COMPOUNDS WHICH ARE ANTAGONISTS OF THE A3-ADENOSINE RECEPTOR, A METHOD FOR PREPARING THEM AND MEDICAL USE THEREOF Russian patent published in 2020 - IPC C07D471/04 C07D487/04 A61K31/4196 A61K31/437 A61K31/4985 A61P27/06 

FIELD: pharmaceuticals.

SUBSTANCE: invention refers to a compound of formula I or its pharmaceutically acceptable salt. In formula IX is sulfur or oxygen; Z¹ and Z² are identical or different and each independently represents nitrogen or CH; R¹ denotes NR³R⁴, wherein said R³ and R⁴ each independently denotes H, C1-6 alkyl, substituted C1-6 alkyl, C3-7 cycloalkyl, substituted C3-7 cycloalkyl or heterocycle, R² represents H or halogen; wherein substituted C1-6 alkyl is C1-6 alkyl substituted with one or more substituents, selected from the group consisting of C1-3 alkyl, optionally having from one to three fluorine substitutes, amino, aryl, heteroaryl, heterocycle and halogen; substituted C3-7 cycloalkyl is C3-7 cycloalkyl, substituted with one substitute selected from aryl; aryl is phenyl, optionally substituted with one or more substitutes selected from a group consisting of substituted C1-3 alkyl, optionally having from one to three fluorine substitutes, heteroaryl, heterocycle, aryl, C1-3 alkoxy, optionally having from one to three fluoro substitutes, aryloxy, acyloxy, carboxy, amino, cyano and halogen; heteroaryl is benzoimidazolyl, furanyl, imidazopyridinyl, indolyl, oxazolyl, oxadiazolyl, pyridyl, pyrazinyl, pyrimidyl, thiophenyl, tetrazolyl or thiazolyl, optionally substituted with one or more substitutes selected from C1-3 alkyl; and the heterocycle is piperidinyl, piperazinyl or morpholinyl; or a compound selected from the group given in the claim. Invention also relates to a pharmaceutical composition, to a method for preventing, relieving the severity or treating a condition, to a method for antagonizing the A3-adenosine receptor.

I

EFFECT: technical result is obtaining novel compounds of formula I, which have the properties of the antagonist of the A3-adenosine receptor and are useful in treating glaucoma.

10 cl, 5 tbl, 244 ex