COMPOSITIONS AND METHODS FOR INHIBITING VIRAL POLYMERASE Russian patent published in 2018 - IPC C07H19/14 C07H19/213 C07D487/04 C07D491/56 C07F9/6571 A61K31/7064 A61K31/519 A61P31/14 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to novel compounds of formula (I) which possess the properties of an inhibitor of viral RNA polymerase activity and replication of RNA viruses, such as orthomixovirus, paramyxovirus, arenavirus, bunyavirus, flavivirus, filovirus, togavirus, picornavirus and coronavirus, adenovirus, rhinovirus, hepatitis A virus, hepatitis C virus, poliomyelitis virus, measles virus, Ebola virus, Coxsackie virus, West Nile fever virus, smallpox virus, yellow fever virus, Dengue Fever virus, influenza A virus, influenza B virus, Lassa virus, lymphocytic choriomeningitis virus, Junin virus et al. In the formula (I)

L¹, L² and L³ each independently, are a bond or a linker -C(R⁰)₂-O-; L⁴, L⁵ and L⁶ each is a bond; R⁰, independently for each occurrence, is H or (C₁-C₆)alkyl; R¹, R² and R³ each independently, are selected from the group consisting of H; aminoacyl, wherein independently for each occurrence, aminoacyl -C(=O)CH(NH₂)(CH₂)_nCHR³⁰R³¹, where n is 0 or 1; and R³⁰ and R³¹ each independently are H or (C₁-C₆) alkyl; acyl, wherein independently for each occurrence, acyl is -C(=O)R⁴⁰, where R⁴⁰ is (C₁-C₆) alkyl; R¹⁰OC(O)-; phosphoryl; and aminophosphoryl, wherein independently for each occurrence, aminophosphoryl is -P(=O)(OR⁵⁰)NR⁵¹R⁵², where R⁵⁰ is selected from the group consisting of phenyl, naphthyl and -(CH₂)_mSC(=O)C(CH₃)₂CH₂OH, m is 1 or 2, R⁵¹ is H or (C₁-C₆) alkyl, and R⁵² is selected from the group consisting of H, (C₁-C₆) alkyl, benzyl and -CR⁶⁰R⁶¹C(=O)OR⁶², where R⁶⁰ and R⁶¹ each independently are H or (C₁-C₆) alkyl; and R⁶² is H or (C₁-C₆) alkyl; or R¹ and R², taken together, or R² and R³, taken together, may be selected from the group consisting of carbonyl, phosphoryl and (C₁-C₆) alkylphosphoryl; R⁴, R⁵ and R⁶ are H; R⁷ is H; R¹⁰, independently for each occurrence, is H or (C₁-C₆)alkyl.

EFFECT: invention relates to novel compounds which possess the properties of an inhibitor of viral RNA polymerase activity and replication of RNA viruses.

30 cl, 2 dwg, 19 ex, 8 tbl