SERINE/THREONINE KINASE INHIBITORS Russian patent published in 2018 - IPC C07D401/04 C07D401/14 C07D405/14 C07D409/14 C07D413/14 C07D417/14 A61K31/435 A61K31/506 A61P29/00 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound selected from Formula I: I in which X₁ is selected from CH and N; X₂ is selected from CR⁵ and N; Y₁ is selected from CR⁶ and N; Y₂ is selected from CR⁷ and N; R¹ is selected from: (a) C₁-C₆ alkyl optionally substituted with one or more groups independently selected from halogen, OR^a, NR^bR^c, C₃-C₆ cycloalkyl and 3-7 membered heterocycle containing one heteroatom selected from O, (b) C₃-C₇ cycloalkyl optionally substituted with one or more groups independently selected from halogen and OR^a, (c) phenyl optionally substituted with one or more groups independently selected from halogen and C₁-C₃ alkyl, (d) 4-6 membered saturated heterocycle containing one heteroatom selected from the group consisting of O, S and N, optionally substituted with one or more groups independently selected from halogen, oxo and C₁-C₃ alkyl optionally substituted with one or more OR^d, (e) 5-6 membered heteroaryl containing one, two, three or four heteroatoms selected from the group consisting of N and O, optionally substituted with one or more groups independently selected from halogen, OR^e, oxide, CN, C₃-C₆ cycloalkyl and C₁-C₃ alkyl optionally substituted with one or more groups independently selected from halo, oxo and OR^d, and (f) 7-10 membered bicyclic saturated or partially unsaturated heterocycle containing one or two heteroatoms, selected from the group consisting of O and N, optionally substituted with one or more groups independently selected from oxo and C₁-C₃ alkyl; values of other radicals are given in the patent claim. Invention also relates to individual compounds, to pharmaceutical compositions, to the use of the compound, to methods for inhibiting ERK protein kinase activity, to a method for treating or alleviating the severity of a hyperproliferative disorder modulated by ERK, to a method of treating or alleviating the severity of rheumatism, to a compound of Formula 10.1, to a compound of Formula 10.2, a compound of Formula 10.6, to a process for the preparation of a compound of Formula 10.1, to a process for the preparation of a compound of Formula 10.2, to a process for the preparation of a compound of Formula 10.6, to a process for the preparation of a compound of Formula 10.8, to processes for the preparation of a compound of Formula I, to a compound selected from Formula XI.

EFFECT: technical result: new compounds of Formula I have been obtained which possess ERK inhibitory activity.

159 cl, 2 tbl, 66 ex