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    Partial and full agonists of A1 adenosine receptors
    62.
    发明授权
    Partial and full agonists of A1 adenosine receptors 失效
    A1腺苷受体的部分和全部激动剂

    公开(公告)号：US07022681B2

    公开(公告)日：2006-04-04

    申请号：US10641930

    申请日：2003-08-15

    申请人： Jeff Zablocki ,  Venkata Palle ,  Elfatih Elzein ,  Xiaofen Li

    发明人： Jeff Zablocki ,  Venkata Palle ,  Elfatih Elzein ,  Xiaofen Li

    IPC分类号： A61K31/70 ,  C07H19/167

    CPC分类号： C07H19/16

    摘要： 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.

    摘要翻译： 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。