Purine derivatives as a3 and a1 adenosine receptor agonists

Details Purine derivatives as a3 and a1 adenosine receptor agonists Purine derivatives as a3 and a1 adenosine receptor agonists

C - Chemistry, Metallurgy

07

D

C07D 473/00 (2006.01) A61K 31/52 (2006.01) A61P 9/00 (2006.01)

Patent

CA 2601996

Disclosed are (N)-methanocarba adenine nucleosides of the formula: [Formula] as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.

L'invention concerne des nucléosides (N)-méthanocarba adénine de la formule, en tant qu'agonistes du récepteur d'adénosine A3 particulièrement puissant, des compositions pharmaceutiques comprenant ces nucléosides, et un procédé d'utilisation de ces nucléosides. R1-R6 sont définis dans le descriptif. Ces nucléosides sont destinés à servir dans le traitement d'un certain nombre de maladies, telles que inflammation, ischémie cardiaque, accident cérébrovasculaire, asthme, diabètes, et arythmie cardiaque. L'invention concerne également des composés qui sont des agonistes des deux récepteurs d'adénosine A1 et A3 à utiliser en cardioprotection.

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