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(Ra)C(O)-Re-; 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, -Re, -Re-C(O)-Re-, -Re-O-Re-, -Re-N(Ra)-Re-, -Re-N(Ra)C(O)-Re-, -ReC(O)N(Ra)Re-, -Re-N(Ra)S(O)2-Re- or -Re-N(Ra)S(O)2N(Ra)-Re-; where in all cases E is bound either with a carbon atom or with a nitrogen atom in D; G represents hydrogen, -N(Ra)(Rb), -(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(Ra)(Rb), nitrogen, Ra and Rb can form a ring in such a way that -N(Ra)(Rb) represents C4monoheterocyclyl, where monoheterocyclyl contains 1-2 heteroatoms, independently selected from nitrogen or oxygen; R4 represents hydrogen or -(C1-C6)alkyl; Ra and Rb, each independently represent hydrogen, (C1-C6)alkyl, oxetane; and Re 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
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Authors
Dates
2015-12-10—Published
2010-12-01—Filed