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1. (WO2017153950) INHIBITORS OF INFLUENZA VIRUS NUCLEASE (POLYMERASE COMPLEX)

Pub. No.:    WO/2017/153950    International Application No.:    PCT/IB2017/051397
Publication Date: Fri Sep 15 01:59:59 CEST 2017 International Filing Date: Fri Mar 10 00:59:59 CET 2017
IPC: A61K 31/216
A61K 31/343
A61K 31/235
A61K 31/215
C07C 69/76
C07D 317/68
C07C 233/33
C07C 69/757
A61P 31/12
Applicants: BIOTECH INNOVATIONS SPÓŁKA Z OGRANICZONĄ ODPOWIEDZIALNOŚCIĄ
Inventors: KAMIŃSKA, Katarzyna
BUJNICKI, Janusz
Title: INHIBITORS OF INFLUENZA VIRUS NUCLEASE (POLYMERASE COMPLEX)
Abstract:
The 4-hydroxyphenyl-2-oxoethyl carboxylic derivatives of the general formula: R1-A- R2, wherein the core A is: Formula (I) and R1 is phenyl substituted with two C1-C4 alkyl, 1,3-benzodioxolyl or bicyclo[3.3.1]nonanyl and R2 is H, hydroxyl, amino group optionally substituted with carbonyl- C1-C4 alkyl or amide optionally substituted by C1-C4 alkyl; as well as their pharmaceutically acceptable salts, solvates, polymorphs, co-drugs, cocrystals, prodrugs, tautomers, racemates, enantiomers or diastereomers, or mixtures thereof; as endonucleolytic activity inhibitors in viruses with segmented negative- sense RNA genome for use as an antiviral drug. The invention further includes the use of the said derivative for manufacturing of a medicine for treatment, alleviation or prophylaxis of viral infection caused by viruses from Orthomyxoviridae family among others, including influenza and its complications, as well as for combination therapy with neuraminidase inhibitor, amantadine, neuraminidase, amantadine or rimantadine, or any other combination thereof.