COMPOUNDS BASED ON 7-SUBSTITUTED PYRROLOTRIAZINE OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS AND METHODS FOR THEIR PREPARATION AND APPLICATION Russian patent published in 2021 - IPC C07D487/04 C07D519/00 A61K31/53 A61K31/5377 A61K31/5386 A61P35/00 A61P35/02 A61P37/00 

FIELD: organic chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to a compound based on a 7-substituted pyrrolo[2,1-f][1,2,4] triazine of the general formula I or to a pharmaceutically acceptable salt thereof, where R₁ is halogen, or C_1-6alkyl, which is unsubstituted or substituted by at least one substituent, the substituent being halogen; R₂ is: unsubstituted or substituted with one or two substituents -CH₂NH-C_1-6alkyl, -CH₂N(C_1-6alkyl)-(C_1-6alkyl), -CH₂-(saturated heterocyclyl containing 1-2 heteroatoms and 4-5 carbon atoms), -CH₂-(saturated heterocyclyl containing 1-2 heteroatoms and 3-5 carbon atoms)-(saturated heterocyclyl containing 1-2 heteroatoms and 3-5 carbon atoms), -CH₂-(saturated spirocyclic group containing 2 heteroatoms and 5-7 carbon atoms), -CH₂-(saturated bridging ring group containing 2 heteroatoms and 5 carbon atoms)-(saturated heterocyclyl containing 1 heteroatom and 3 carbon atoms), or -CH₂- (saturated ring group with bridging bond containing 2 heteroatoms and 5 carbon atoms), where the substituent is: -N(C_1-4alkyl)-(C_1-4alkyl), -S(O)₂-C_1-4alkyl, -C_1-4alkyl-N (C_1-4alkyl)-(C_1-4alkyl), C_1-4alkyl-O-C_1-4alkyl which is substituted with two methyls, -C_1-4alkyl-CONH₂ which is substituted with two methyls, -COO-C_1-4alkyl, -CO-C_1-4alkyl which i is substituted with one substituent A, where substituent A is hydroxyl, or C_1-4 alkyl, which is unsubstituted or substituted with one to three substituents B, where substituent B is -NH₂, -OCH₃, -CONH₂, -OH, or -CF₃; in R₂, the heteroatom is selected from the group consisting of: (i) N, and (ii) a combination of N and one of O and S; R₃ is , where each of R₇, R₈, R₉ and R₁₀ is independently hydrogen or C_1-6alkyl, which is unsubstituted; R₄ is -NH₂, -NHCONHR₁₁ or -NHCO₂R₁₂, where each of R₁₁ and R₁₂ is independently C_1-6alkyl, C_3-8cycloalkyl or phenyl, which is unsubstituted or substituted with one substituent selected from halogen and -C(O)OR₁₃, where R₁₃ is C_1-6alkyl, which is unsubstituted. The invention also relates to the use of a compound of the formula I and to a pharmaceutical composition based on it.

EFFECT: new heterocyclic compounds have been obtained that effectively inhibit the activity of PI3K kinase and are useful for the treatment of diseases associated with the PI3K pathway, especially for the fight against cancer or for the treatment of tumors, including leukemia, and autoimmune diseases.

17 cl, 5 tbl