COMBINED TREATMENT BY A TOLL-LIKE RECEPTOR (TLR7) AGONIST AND A HEPATITIS B VIRUS CAPSID ASSEMBLY INHIBITOR Russian patent published in 2020 - IPC A61K31/506 A61K31/7064 A61P31/20 

Abstract RU 2718917 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: group of inventions relates to a pharmaceutical composition comprising a TLR7 agonist selected from [(1S)-1-[(2S,4R,5R)-5-(5-amino-2-oxo-thiazolo[4,5-d]pyrimidin-3-yl)-4-hydroxy-tetrahydrofuran-2-yl]propyl]acetate and 5-amino-3-[(2R, 3R, 5S)-3-hydroxy-5-[(1S)-1-hydroxypropyl]tetrahydrofuran-2-yl]-6H-thiazolo[4,5-d]pyrimidine-2,7-dione, and a HBV capsid assembly inhibitor selected from 3-[(8aS)-7-[[(4R)-4-(2-chloro-3-fluoro-phenyl)-5-ethoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-2,2-dimethyl-propanoic acid and 3-[(8aS)-7-[[(4S)-5-ethoxycarbonyl-4-(3-fluoro-2-methyl-phenyl)-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-2,2-dimethyl-propanoic acid, in a pharmaceutically acceptable carrier. Other objects relate to a method for preparing a drug, a method, a kit and use of a pharmaceutical composition for treating or preventing hepatitis B viral infection.

EFFECT: technical effect consists in the synergetic antiviral effect of the combined therapy using specific TLR7 agonist combinations and HBV capsid assembly inhibitors.

13 cl, 11 dwg, 3 tbl, 8 ex

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RU 2 718 917 C2

Authors

Daj, Lue

Gao, Lu

Dates

2020-04-15Published

2016-03-15Filed