Abstract: The invention provides new methods for synthesis of 2-aralkyloxyadenosines and 2-alkoxyadenosines. The invention is particularly useful for synthesis of 2-[2-(4-chlorophenyl)ethoxy]adenosine. Preferred methods of the invention include activating a guanosine compound followed by hydrolysis; alkylating the hydrolyzed compound with subsequent animation to provide a 2-aralkyloxyadenosine or a 2-alkoxyadenosine compound.

Abstract: The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.

Abstract: New compounds having a tricyclic pyrazolotriazolopyrimidine ring structure are provided and methods of using those compounds for a variety of therapeutic indications.

Abstract: The compounds of formula I wherein R, R1, R2 R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor agonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor.

Abstract: The present invention discloses a method for measuring myocardial function in a mammal in need of such measurement by: a) administering 2-substituted adenosine carboxamide derivatives at a dosage rate of less than 1 &mgr;g/kg/min, preferably between about 0.01 and 1 &mgr;g/kg/min; and then: b) performing a technique on the mammal to detect myocardial function. The method can be used to diagnose myocardial dysfunction by electrophysiologic analysis or by imaging the vasculature of the heart, especially under conditions that simulate stress.

Abstract: The compounds of the formula described herein wherein R, R1, R2 and R3 have the meanings given in the specification, are endowed with A3 adenosine receptor agonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.

Abstract: A method of and a formulation for treating hyper-excited sensory nerve functions are provided. The method comprises administering to a patient in need of treatment thereof a pharmaceutical composition comprising an effective amount of 2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)(4-chlorophenyl) methanone or a pharmaceutically acceptable salt thereof. The disorder treated include hyperesthesia, dysesthesia, allodynia, hyperalgesia, tinnitus, ganglionic dysfunction and combinations thereof. The co-administration of adenosine is not needed. The pharmaceutical preparation is suitable for oral administration. The pharmaceutical preparation is useful in the reduction of neuropathic pain in a conscious human. The use of the pharmaceutical preparation does not result in medically adverse cardiovascular symptoms associated with administration of adenosine.