ALKYL2-{[(2R,3S,5R)-5-(4-AMINO-2-OXO-2H-PYRIMIDINE-1-YL)- -HYDROXY- TETRAHYDRO-FURAN-2-YLMETHOXY]-PHENOXY-PHOSPHORYLAMINO}-PROPTONATES, NUCLEOSIDE INHIBITORS OF RNA-POLYMERASE HCV NS5B, METHODS FOR PRODUCING AND USING THEM Russian patent published in 2014 - IPC C07H19/10 A61K31/7068 A61P31/16 A61P31/12 C07F9/44 C07F9/6558 A61K31/664 A61K31/665 

Abstract RU 2534613 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of general formula 1 or their stereoisomers or pharmaceutically acceptable salts possessing the properties of inhibitors of RNA polymerase HCV NS5B, and to methods for producing them. In general formula 1 R1 represents C1-C4alkyl; R2 and R3 represents fluorine, or R2 represents fluorine, while R3 represents methyl; one of R4 and R5 represents hydrogen, and the other of R4 and R5 represents C1-C6acyl optionally substituted by α-aminoacyl specified in a group containing (dimethylamino)acetyl, 1-tert-butoxycarbonylamino-2-methyl-propylcarbonyl, 1-methylpyrrolidine-2-carbonyl, 1-methylpiperidine-3-carbonyl and 1-methylpiperidine-4-carbonyl, R6 represents hydrogen, methyl, methoxy and halogen.

EFFECT: compounds can be used for treating and preventing viral infections, including hepatitis C, optionally with additional agents specified in an inhibitor of inosin-5-monophosphate dehydrogenase, eg Ribamidine, an inhibitor of hepatitis C protease C NS3, eg Asunaprevir (BMS-650032), an inhibitor of hepatitis C protease C NS3/4A, eg Sofosbuvir (TMC435), an inhibitor of RNA-polymerase NS5A, eg Daclatasvir (BMS-790052) or Ledipasvir (GS-5885).

18 cl, 1 tbl, 14 ex

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RU 2 534 613 C2

Authors

Ivashchenko Aleksandr Vasil'Evich

Dates

2014-11-27Published

2013-03-22Filed