INHIBITORS JAK2 AND ALK2 AND METHODS OF USE THEREOF Russian patent published in 2019 - IPC C07D401/14 C07D239/42 A61K31/506 A61P35/00 

FIELD: chemistry; pharmaceutics.

SUBSTANCE: invention relates to a new compound of formula (I) or a pharmaceutically acceptable salt thereof. Compounds have the properties of ALK2 and/or JAK2 kinase inhibitors. Compounds show selective activity with respect to ALK2 relative to JAK2. Inhibition of ALK2 activity reduces the number of sudden exacerbations of a child's genetic disease, called progressive ossificating fibrodysplasia (FOR). In formula (I)

A denotes 6-member heteroaryl ring containing a nitrogen atom; X is -NH-; R¹ is H, halogen or C₁-C₆ alkoxy group; R² is halogen or C₁-C₆ alkoxy group; R³ is halogen, C₁-C₆ alkoxy group or -(CH₂)_nNR^aR^b; R⁴ is H; R⁵ is H; each of R⁶ and R⁷ independently is H, halogen, hydroxyl, C₁-C₆ alkyl, C₁-C₆ cyanoalkyl or C₃-C₆ cyanocycloalkyl; R⁸ is 6-member heteroaryl containing a nitrogen atom, optionally substituted alkylaminoalkyl; each of R^a and R^b independently is -H, C₁-C₆ alkyl, C₁-C₆ hydroxyalkyl, or R^a and R^b together with nitrogen atom, to which they are attached, form 5- or 6-member is a saturated carbocyclic or heterocyclic ring optionally substituted with one or more substituents selected from C₁-C₆ alkyl, C₁-C₆ carboxyalkylcarbonyl and C₁-C₆ hydroxyalkyl; n equals 0 or 1; and z equals 0 or 1. Invention also relates to a method of producing compounds of formula I. Method is carried out according to the following scheme

.

Values of radicals correspond to values specified above. LG and LG' represents a leaving group - halogen.

EFFECT: compounds can be used for treating anemia of a chronic disease, anemia of chronic inflammation, anemia of oncological disease or progressive ossificating fibrodysplasia, as well as for treating myeloproliferative disorder, lymphoma, solid tumor, glioma, fibrodysplasia.

44 cl, 9 dwg, 2 tbl, 2 ex