which has been modified by nitrogen desulfatation and succinylation, which fraction contains less than 10% of the N-sulfate groups of the heparin starting material and more than 0.6 succinyl radicals per disaccharide unit. The method of treatment is described.

Modified glucosaminoglucans having antithrombotic activity

The invention relates to succinylated proteins, with a degree of succinylation of between 20 to 100%, containing from 0.1 to 20% by weight of iron, obtained by treating succinylated proteins with iron salts in suitable pH ranges. The compounds in question, which are completely tolerated, are characterized by an optimum bioavailability of iron.

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Milan, Italy

Piergiuseppe Pagella