INFLUENZA VIRUS REPLICATION INHIBITORS, METHODS OF APPLICATION AND USING Russian patent published in 2020 - IPC C07D471/04 C07D519/00 A61K31/437 A61K31/506 A61K31/517 A61P31/16 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, which have activity on influenza virus RNA polymerase. In formula (I), each R¹ and R³ independently represents H, F, Cl, Br, C_1-6 alkyl or C₆ aryl and where C₆ aryl is not independently substituted or substituted with one, two, three or four substitutes independently selected from F, Cl or Br; n is equal to 0, 1, 2 or 3; each R² independently represents F, C_2-6 alkynyl, OR^b, C_3-12 carbocyclyl, C₆ aryl or 5- to 14-membered heteroaryl comprising 1 to 4 heteroatoms independently selected from N, O and S, or two adjacent R² together with the atoms to which they are attached form C_5-8 carbocyclic ring, C₆ aromatic ring or 5- to 6-member heteroaromatic ring containing from 1 to 4 heteroatoms independently selected from N, O and S, and where each of C_2-6 alkynyl, C₆ aryl, from 5- to 14-functioned heteroaryl, C₆ aromatic ring and 5- to 6-member heteroaromatic ring is independently not substituted or substituted with one, two, three, four or five R', where R^b is C₆ aryl; provided that when m is 1, R² is not F and, when m is equal to 2, two of R² are not F simultaneously; each R' independently represents F, Cl, Br, CN, NO₂, OR^b, R^bO-C_1-4 alkylene, C_1-10 alkyl, C_1-6 haloalkyl, C_3-6 cycloalkyl, C₆ aryl, C_6-10 aryl-C_1-4 alkylene or 6-member heterocyclyl containing 1 to 2 heteroatoms independently selected from N, O and S, where R^b represents H, C_1-6 alkyl or C₆ aryl; m is 1 or 2; X has one of subformulas (X-2), (X-3) and (X-5), where R⁴ is H; each R⁵ and R⁶ independently represent H or C_1-6 alkyl; W is C_6-8 mono- or b-carbocyclic system; each V and V' independently represent C_5-8 cycloalkane ring, 5- to 6-member heterocyclic ring containing from 1 to 4 heteroatoms independently selected from N, O and S, or from 5- to 6-member heteroaromatic ring, containing from 1 to 4 heteroatoms independently selected from N and S; each R^w independently represents -C(=O)OR^b, -NR^cR^d or C_1-6 alkyl, where each R^b, R^c and R^d independently represents H, C_1-6 alkyl or C₆ aryl; s is 0 or 1; t is equal to 0; p is equal to 1. Invention also relates to a pharmaceutical composition for use in influenza virus RNA polymerase inhibition, containing an effective amount of said compound and optionally further comprising a pharmaceutically acceptable excipient, an adjuvant, a carrier or a combination thereof.

EFFECT: there are offered influenza virus replication inhibitors, methods for using them and use.

18 cl, 3 tbl, 80 ex