Title compd. I [R1 = H, (un)substituted alkyl, aryl or cycloalkyl; R2, R3 and R4 independently = H, halo, OH, NO2, CN, (un)substituted alkyl, aryl, cycloalkyl or alkoxy; Q = (un)substituted piperidinyl, azepinyl, 5-membered spirocyclic ring, etc.], and their pharmaceutically acceptable salts, are prepd. and disclosed as allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. E.g., II was prepd. and demonstrated an IC50 value of about 100 nM in a functional assay measuring the cAMP level in CHO cells expressing the human A1-adenosine receptor. As allosteric modulators of the A1 adenosine receptor, I should be prove useful for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurol. disease or injury; sleep disorder; epilepsy; and depression.

Allosteric modulators of the A1 adenosine receptor

BARALDI, Pier Giovanni;ROMAGNOLI, Romeo
2008

Abstract

Title compd. I [R1 = H, (un)substituted alkyl, aryl or cycloalkyl; R2, R3 and R4 independently = H, halo, OH, NO2, CN, (un)substituted alkyl, aryl, cycloalkyl or alkoxy; Q = (un)substituted piperidinyl, azepinyl, 5-membered spirocyclic ring, etc.], and their pharmaceutically acceptable salts, are prepd. and disclosed as allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. E.g., II was prepd. and demonstrated an IC50 value of about 100 nM in a functional assay measuring the cAMP level in CHO cells expressing the human A1-adenosine receptor. As allosteric modulators of the A1 adenosine receptor, I should be prove useful for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurol. disease or injury; sleep disorder; epilepsy; and depression.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11392/530126
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