Mediolanum Farmaceutici, S.r.l.

Rinaldo Del Bono

Luigi De Ambrosi

Gianni Ferrari

Pier G Pagella

Pier L Rugarli

Piergiuseppe Pagella

A process for preparing dermatan sulphate (DS) of pharmaceutical purity from animal organs rich in micropolysaccharides (MPS), by: a) stabilizing the fresh organs by freezing them either as such or in the form of powder, b) micronizing the material containing the MPS with an aqueous CaCl.sub.2 solution, c) digesting the homogenate comprising the raw material and the CaCl.sub.2 with proteolytic enzyme at alkaline pH and at low temperature, d) acidifying, heating and filtering the lysate, e) treating the filtrate with quaternary ammonium salts able to undergo complexing with and thus precipitate either the DS alone or all the MPS selectively, f) recovering and purifying the DS either directly from the ammonium salt complex containing it or from the complex obtained from the mixture of ammonium salt complexes of all the MPS by fractional solubilization with acetone.

High-purity dermatan sulphate

A process for preparing dermatan sulphate (DS) of pharmaceutical purity from animal organs rich in mucopolysaccharides (MPS), by: (a) stabilizing the fresh organs by freezing them either as such or in the form of powder, (b) micronizing the material containing the MPS with an aqueous CaCl.sub.2 solution, (c) digesting the homogenate comprising the raw material and the CaCl.sub.2 with proteolytic enzymes at alkaline pH and at low temperature, (d) acidifying, heating and filtering the lysate, (e) treating the filtrate with quaternary ammonium salts able to undergo complexing with and thus precipitate either the DS along or all the MPS selectively, (f) recovering and purifying the DA either directly from the ammonium salt complex containing it or from the complex obtained from the mixture of ammonium salt complexes of all the MPS by fractional solubilization with acetone.

Process for preparing high-purity dematan sulphate, and pharmaceutical

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

1,2 Benzothiazino[3,4-d]pyrazoles of the following general formula ##STR1## wherein R stands for a linear or branched (C.sub.2-4) alkyl chain bearing a substituent of formula ##STR2## in which the R' radicals may be the same or different and represent hydrogen, (C.sub.2-4)alkyl, (C.sub.4-7) cycloalkyl or, taken together with the adjacent nitrogen atom, may also represent a saturated, 5 to 7 membered heterocyclic ring containing from one to three heteroatoms independently selected from O,N and S, or R may represent the 1-ethyl-pyrrolidine-2-yl-methyl radical, and R' is hydrogen, a halogen atom or a (C.sub.1-4) alkyl radical; methods for their preparation; pharmaceutical compositions containing them. The compounds possess antiinflammatory, antipyretic and analgesic activity.

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Milan, Italy

Rinaldo Del Bono