CONDENSED HETEROARYLS AND THEIR APPLICATION Russian patent published in 2015 - IPC C07D471/04 C07D471/14 C07D487/04 A61K31/4745 A61K31/4375 A61K31/4985 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of formula (1) and/or to their pharmaceutically acceptable salts, where A¹ represents CH; A⁴and A⁵ independently represent CR² or N; A² and A³ together with ring B represent 5-membered heteroaryl or heterocycle, with said 5-membered heteroaryl or heterocycle being selected from where t represents 1 or 2; and R³ is independently selected from H, C₁-C₆ alkyl, C₆-aryl, C₃-C₆-membered cycloalkyl, C(O)NR^cR^d, -OR^b, heteroaryl, representing pyridine, and heterocycle, representing piperidine and tetrahydropyran; and each of said alkyl, aryl, cycloalkyl, heteroaryl and heterocycle can be substituted with one group, independently selected from C₁-C₆ alkyl, possibly substituted with one substituent, selected from -CONMe₂, C₃-membered cycloalkyl, -CN, -OMe, -pyridine, tetrahydropyran, -CO-morpholine, -CO-pyrrolidine, (3-methyl)oxetane; -OH; -C(O)R^a; -CN; -C(O)NR^cR^d; -NR^cR^d; -OR^b; -S(O)_nR^e; halogen, and substituted with one group -COMe heterocycle, representing piperidine, on condition that when A⁴ represents CR², A² and A³ together with ring B are selected from structure (3), (5) or (6); represents single bond or double bond; R¹ represents heteroaryl, representing 6-membered or 9-10-membered aromatic mono- or bicyclic ring, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; possibly substituted with one or two groups, independently selected from C₁alkyl, C₂alkinyl, -NR^cR^d, -NR^cS(O)_nR^e, -OR^b, halogen, halogenalkyl; R² is independently selected from H; each R^a, R^b, R^c, R^d, and R^e is independently selected from H; C₁-C₄alkyl, possibly substituted with one substituent, selected from -OH, -OMe, -CN, -NH₂, -NMe₂, C₃-cycloalkyl; C₂-C₃alkenyl; C₃alkinyl; C₆aryl, possibly substituted with one or more substituents, selected from fluorine or methyl group; C₃-membered cycloalkyl, possibly substituted with one substituent, selected from -OH and -CN; halogenalkyl; heteroaryl, representing pyridine; and substituted with one methyl group heterocycle, representing piperidine, or R^c and R^d together with atom (atoms) which they are bound to form 5-6-membered heterocyclic ring, representing pyrrolidine or morpholine; and in each case n is independently equal 2. Invention also relates to particular compounds, pharmaceutical composition, based on claimed compounds; method of inhibiting PI3K and/or mTOR activity and to application of claimed compounds.

EFFECT: novel compounds, useful for inhibiting PI3K and/or mTOR activity have been obtained.

15 cl, 16 ex