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：
RU2009118617/04
公开号：
RU0002474582C2
申请日:
2007.10.18
申请国别(地区):
RU
年份:
2013
代理人:
摘要：
FIELD: medicine.SUBSTANCE: invention refers to new heteroaryl compounds of general formula (I) and their pharmaceutically acceptable salts possessing the properties of protein kinase inhibitor, such as mTOR, IKK-2, Tyk2, Syk-kinase. In formula (I) R1 represents substituted or unsubstituted C1-8alkyl, substituted or unsubstituted aryl, specified in phenyl, substituted or unsubstituted 5-6-member heteroaryl with 1-3 nitrogen atoms in a cycle specified in pyridine, pyrazole, indole, indazole, triazole, benzimidazole, 2-(1H-imidazo-[4,5-b]pyridine, substituted or unsubstituted 5-7- member cycloalkyl or substituted or unsubstituted heterocycloalkyl specified in pyrrolidinyl； -X-A-B-Y- taken together form -N(R2)CH2C(O)NH-, -N(R2)C(O)CH2NH-, -N(R2)C(O)NH-, -N(R2)C=N- or -C(R2)=CHNH-； L represents a direct bond, NH or O； R2 represents substituted or unsubstituted C1-8alkyl, substituted or unsubstituted aryl specified in phenyl, tetrahydronaphthalene, unsubstituted 5-7- member mono- or 8- member bicycloalkyl； and R3 and R4 independently represent H or C1-8alkyl. The substitutes in the substituted groups are specified in one or more halogen, C1-8alkyl, hydroxyl, amino, nitro, thiol, C1-4alkyl thioether, cyano, carboxyl, C1-4alkyl ester, halogen alkyl, C6cycloalkyl or heteroaryl specified in pyridyl, triazole, O-lower alkyl, aryl specified in phenyl, phenyl-lower alkyl, CO2CH3, CONH2, OCHF2, CF3 or OCF3 groups wherein CONH2 group may be substituted by cyclohexyl.EFFECT: compounds can find application for treating or preventing cancer, inflammatory pathological conditions, metabolic pathological conditions.24 cl, 8 dwg, 2 tbl, 169 exИзобретение относится к новым гетероарильным соединениям общей формулы (I) и его фармацевтически приемлемым солям, обладающим свойствами ингибитора протеинкиназы, такой как mTOR, IKK-2, Tyk2, Syk-киназ. Соединения могут найти применение для лечения или предупреждения рака, воспалительных патологических состояний, иммунологических патологических с
