POLYANIONIC NORBORNAN DERIVATIVES, METHOD FOR PRODUCTION THEREOF AND REPRODUCTION INHIBITORS OF HUMAN IMMUNOGENICITY VIRUS BASED ON THE SAME Russian patent published in 2006 - IPC C08F224/00 C08F122/00 A61K31/341 A61P31/18 

Abstract RU 2281297 C2

FIELD: polymers, immunology.

SUBSTANCE: invention relates to polyanionic norbornan derivatives of formula I: , wherein or is residue of another oxygen-containing monomer, such as ; n>=15. Preferably n = 35-100 (polymerization ratio); M is H, Na, K, NH4; X is OH, OM, ONH3-Y-Nb, NH-Y-Nb, wherein not less 3 % of total X represent sum of ONH3-Y-Nb and NH-Y-Nb (modification ratio with norbornan), and spacer group -Y- represents - (Yi)m [Yi is CH , CH(CH3), CH(CH2CH3); m>=0, preferably m = 1-3). And norbornan pharmacophor has formula , wherein represents bicyclic norbornan carbon skeleton including seven carbon (C) atoms in 1-7 sites and one (any) substituent from R1, R2a, R2b, R3a, R3b, R4, R5a, R5b, R6a, R6b, R7a, R7b, represents covalent bond between Nb and Y; and the rest eleven substiruents represent H or alkyl, or two by two represent covalent chemical bond in bicyclic hydrocarbon skeleton, i.e. additional double bond between carbon atoms. Method for production of formula I compounds also is disclosed. Said compounds have high selectivity index in relation to HIV-1 strains, having resistance to known azidotimidine pharmaceutical agent.

EFFECT: polyanionic norbornan derivatives useful as active ingredients of antiviral pharmaceutical formulation.

3 cl, 6 ex, 2 tbl, 4 dwg

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RU 2 281 297 C2

Authors

Bukrinskaja Alisa Grigor'Evna

Burshtejn Marina Efimovna

Alikhanova Ol'Ga Leonidovna

Ermakov Igor' Vladimirovich

Kas'Jan Lilija Ivanovna

Kas'Jan Andrej Olegovich

Serbin Aleksandr Vladimirovich

Tarabara Igor' Nikolaevich

Dates

2006-08-10Published

2004-08-23Filed