CLOSED JOINT STOCK COMPANY "BIOCAD";MOROZOV, Dmitriy Valentinovich
发明人:
CHERNOVSKAYA, Tatyana Veniaminovna,DENISOV, Lev Alexandrovich,RUDENKO, Elena Georgievna,KLENOVA, Angelina Vsevolodovna
申请号:
RURU2010/000529
公开号:
WO2012/011836A1
申请日:
2010.09.24
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
The invention is related to the pharmaceutical industry and medicine, in particular, to new PEG-interferon derivatives and the discovery of a new functionally active, highly stable conjugate of interferon to polyethylene glycol with an activity of interferon alpha, with reduced immunogenicity, with prolonged biological effects and improved pharmacokinetic parameters of general formula: (I) where: n - integral values from 227 to 10 000, so that the molecular weight of PEG is about 10 000 - 40 000 Da; m - integer >; 4; IFN- natural or recombinant polypeptide having the activity of IFN-alpha. Also, the invention is related to drugs containing the declared conjugate of the formula (I), pharmaceutical compositions containing PEG-IFN conjugate and therapeutically acceptable excipients suitable for treatment of viral infections and cancer, as well as diseases associated with primary or secondary immunodeficiency. The invention is related to the use of conjugate of formula (I) in medicinal products, which have antiviral, antiproliferative and immunomodulatory activity, to approaches for prevention and / or treatment of diseases associated with primary or secondary immunodeficiency that include administration of therapeutically effective amount of conjugate of formula (I), and to the container with such pharmaceutical composition.Cette invention concerne l'industrie pharmaceutique et la médecine, en particulier, de nouveaux dérivés de PEG-interféron et la découverte d'un nouveau conjugué très stable et fonctionnellement actif d'interféron et polyéthylène glycol ayant une activité interféron alpha, une immunogénicité réduite, des effets biologiques prolongés et des paramètres pharmacocinétiques améliorés, de formule générale : (I), n dans la formule représentant des valeurs entières de 227 à 10 000, de façon que le poids moléculaire du PEG soit d'environ 10 000 à 40 000 Da; m - étant un entier >; 4; et IFN-, un polypeptide naturel ou recombinant ayant une activité IFN-alp