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, C1-6 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, C2-6 alkynyl, ORb, C3-12 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 C5-8 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 C2-6 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 Rb 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, ORb, RbO-C1-4 alkylene, C1-10 alkyl, C1-6 haloalkyl, C3-6 cycloalkyl, C6 aryl, C6-10 aryl-C1-4 alkylene or 6-member heterocyclyl containing 1 to 2 heteroatoms independently selected from N, O and S, where Rb represents H, C1-6 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 C1-6 alkyl; W is C6-8 mono- or b-carbocyclic system; each V and V' independently represent C5-8 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 Rw independently represents -C(=O)ORb, -NRcRd or C1-6 alkyl, where each Rb, Rc and Rd independently represents H, C1-6 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
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Authors
Dates
2020-11-25—Published
2016-12-08—Filed