IVASHCHENKO ANDREJ ALEKSANDROVICH,Иващенко Андрей Александрович,IVASHCHENKO ALEKSANDR VASILEVICH,Иващенко Александр Васильевич,MITKIN OLEG DMITRIEVICH,Митькин Олег Дмитриевич
申请号：
RU2013152522/04
公开号：
RU0002553996C1
申请日:
2013.11.27
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: present invention relates to a novel (2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate of general formula I or a stereoisomer or a pharmaceutically acceptable salt thereof, having properties of nucleoside inihibitors of RNA polymerase NS5B of the hepatitis C virus. The invention also relates to a method of producing compounds, pharmaceutical compositions and a medicinal agent based on said compounds. In general formula 1 , R1 is hydrogen, (CH3)2[(CH3)3C]Si, C2-C6acyl, optionally substituted with a benzyloxy group, NR5R6 group, wherein R5 and R6 are independently hydrogen or C1-C4alkyl 1-pyrrol-2-ylcarbonyl, piperidin-3-ylcarbonyl or piperidin-4-ylcarbonyl R2 and R3 are F or R2 is F or OH and R3 is CH3 R4 is hydrogen or methyl Ar is phenyl, pyridyl or naphthyl, where the phenyl, pyridyl or naphthyl is optionally substituted with at least one of C1-3alkyl, C2-4alkenyl, C2-4alkynyl, C1-3alkoxy, F, Cl, Br, I, nitro, cyano, -N(C1-3alkyl)2 Pm is 2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl or 4-(4-amino-2-oxo-2H-pyrimidin-1-yl), wherein the amino group is optionally substituted with 1-pyrrol-2-ylcarbonyl, piperidin-3-ylcarbonyl, piperidin-4-ylcarbonyl or a C(O)R8 radical, where R8 is C1-C4alkyl, optionally substituted with a NR6R7 group, where R6 and R7 are independently hydrogen or C1-C4alkyl C1-3alkoxy, optionally substituted with a phenyl X is O or N-R9, where R9 is C1-C4alkyl, optionally substituted with OH or OCH3 n=1, 2 or 3.EFFECT: compounds can be used to prevent and treat viral infections, including hepatitis C.12 cl, 1 tbl, 11 exДанное изобретение относится к новому (2R,3R,5R)-3-гидрокси-(5-пиримидин-1-ил)тетрагидрофуран-2-илметил арил фосфорамидату общей формулы 1 или его стереоизомеру, или фармацевтически приемлемой соли, которые обладают свойствами нуклеозидных ингибиторов РНК-полимеразы NS5B вируса гепатита С. Соединения могут найти применение для профилактики и лечения вирусных инфекций, включая г
