ENDRYUS Stiven Vejd (US),ЭНДРЮС Стивен Вейд (US),KONDROSKI Kevin Ronald (US),КОНДРОСКИ Кевин Рональд (US),KHAAS YUliya (US),ХААС Юлия (US),TSZYAN YUjtun (US),ЦЗЯН Юйтун (US),KOLAKOVSKI Gabriel R. (US),КОЛАКОВСКИ Габриель Р. (US),СЕО Дзеонгбеоб (US),ЯН Хун-Воон (US),ЧЖАО Цянь (US)
申请号：
RU2012155278/04
公开号：
RU0002594742C2
申请日:
2011.05.13
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention relates to compound of formula I or its pharmaceutically acceptable salts, which are inhibitors of Trk kinases and are useful for treating pain, malignant oncological disease, inflammation, neurodegenerative diseases and Trypanasoma Crusi infections. Invention also describes versions of methods of producing compound of formula I. In Formula I (I) ring A is selected from A-1, A-2, A-3, having structure , where wavy line marked 1 indicates connection point of ring A to ring B, and wavy line marked 2 indicates point of connection ring A to W； X is N or CH； Y is H or F； R1 is H or halogen； ring B is selected from rings B-1 and B-2, having structure , where wavy line marked 3 indicates point of connection to ring A, and wavy line marked 4 indicates point of connection to pyrazolo[1,5-a]pyrimidine ring of formula I； W is O, NH or CH2, wherein, when ring A is A-2, then W is CH2； m is 0, 1 or 2； D is carbon, R2 and R2a independently represent H, F, (1-3C)alkyl or OH (provided that R2 and R2a are not simultaneously OH), and R3 and R3a are independently H or (1-3C)alkyl, or (D) is carbon or nitrogen, R2 and R3 are absent, and R2a and R3a together with atoms to which they are bonded, form 5-6-member heteroaryl ring containing 1-2 heteroatoms ring； Z is *-NR4aC(=O)-, *-ONHC(=O)-, *-NR4bCH2- or *-OC(=O)-, where asterix indicates connection point of Z to containing carbon R3； R4a is H or (1-6C)alkyl； R4b is H, (1-6C)alkyl, ((1-6C)alkyl)C(O)-, HOCH2C(O)-, ((1-6 C)alkyl) sulfonyl, HO2CCH2- or ((1-6C)alkyl)NH(CO)-； and R-5 and R6 independently represent H, halogen, OH or (1-6C)alkyl.EFFECT: useful for treating pain, malignant oncological disease, inflammation, neurodegenerative diseases and Trypanasoma Crusi infections.73 cl, 1 tbl, 45 exИзобретение относится к соединению Формулы I или его фармацевтически приемлемым солям, которые являются ингибиторами киназ Trk и полезны для лечения боли, злокачественного онкологического заболевания, воспале
