Contipro A.s.

Contipro Biotech S.r.o.

Petra Sedova

Vladimir Velebny

Radovan Buffa

Ivana Basarabova

Kristina Nesporova

Tomas Bobula

Lucie Wolfova

Pavlina Prochazkova

Hana Vagnerova

Iva Doleckova

Sona Moravcikova

Tereza Ehlova

Ondrej Kotland

Leos Hromek

Robert Pospisil

Martina Hasova

Martina Moravcova

Tereza Silova

The invention relates to the preparation of new polysaccharide derivatives comprising a double bond in the positions 4 and 5 of the pyranose cycle. The method of preparation consists in the oxidation of OH group in the position 6 to an aldehyde, followed by the elimination to form a double &#x2014;C&#x2550;C&#x2014; bond in the positions 4 and 5, and the final reduction of the aldehyde group in the position 6 into the original alcohol. The derivatives of polysaccharides prepared according to the invention show an enhanced antioxidant activity and some of them also a selective negative influence on carcinoma cell viability. (formula) where R represents &#x2014;NH&#x2014;CO&#x2014;CHor &#x2014;OH. 

Unsaturated derivatives of polysaccharides, method of preparation thereof and use thereof

The invention relates to conjugates of hyaluronic acid oligomer according to the general formulae I, II III or IV, or a salt thereof, the method of preparation thereof and use thereof, where the oligomer is bonded to the respective substrate by its ending anomeric center via a bi-functional amino linker by means of an amino or imino bond. This type of conjugates allows releasing oligomers in their native form. The prepared systems exhibited an enhanced biological activity against selected lines of cancer cells. 

Conjugates of oligomer of hyaluronic acid or of a salt thereof, method of preparation thereof and use thereof

The invention relates to the preparation and use of &#x3b1;,&#x3b2;-unsaturated aldehyde of hyaluronan having a double bond in the positions 4 and 5 and an aldehydic group in the position 6 of the glucosamine part of the polysaccharide. The method of preparation is based on dehydration of hyaluronan having an aldehydic group in the position 6 of the glucosamine part of the polysaccharide. Two methods have been described, which are dehydration in a solution or heating in solid state in absence of solvents, bases or other additives. This derivative allows stabilization of conjugates of hyaluronan with amino compounds by means of a multiple bond from the aldehyde side, and therefore, it is possible to effectively immobilize practically any compound containing an amino group to such modified hyaluronan in physiological conditions. In case of using a diamine or compounds or polymers containing three or more amino groups, it is possible to prepare crosslinked hyaluronan derivatives. The described solution brings along a significant advantage not only in the field of carriers of biologically active substances, but also in tissue engineering where crosslinking with biologically acceptable amino compounds in physiological conditions is very much demanded. 

Hyaluronic acid derivative, method of preparation thereof, method of modification thereof and use thereof

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Petra Sedova