VISHART Nil (US),ВИШАРТ Нил (US),ARDZHIRIADI Mariya A. (US),АРДЖИРИАДИ Мария А. (US),KOLDERVUD Devid Dzh. (US),КОЛДЕРВУД Дэвид Дж. (US),ERIKSSON Anna M. (US),ЭРИКССОН Анна М. (US),FYAMENGO Brajan A. (
申请号:
RU2012127306
公开号:
RU0002570416C9
申请日:
2010.12.01
申请国别(地区):
RU
年份:
2019
代理人:
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 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 monoheterocycl