SIGNAL FARMASJUTIKALZ;SIGNAL FARMAS'JUTIKALZ; EHLEHLSI
发明人:
MORTENSEN Debora S'ju (US),МОРТЕНСЕН Дебора Сью (US),MEDEROS Marija Mersedes Del'gado (US),МЕДЕРОС Мария Мерседес Дельгадо (US),SAPIENZA Dzhon Dzhozef (US),САПИЕНЗА Джон Джозеф (US),AL'BERS Ronald Dzh,MORTENSEN DEBORA SJU,МОРТЕНСЕН Дебора Сью,MEDEROS MARIJA MERSEDES DELGADO,МЕДЕРОС Мария Мерседес Дельгадо,SAPIENZA DZHON DZHOZEF,САПИЕНЗА Джон Джозеф,ALBERS RONALD DZH.,АЛЬБЕРС Роналд Дж.,LI BREHNDEN
申请号：
RU2009118623/04
公开号：
RU0002478635C2
申请日:
2007.10.18
申请国别(地区):
RU
年份:
2013
代理人:
摘要：
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to new imidazo[4,5-b]pyrazine derivatives of general formula or to its pharmaceutically acceptable salt wherein: R1 represents either aryl unsubstituted or substituted by one of the groups: halogen, hydoxyl, C1-6alkyl, C1-6alkoxyl, NH2, NHC1-6alkyl, N(C1-6alkyl)2, NHC1-6alkylC1-6alkoxy, C1-6alkylhydroxy, -C(O)NH2, -C(O)OC1-6alkyl, -C(O)NH C1-6alkyl, cyano, carboxy, heteroaryl and heterocycloalkyl； or heteroaryl unsubstituted or substituted by one of the groups: C1-6alkoxy, hydroxy, -C1-6alkyl, NH2 and NHC1-6alkyl； heterocycloalkyl unsubstituted or substituted by one group =O； and R2 represents H； unsubstituted C3-4alkyl； C1-4alkyl substituted by C5-6cycloalkyl unsubstituted or substituted by one group specified in amino, hydroxyl, C1-6alkoxy, or heterocycloalkyl unsubstituted or substituted by 1-2 groups specified in =O, C1-6alkyl； or C5-6cycloalkyl substituted by one group specified in hydroxyl, C1-6alkoxyl, C1-6alkylC1-6alkoxy, C1-6alkylhydroxy, CONH2； or substituted ir unsubstituted heterocycloalkyl； wherein aryl represents an aromatic structure consisting of 6-10 carbon atoms containing one ring or two condensed rings； wherein heteroaryl represents a 5-10-member aryl ring system containing 1-2 heteroatoms specified in nitrogen, oxygen and sulphur； wherein heterocycloalkyl represents a 5-9-member nonaromatic cycloalkyl wherein 1-2 heteroatoms specified in nitrogen and oxygen； provided the compound does not represent 1,3-dihydro-5-phenyl-2H-imidazo[4,5-b]pyrazin-2-one. Also, the invention refers to the specific imidazo[4,5-b]pyrazine derivatives, to a based pharmaceutical composition, to a method of treating or preventing cancer, inflammatory conditions, immunological diseases, metabolic conditions, and to a method of kinase inhibition in a cell expressing said kinase.EFFECT: there are produced new imidazo[4,5-b]pyrazine derivatives showing effective biological properties.17 cl, 2 tbl, 210 exИзо
