NEW ACYLATED PSEUDODIPEPTIDES WITH ACCESSORY FUNCTIONALIZED BRANCHING, METHODS FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEREOF Russian patent published in 2006 - IPC C07K5/02 C07K1/02 C07C237/22 A61K31/66 A61K39/39 A61P37/02 

Abstract RU 2275378 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new N-acylated pseudodipeptides comprising acidic group in neutral or charged form by one end of pseudodipeptide and accessory functionalized branching by the opposite end and corresponding to the general formula (I): wherein each R1 and R2 means acyl group of saturated or unsaturated, linear or branched carboxylic acid comprising from 2 to 24 carbon atoms, unsubstituted or comprising a substitute or substitutes chosen from hydroxyl, alkoxy- and acyloxy-groups; coefficient n has values from 0 to 3; coefficients p and q have values from 1 to 3; coefficient m has values from 1 to 3 except for a case when X means carboxyl or one of its derivative, and in this case it means values form 0 to 3; Y means oxygen atom (O) or -NH; X and Z mean accessory functionalized branching or acidic group in neutral or charged form chosen from the following groups: carboxyl, carboxy-(C1-C5)-alkoxy-, carboxy-(C1-C5)-alkylthio-, phosphono-(C1-C5)-alkoxy-, dihydroxyphosphoryloxy-, hydroxysulfonyloxy-, (carboxy-(C1-C5)-alkyl)aminocarbonyl, (dicarboxy-(C1-C5)-alkyl)aminocarbonyl, (ammonio-(C1-C5)-aminocarbonyl, carboxy-(amino-(C1-C5)-alkyl)aminocarbonyl under condition that at least one substitute among X and Z means an accessory functionalized branching, and their enantiomers and diastereoisomers. Proposed compounds show immunomolulating properties as adjuvants and these compounds can be grafted to antigen to modulate the immune response or can be grafted to pharmacophore to improve the therapeutic effect or its directed delivery.

EFFECT: improved preparing methods, improved and valuable medicinal properties of substances and compositions.

48 cl, 3 tbl, 112 dwg, 5 ex

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RU 2 275 378 C2

Authors

Boer Zhak

Martehn Oliv'E Rishar

Rodrige Sil'Ven

Dates

2006-04-27Published

2000-12-21Filed