ASPARTYL DERIVATIVES OF HISTAMINE, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND THEIR USING AS MODULATORS OF ENZYME ACTIVITY OF ANTIOXIDANT PROTECTION Russian patent published in 2006 - IPC C07D233/64 C07D233/54 A61K31/417 A61K38/05 C07D233/00 

Abstract RU 2287524 C1

FIELD: bioorganic chemistry, biochemistry, pharmacy.

SUBSTANCE: invention relates to novel aspartyl derivatives of histamine of the general formula (I): , wherein R means hydrogen atom (H), or , or that are able to modulate activity of enzymes of antioxidant protection - superoxide dismutase (SOD) and catalase. Also, invention relates to using the known compounds of the general formula (I) for the same designation wherein at the same values of X the value R represents acetyl group, and to their pharmaceutically acceptable salts. Also, invention relates to a pharmaceutical composition possessing capacity to modulate activity of SOD and catalase and comprising the effective amount of compound of the general formula (I), and to a method for synthesis of compounds of the general formula (I). Method involves interaction of pentafluorophenyl ester Nα-Z-, β- or α-benzyl ester of aspartic acid with histamine followed by hydrogenolysis without isolation of intermediated protected derivatives of aspartyl histamine.

EFFECT: improved method of synthesis, valuable biochemical properties of derivatives.

12 cl, 3 tbl, 2 sch, 2 dwg, 8 ex

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RU 2 287 524 C1

Authors

Nebol'Sin Vladimir Evgen'Evich

Zheltukhina Galina Aleksandrovna

Kromova Tat'Jana Aleksandrovna

Dates

2006-11-20Published

2005-03-31Filed