Общество с ограниченной ответственностью "НПО Петровакс Фарм" (RU)
发明人:
Некрасов Аркадий Васильевич (RU),Медведев Сергей Алексеевич (RU),Козюков Александр Владимирович (RU),Карапутадзе Темури Мусаевич (RU),Пучкова Наталья Григорьевна (RU)
申请号:
RU2013132161/10
公开号:
RU2013132161A
申请日:
2013.07.11
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
1. A conjugate of glycoprotein having the activity of erythropoietin derivatives with polietilenpiperazina N-oxide corresponding to the general formula (1) [- ABC- (DC (O) -NH-EPO) -], and having a molecular weight of 50-190 kDa, where C (O) -group copolymer, which forms a covalent chemical bond with an amino amide glycoprotein NH-EPO, Aoboznachaetgde k - number of units containing etilenpiperazin equal 50-235, Boboznachaetgde l - number of units containing N-oxide etilenpiperazina equal 120-475 Coboznachaetgde Hal- halogen, m - the number of units containing a functional group is equal to 4-77 group (D-CO-NH-EPO) oboznachaetgde Hal- halo, p - the number of units containing erythropoietin (EPO), from 1 to 3, n = k + l + m + p is a number from about 175 to 790, wherein etilenpiperazinovye units a, B, C and D are interconnected copolymer by chemical bonds and are distributed along the chain statisticheski.2 copolymer. The conjugate of claim 1, wherein Haloznachaet Br, Cl, 3. The conjugate of claim 1, wherein the copolymer comprises derivative etilenpiperazina N-oxide, a molecular weight of from 20 kDa to 90 kDa, which is biodegradable fragment 4. The conjugate corresponding to the general structural formula (II): where EPO - glycoprotein is erythropoietin alpha or beta R - means -COOH, Haloznachaet - Br, Cl k - number of units containing etilenpiperazin, from 50 to 235 l - number units containing etilenpiperazina N-oxide, from 120 to 475 p - the number of units containing EPO, from 1 to 3 m - the number of units containing a functional group R, - 4-77 n = k + l + m + p = 175-790.5. The conjugate according to claim 1 for the treatment of anemia associated with chronic renal failure, cancer patients undergoing chemotherapy patients SPIDom.6. The conjugate of claim 1, having prol1. Конъюгат гликопротеина, обладающего активностью эритропоэтина, с производными N-оксида полиэтиленпиперазина, соответствующий общей формуле (1)[-Aк-Bl-Cm-(D-C(O)-NH-EPO)p-]n,и имеющий молекуля