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SUBSTITUTED COMPOUNDS OF PYRAZOLE[1,5-a]PYRIMIDINE AS TRK KINASE INHIBITORS
专利权人:
ERREJ BIOFARMA INK.
发明人:
ALLEN SHelli (US),АЛЛЕН Шелли (US),ENDRJUS Stiven S. (US),ЭНДРЮС Стивен С. (US),KONDROSKI Kevin Ronald (US),КОНДРОСКИ Кевин Рональд (US),KHAAS JUlija (US),ХААС Юлия (US),KHUAN Lili (US),ХУАН Лили (US),ЦЗЯН Юйтун (US),КЕРХЕР Тимоти (US),СЕО Дзеонгбеоб (US)
申请号:
RU2012104493/04
公开号:
RU0002584157C2
申请日:
2010.07.09
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
FIELD: biotechnology.SUBSTANCE: invention relates to a compound having the general formula,or its pharmaceutically acceptable salt, where R1 is H or (1-6C alkyl); R2 is H, (1-6C)alkyl, -(1-6C) fluoroalkyl, -(1-6C)difluoroalkyl, -(1-6C)trifluoroalkyl, -(1-6C)chloralkyl, -(2-6C)chlorfluoroalkyl, -(2-6C)chlorhydroxyalkyl, -(1-6C)hydroxyalkyl, -(2-6C)dihydroxyalkyl, -(1-6C alkyl)CN, -(1-6C alkyl) SO2NH2, -(1-6C alkyl)NHSO2(1-3C alkyl), -(1-6C alkyl)NH2, -(1-6C alkyl)NHC(= O)O(1-4C alkyl), -(1-6C alkyl) getSus1, -(1- 6C alkyl)getAr1, getAr2, getSus2, -O(1-6C alkyl), which is optionally substituted by halogen, OH or (1-4C)alkoxy, Sus1, -(1-6C alkyl)(3-6C cycloalkyl), -(1-6C alkyl)(1-4C alkoxy), -(1-6C hydroxyalkyl)(1-4C alkoxy) with bridged 7-membered cycloalkyl ring optionally substituted with (1-6C)hydroxyalkyl, or bridged 7-8-membered heterocyclic ring having 1-2 ring nitrogen atoms; or NR1R2 forms a 4-6-membered azacyclic ring optionally substituted with one or more substituents independently selected from (1-6C)alkyl, OH, CO2H, (1-3C alkyl)CO2H, -O(1-6C alkyl) and (1-6C)hydroxyalkyl; Y is (i) phenyl optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkoxy, -CF3 -O(1-4C alkyl)getSus3, -(1-4C alkyl)getSus3, -O(1-4C alkyl)O(1-3C alkyl) and -O(3-6C dihydroxyalkyl), or (ii) pyridyl, where the said pyridyl is optionally substituted with one or more substituents independently selected from halogen, -O(1-4C alkyl), (1-4C) alkyl and NH2, or (iii) pyrid-2-on-3-yl ring optionally substituted by one or more substituents independently selected from halogen and (1-4C)alkyl; X is -CH2-; R3 is H; each of R4 is independently selected from halogen, -(1-4C)alkyl, -OH and -CH2OH; and n is equal to 0, 1 or 2. The invention also relates to variants of methods of preparing compounds of formula I. The invention relates to specific compounds of the formula I. The compounds are intended for use in treating pain, cancer, inflammation, neurodegenera
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