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 

Abstract RU 2570416 C2

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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RU 2 570 416 C2

Authors

Vishart Nil

Ardzhiriadi Marija A.

Koldervud Dehvid Dzh.

Ehriksson Anna M.

F'Jamengo Brajan A.

Frehnk Kristin E.

Fridman Majkl

Dzhorzh Don M.

Godken Ehrik R.

Dzhozefson Natan S.

Li Bitsin' S.

Morytko Majkl Dzh.

Stjuart Kent D.

Voss Dzheffri V.

Uollejs Grir A.

Van Lu

Voller Kevin R.

Dates

2015-12-10Published

2010-12-01Filed