| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to the field of organic chemistry, namely to a novel imidazopyrrolopyrazine derivative of formulaand to its pharmaceutically acceptable salt, stereoisomer or isomer, where R, Rand Rrepresent H; Rrepresents (C-C)cycloalkyl, substituted with one group, independently selected from CHNHor NH; or Rrepresents -A-D-E-G, where: A represents a bond or -N(R)C(O)-R-; D represents (C-C)alkylene, bound by a bridge bond (C)cycloalkylene, (C-C)cycloalkylene, substituted with one substituent, selected from (C-C)alkyl; (C-C)monoheterocyclylene, optionally substituted with one substituent, selected from (C-C)alkyl, where monoheterocyclylene contains 1-2 heteroatoms, independently selected from carbon or oxygen atoms; E represents a bond, -R, -R-C(O)-R-, -R-O-R-, -R-N(R)-R-, -R-N(R)C(O)-R-, -RC(O)N(R)R-, -R-N(R)S(O)-R- or -R-N(R)S(O)N(R)-R-; where in all cases E is bound either with a carbon atom or with a nitrogen atom in D; G represents hydrogen, -N(R)(R), -(C-C)alkyl, optionally substituted with 1-3 substituents, independently selected from a halogen, hydroxyl or cyano; (C-C)monocycloalkyl, optionally substituted with 1-2 substituents, independently selected from a halogen, cyano, monocyclic (C-C)heteroaryl, optionally substituted with one substituent, independently selected from cyano, where heteroaryl contains 2 heteroatoms, independently selected from nitrogen atoms; (C-C)monoheterocyclyl, optionally substituted with 1 or 2 substituents, independently selected from methyl, -CF, halogen or CHCN, where monoheterocyclyl contains 1-2 heteroatoms, independently selected from nitrogen or oxygen atoms; (C)aryl, optionally substituted with 1-2 substituents, independently selected from a halogen or cyano; where in the fragment, containing -N(R)(R), nitrogen, Rand Rcan form a ring in such a way that -N(R)(R) represents Cmonoheterocyclyl, where monoheterocyclyl contains 1-2 heteroatoms, independently selected from nitrogen or oxygen; Rrepresents hydrogen or -(C-C)alkyl; Rand R, each independently represent hydrogen, (C-C)alkyl, oxetane; and Rfor each case independently represents a bond or -(C-C)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 |
