JAK KINASE-MODULATING QUINAZOLINE DERIVATIVES AND METHODS OF APPLYING THEREOF Russian patent published in 2014 - IPC C07D401/14 C07D403/12 C07D405/14 C07D413/14 A61K31/517 A61P19/00 A61P29/00 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) , where R¹ and R² have the following values: (i) R¹ and R² together form =O; (ii) R¹ and R² together with carbon atom, which they are bound with, form duoxacycloalkyl; R¹ represents hydrogen or halogen; and R² represents halogen; (iv) R¹ represents C_1-6alkyl, where alkyl is optionally substituted with cyano, -R^xS(O)_qR^v or -R^xNR^yR^z; and R² represents hydrogen; (v) R¹ represents -OR¹² or -NR¹³R¹⁴; and R² represents hydrogen, deutero or phenyl, which is optionally substituted with halogen; R³ represents hydrogen, halogen, C_1-6alkyl, cyano, halogen C_1-6alkyl, C_3-10cycloalkyl or C_1-6alkoxy; R⁴ and R⁵ represent hydrogen; R⁶ is independently selected from halogen, C_1-6alkyl, halogenC_1-6alkyl, -R^xOR¹⁸ and -R^xS(O)_qR^v; R⁷ independently represents halogen or -R^xOR^w; R¹² is selected from hydrogen and C_1-6alkyl, R¹³ represents hydrogen; R¹⁴ is selected from hydrogen, C_3-10cycloalkyl, -C(O)R^v and -C(O)OR^w; R¹⁸ represents hydrogen, C_1-6alkyl, or pyperidinyl, where R¹⁸ is optionally substituted with 1-3 Q¹ groups, each Q¹ is independenly selected from hydroxyl, C_1-6alkoxy, C_1-6alkoxycarbonyl, carboxyl and morpholinyl; R^x independently represents C_1-6alkylene or simple bond; R^v and R^w represent hydrogen or C_1-6alkyl; R^y and R^z represent hydrogen; n has value 0-4; p has value 0-5; and each q independently has value 0, 1 or 2. Invention also relates to compounds of formula (II) , where substituents have values, given in the invention formula, to pharmaceutical composition, possessing inhibiting activity with respect to JAK kinases, containing compounds of formula (I) or (II), methods of treating JAK-modulated disease, and application of compounds of formula (I) or (II).

EFFECT: compounds of formula (I) or (II) as inhibitors of JAK kinases.

32 cl, 6 dwg, 2 tbl, 84 ex