DIAMINOPYRIMIDINES AS P2X RECEPTOR ANTAGONISTS Russian patent published in 2011 - IPC C07D239/48 C07D403/12 C07D405/12 C07D409/12 C07D413/12 C07D417/12 A61K31/505 A61P13/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I) and to their pharmaceutically acceptable salts exhibiting P2X₃ receptor antagonist activity. In formula (I), X represents -O-; Y represents -NR^dR^e where one of radicals R^d and R^e means hydrogen, and the other means hydrogen; C₁-C₁₂alkyl; C₅-C₇cycloalkyl; C₅-C₇cycloalky-C₁-C₁₂alkyl; hydroxy-C₁-C₁₂alkyl; acetyl; aminocarbonyloxy- C₁-C₁₂alkyl or heterocyclyl representing a 6-members saturated ring containing heteroatom S substituted by two oxo groups; D represents optional oxygen; R¹ represents isopropyl; R² represents hydrogen; R⁵ represents hydrogen or C₁-C₁₂alkyl; R⁴ means hydrogen; C₁-C₁₂alkyl; halogen; halogen- C₁-C₁₂alkyl; C₁-C₁₂alkoxy; hydroxy; halogen- C₁-C₁₂alkoxy; nitro; amino; hydroxy- C₁-C₁₂alkyl; C₁-C₁₂alkoxyalkyl; hydroxy- C₁-C₁₂alkoxy; C₁-C₁₂alkylsulphonyl; cyano; heteroaryl representing a 5-members aromatic ring containing one, two or three heteroatoms selected from O, S and N which can be optionally substituted by a thio group, C₁-C₁₂alkyl or C₁-C₁₂alkylsulphonyl; heterocyclyl representing a 6-members saturated ring containing two heteroatoms N, one of which is substituted C₁-C₁₂alkylsulphonyl; -(CH₂)_m-(Z)n-(CO)-R^f or -(CH₂)_m-(Z)_n-SO₂-(NR^g)_n-R^f where each m and n independently represents 0 or 1, Z means NR⁸, R^f means C₁-C₁₂alkyl, hydroxy, amino or hydroxy- C₁-C₁₂alkyl, and R^g means hydrogen; R³ represents methoxy; R⁶ represents hydrogen; and one of radicals R⁷ and R⁸ represents hydrogen, and the other represents hydrogen, acetyl or phenyl.

EFFECT: also, the invention refers to a pharmaceutical composition and to an application of the compound of formula (I) for preparing a drug.

8 cl, 3 tbl, 70 ex