King Pharmaceuticals Research and Development, Inc.

Other

King Pharmaceuticals Reseach and Development, Inc.

Edward Leung

Pier Giovanni Baraldi

Pier Andrea Borea

Allan R Moorman

Michael Scannell

Thiagarajan Balasubramanian

Russell Outcalt

Shih-Fong Chen

Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.

Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs

The present invention relates to Compound T62, pharmaceutically acceptable salts thereof, and their use in medicine as allosteric adenosine A receptor enhancers and uses including treatment of pain, for example, persistent chemical pain, neuropathic pain and acute pain states such as that induced by chemical irritation, gastrointestinal disturbance, migraine and all forms of headache. Compound T62 is represented by the formula:

Method for treating pain in humans

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.

Diagnostic uses of 2-substituted adenosine carboxamides

Tumor growth and metastasis can be inhibited by administration of adenosine A,and/or A,antagonists, preferably A,antagonists, to a patient. The antagonists can be, and preferably are, administered in combination with other anti-tumor agents, such as anti-angiogenic agents (including adenosine A,antagonists) and/or cytotoxic agents. Because the cytotoxic agents attack the tumor cells themselves, and the anti-angiogenic agents prevent the growth of vasculature which would otherwise support the growth of the tumor cells.

Use of adenosine A3 receptor antagonists to inhibit tumor growth

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&lsqb;b&rsqb;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.

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Cary, NC, United States of America

Edward Leung