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    • 39. 发明授权
    • Partial and full agonists of A1 adenosine receptors
    • A1腺苷受体的部分和全部激动剂
    • US07022681B2
    • 2006-04-04
    • US10641930
    • 2003-08-15
    • Jeff ZablockiVenkata PalleElfatih ElzeinXiaofen Li
    • Jeff ZablockiVenkata PalleElfatih ElzeinXiaofen Li
    • A61K31/70C07H19/167
    • C07H19/16
    • Disclosed are A1 adenosine receptor agonists of the formula: wherein: R1 is optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl; R2 is hydrogen, halo, trifluoromethyl, or cyano; R3 is hydrogen, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl, R4 and R5 are independently hydrogen or optionally substituted acyl; X is a covalent bond or lower alkylene optionally substituted by cycloalkyl; X1 is a covalent bond or alkylene; Y is a covalent bond or lower alkylene optionally substituted by hedroxy or cycloalkyl; and Z is —C≡C—, —R6C═CR7—, or —CHR6CHR7—, in which R6 and R7 at each occurrence are hydrogen or lower alkyl.
    • 公开了下式的A 1 N 2腺苷受体激动剂:其中:R 1是任选取代的环烷基,任选取代的杂环基,任选取代的芳基或任选取代的杂芳基; R 2是氢,卤素,三氟甲基或氰基; R 3是氢,任选取代的环烷基,任选取代的芳基,任选取代的杂芳基或任选取代的杂环基,R 4和R 5独立地是 氢或任选取代的酰基; X是共价键或任选被环烷基取代的低级亚烷基; X 1是共价键或亚烷基; Y是共价键或任选被羟基或环烷基取代的低级亚烷基; 并且Z是-C≡C-,-R 6 C-CR 7或-CHR 6 CHR 7, 其中每次出现的R 6和R 7都是氢或低级烷基。