IMIDAZOPYRROLOPYRAZINE DERIVATIVES, USEFUL FOR TREATMENT OF DISEASES, CAUSED BY ABNORMAL ACTIVITY OF PROTEINKINASES Jak1, Jak3 OR Syk Russian patent published in 2015 - IPC C07D471/14 C07D487/14 A61K31/437 A61K31/4985 A61P37/06 A61P11/06 A61P25/28 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of organic chemistry, namely to a novel imidazopyrrolopyrazine derivative of formula

and to its pharmaceutically acceptable salt, stereoisomer or isomer, where R¹, R² and R⁵ represent H; R³ represents (C₃-C₆)cycloalkyl, substituted with one group, independently selected from CH₂NH₂ or NH₂; or R³ represents -A-D-E-G, where: A represents a bond or -N(R^a)C(O)-R^e-; D represents (C₁-C₃)alkylene, bound by a bridge bond (C₈)cycloalkylene, (C₄-C₆)cycloalkylene, substituted with one substituent, selected from (C₁-C₃)alkyl; (C₄-C₅)monoheterocyclylene, optionally substituted with one substituent, selected from (C₁-C₃)alkyl, where monoheterocyclylene contains 1-2 heteroatoms, independently selected from carbon or oxygen atoms; E represents a bond, -R^e, -R^e-C(O)-R^e-, -R^e-O-R^e-, -R^e-N(R^a)-R^e-, -R^e-N(R^a)C(O)-R^e-, -R^eC(O)N(R^a)R^e-, -R^e-N(R^a)S(O)₂-R^e- or -R^e-N(R^a)S(O)₂N(R^a)-R^e-; where in all cases E is bound either with a carbon atom or with a nitrogen atom in D; G represents hydrogen, -N(R^a)(R^b), -(C₁-C₆)alkyl, optionally substituted with 1-3 substituents, independently selected from a halogen, hydroxyl or cyano; (C₃-C₆)monocycloalkyl, optionally substituted with 1-2 substituents, independently selected from a halogen, cyano, monocyclic (C₃-C₅)heteroaryl, optionally substituted with one substituent, independently selected from cyano, where heteroaryl contains 2 heteroatoms, independently selected from nitrogen atoms; (C₃-C₅)monoheterocyclyl, optionally substituted with 1 or 2 substituents, independently selected from methyl, -CF₃, halogen or CH₂CN, where monoheterocyclyl contains 1-2 heteroatoms, independently selected from nitrogen or oxygen atoms; (C₆)aryl, optionally substituted with 1-2 substituents, independently selected from a halogen or cyano; where in the fragment, containing -N(R^a)(R^b), nitrogen, R^a and R^b can form a ring in such a way that -N(R^a)(R^b) represents C₄monoheterocyclyl, where monoheterocyclyl contains 1-2 heteroatoms, independently selected from nitrogen or oxygen; R⁴ represents hydrogen or -(C₁-C₆)alkyl; R^a and R^b, each independently represent hydrogen, (C₁-C₆)alkyl, oxetane; and R^e for each case independently represents a bond or -(C₁-C₄)alkylene. The invention also relates to particular imidazopyrrolopyrazine derivatives, a pharmaceutical composition, based on the claimed compound and to the application of the claimed compound.

EFFECT: invention provides obtaining novel imidazopyrrolopyrazine derivatives, useful in the treatment of conditions, mediated by the activity of Jak1, Jak3 and Syk proteinkinases.

23 cl, 54 tbl, 690 ex