Disclosed are A1 adenosine receptor agonists of the formula: ##STR1##

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 —CC—, —R6CCR7—, or —CHR6CHR7—, in which R6 and R7 at each occurrence are hydrogen or lower alkyl.
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