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COMBINATION OF CYCLOSPORIN DERIVATIVE AND NUCLEOSIDES FOR TREATMENT OF HEPATITIS C VIRUS INFECTION
专利权人:
ИНК. (US);САЙНЕКСИС
发明人:
ХОПКИНС Сэмюэль Эрл (US)
申请号:
RU2011127079/15
公开号:
RU2011127079A
申请日:
2010.01.07
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
1. A method of treating HCV infection in a patient in need thereof, which comprises administering to the patient a therapeutically effective amount of: (a) 3 - [(R) -2- (N, N-dimethylamino) ethylthio-Sar] -4- (gammahydroxymethyl- leucine) cyclosporin or a pharmaceutically acceptable salt, solvate or hydrate thereof, and (b) a compound of formula (I): wherein R has the formula (Ia) or (Ib): and R and R are independently hydrogen, a phosphorus-containing group or a -C group (= O ) CH (alkyl); or a pharmaceutically acceptable hydrate, solvate, acid addition salt or prodrug thereof. 2. The method of claim 1, wherein the compound of formula (I) is a compound wherein R is of formula (Ia) and each of R and R is hydrogen, or a prodrug thereof. The method of claim 1, wherein the compound of formula (I) is a compound wherein R is of formula (Ia) and each of R and R is —C (═O) CH (CH), known as R-7128.4. The method of claim 1, wherein the compound of formula (I) is a compound wherein R is of formula (Ib), R is hydrogen, and R is —P (═O) (OH) —O — P (= O) ( OH) -O-P (= O) OH, or a prodrug thereof. 5. The method of claim 1, wherein the compound of formula (I) is a compound wherein R is of formula (Ib), R is hydrogen, and R is phosphate of the formula -P (= O) (OR) NHCH (R) COR, where R 4 is phenyl; R 1 is methyl; and R is isopropyl, known as PSI-7851.6. The method according to any one of claims 1 to 5, wherein (a) 400 mg or more of 3 - [(R) -2- (N, N-dimethylamino) ethylthio-Sar] -4- (gammahydroxymethyl-leucine) cyclosporin is administered in day; and (b) a compound of formula (I) is administered in an amount of from about 50 mg per day to about 5000 mg per day. A composition containing: (a) 3 - [(R) -2- (N, N-dimethylamino) et1. Способ лечения инфекции ВГС у пациента, нуждающегося в этом, который включает введение пациенту терапевтически эффективное количество:(а) 3-[(R)-2-(N,N-диметиламино)этилтио-Sar]-4-(гаммагидроксиметил-лейцин)циклоспорина или его фармацевтически приемлемо
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