VAN ZANDT Majkl (US),ВАН ЗАНДТ Майкл (US),GOLEBIOVSKI Adam (US),ГОЛЕБИОВСКИ Адам (US),TSZI Min Koo (US),ЦЗИ Минь Коо (US),UAJTKHAUZ Darren (US),УАЙТХАУЗ Даррен (US),RAJDER Todd (US),РАЙДЕР Тодд (US),B,VAN ZANDT MAJKL,ВАН ЗАНДТ Майкл,GOLEBIOVSKI ADAM,ГОЛЕБИОВСКИ Адам,TSZI MIN KOO,ЦЗИ Минь Коо,UAJTKHAUZ DARREN,УАЙТХАУЗ Даррен,RAJDER TODD,РАЙДЕР Тодд,BEKKET POL,БЕККЕТ Пол
申请号：
RU2012146819/04
公开号：
RU0002586219C2
申请日:
2011.04.20
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 (I), wherein R1 is selected from group consisting of-OH and ORa； Ra is selected from group consisting of hydrogen, linear or branched (C1-C6)alkyl, (C3-C14)aryl, (C3-C14)heterocycloalkyl-(C1-C6)alkylene-, containing 1-4 heteroatoms selected from O, S and N, (C3-C14)heteroaryl-(C1-C6)alkylene-, containing 1-4 heteroatoms selected from O, S and N, and (C3-C14)aryl(C1-C6)alkylene-； and where (A) R2 is selected from group consisting of (C3-C14)heterocycloalkyl-(C1-C6)alkylene-, containing 1-4 heteroatoms selected from O, S and N, and -(CH2)m-(X)u-(CH2)n-(Y)v-Rf where u is 1； v represents 0； each m and n independently equal to 0, 1, 2, 3, 4, 5 or 6, where m + n≥1, each X and Y is -NH-； Rf is (C3-C14)aryl； and R5 represents linear or branched (C1-C6)alkyl； or where (B) R2 is (C3-C14)heterocycloalkyl-(C1-C2)alkylene, containing 1-4 heteroatoms selected from O, S and N, and R5 is selected from group consisting of n and linear or branched (C1-C6)alkyl； and where each R3 and R4 is hydrogen； D is -CH2CH2CH2CH2-； and where any alkyl or alkylene optionally contains one or more substitutes selected from group consisting of halogen,-OH and (C1-C6)alkoxy； and where any aryl, heteroaryl or heterocycloalkyl, possibly containing one or more substitutes selected from a group consisting of halogen,-OH, oxo,-COOH, (C3-C14)aryl(C1-C6)alkylene-, (C3-C14)aryl, (C3-C14)heteroaryl containing 1-4 heteroatoms selected from O, S and N, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)halogen alkyl and (C1-C6)hydroxy alkyl； or its pharmaceutically acceptable salt, stereoisomer, tautomer or prodrug is revealed. Invention also discloses compound of formula II, pharmaceutical composition, method of inhibiting arginase I, arginase II or their combination in cell, method of treating or preventing disease or condition associated with expression or activity of arginase I, arginase II or their combination, and compound specified in table.EFFECT:
