KHAUBERT Dzhejms Dzheffri (US),ХАУБЕРТ Джеймс Джеффри (US),DITSH Gregori (US),ДИТШ Грегори (US),KHERSHBERG Robert (US),ХЕРШБЕРГ Роберт (US),BERDZHESS Lorens E. (US),БЭРДЖЕСС Лоренс Э. (US),LISSIKATOS,KHAUBERT Dzhejms Dzheffri,ХАУБЕРТ Джеймс Джеффри,DITSH Gregori,ДИТШ Грегори,KHERSHBERG Robert,ХЕРШБЕРГ Роберт,BERDZHESS Lorens E.,БЭРДЖЕСС Лоренс Э.,LISSIKATOS Dzhozef P.,ЛИССИКАТОС Джозеф П.,NYUKHAUS
申请号：
RU2012110251/04
公开号：
RU0002593261C2
申请日:
2010.08.18
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I or tautomer, enantiomer or pharmaceutically acceptable salt thereof, where said formula Y represents -(O)x(CH2)yR11； x is selected from 0 and 1； y is selected from 0, 1, 2, and 3； R11 is selected from phenyl, pyridyl, morpholinyl, 1-oxo-1,3-dihydroisobenzofuranyl and 2-oxo-tetrahydrofuranyl, when x equals 0, said phenyl or pyridinyl substituted -C(O)NR1R2 or T； R1 and R2 is selected independently from hydrogen and C1-6alkyl, wherein said alkyl is optionally substituted -C(O)O(CH2)tR12, or R1 and R2 together with a nitrogen atom to which they are bonded, form a saturated 5-member heterocycle containing 1-4 heteroatoms selected from nitrogen, oxygen and sulphur； t is selected from 0, 1, 2, and 3； R12 is selected from C3-6cycloalkyl and phenyl； T is selected from 2-oxo-1,3-dioxolane, 2-oxotetrahydrofuran -(CHR7)zOR9, -(O)u(CH2)sC(O)R8, -OSO2R13 and -CH(OH)CH2OH； R7 represents H； R8 is -OR10； R9 represents H； R10 is selected from C1-6alkyl, -(CH(2)R12 and hydrogen, wherein said alkyl is optionally substituted with halogen or diC1-6alkylamine； R13 represents CF3； u is selected from 0 and 1； z is selected from 1, 2, and 3； s is selected from 1 and 2； R5 is selected from -NR3R4 and -OR10； R3 and R4 independently selected from H, C1-12alkyl, -(O)q(CH2)rP； said alkyl is optionally substituted with -OH； q is selected from 0 and 1； r is selected from 0, 1, 2, and 3； P is selected from phenyl, -SO2R6, piperidinyl and pirrolidinyl； and R6 is -NH2, provided that when R11 is a phenyl or pyridyl, then a) x+y ≥ 1； or b) R11 is substituted with T； or c) R5 is NR3R4, and at least one of R3 or R4 is -(O)q(CH2)rP-, and q+r ≥ 1； or d) at least one of R1 or R2 represents alkyl, substituted with -C(O)O(CH2)R12. Invention also relates to a pharmaceutical composition exhibiting TLR7- and/or TLR8 agonist activity, comprising an effective amount of a compound of formula I together with a pharmaceutically acceptable diluen
