Partial and full agonists of A1 adenosine receptors

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.