Abstract: The present invention relates to adenosine A3 receptor antagonists and their use for the prevention and treatment of atherosclerosis by administering to a mammal, in need thereof, a therapeutically effective amount of an adenosine A3 receptor antagonist, or a pharmaceutically acceptable salt thereof, alone or in combination with other anti-atherosclerotic agents.

Abstract: The present invention relates to pharmaceutical compositions and methods for promoting wound healing. The invention also relates to methods of making pharmaceutical compositions disclosed herein. Pharmaceutical compositions are disclosed comprising an effective amount of a 2-alkoxyadenosine or 2-aralkoxyadenosine, about 10% to about 70% w/w propylene glycol and a thickening agent.

Abstract: The present invention relates to adenosine A2B receptor antagonists and their use for the prevention and treatment of atherosclerosis by administering to a mammal, in need thereof, a therapeutically effective amount of an adenosine A2B receptor antagonist, or a pharmaceutically acceptable salt thereof, alone or in combination with other anti-atherosclerotic agents.

Abstract: The present invention discloses the use of high affinity adenosine A3 receptor antagonists for enhancing chemotherapeutic treatment of cancers expressing adenosine A3 receptors and cancers expressing P-glycoprotein or MRP. In preferred embodiments, adenosine A3 receptor antagonists are administered before or during administration of a taxane family, vinca alkaloid, camptothecin or antibiotic chemotherapeutic agent.

Abstract: 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.

Abstract: The present invention relates to pharmaceutical compositions and methods for promoting wound healing. The invention also relates to methods of making pharmaceutical compositions disclosed herein. Pharmaceutical compositions are disclosed comprising an effective amount of a 2-alkoxyadenosine or 2-aralkoxyadenosine, about 10% to about 70% w/w propylene glycol and a thickening agent.

Abstract: The invention relates to the diagnosis and prognosis of solid tumors and melanoma by detecting increased cellular levels of A3 receptors in tissue and/or leukocytes obtained from patients with cancer or patients at risk for developing cancer.

Abstract: The present invention relates to the use of adenosine receptor antagonists, preferably A3 receptor antagonists, either alone or in combination with other agents for the treatment, prevention and/or management of diseases or disorders associated with overexpression of HIF-1? and/or increased HIF-1? activity (e.g., cancer, respiratory disease). The methods and compositions of the invention are particularly useful for preventing, treating, or ameliorating symptoms associated with a cancer, disease or disorder associated with hypoxia-inducible factor 1? (HIF-1?) using the A3 receptor antagonists of the invention. The present invention provides methods to inhibit the growth of tumors, particularly solid tumors and more particularly hypoxic tumors.

Abstract: The present invention relates to the use of adenosine receptor agonists, preferably A3 receptor agonists, either alone or in combination with other agents for the treatment, prevention and/or management of diseases or disorders associated with under-expression of HIF-1? and/or decreased HIF-1 ? activity (e.g., ischemic related disorders). The methods of the invention are directed to methods of reducing tissue damage (e.g., substantially prevention tissue damage, inducing tissue protection) resulting from ischemia orhypoxia. The invention provides methods for treating, preventing and/or ameliorating one or more symptoms of hypoxic or HIF-1? related disorders by administering an A3 receptor agonist either alone or in combination with other agents.

Abstract: The present invention discloses the use of high affinity adenosine A3 receptor antagonists for enhancing chemotherapeutic treatment of cancers expressing adenosine A3 receptors and cancers expressing P-glycoprotein or MRP. In preferred embodiments, adenosine A3 receptor antagonists are administered before or during administration of a taxane family, vinca alkaloid, camptothecin or antibiotic chemotherapeutic agent.

Abstract: The present invention discloses the use of high affinity adenosine A3 receptor antagonists for enhancing chemotherapeutic treatment of cancers expressing adenosine A3 receptors and cancers expressing P-glycoprotein or MRP. In preferred embodiments, adenosine A3 receptor antagonists are administered before or during administration of a taxane family, vinca alkaloid, camptothecin or antibiotic chemotherapeutic agent.

Abstract: Methods for minimizing ischemic damage and/or reperfusion injury to heart tissue during cardiac surgery where the heart is removed from the body and then re-implanted into the same body, as well as cardiac transplantation, where the heart is removed from one body and transplanted into another body, are disclosed. Prior to removing the heart from the body, adenosine or adenosine A1 or A3 receptor agonists can be administered to the patient in a manner which provides cardioprotection to the heart. When the heart is removed from the body, it can be stored in a cardioplegic solution which contains adenosine, hypoxanthine and/or adenosine A1 or A3 receptor agonists. After the heart is reimplanted or transplanted, reperfusion injury can be minimized by administering adenosine or adenosine A2 receptor agonists to the patient in a manner which minimizes reperfusion injury. Preferably, all three steps are taken in order to minimize the amount of ischemic damage and reperfusion injury to the heart.

Abstract: The present invention relates to Compound T62, pharmaceutically acceptable salts thereof, and their use in medicine as allosteric adenosine A1 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.

Abstract: The present invention relates to Compound T62, pharmaceutically acceptable salts thereof, and their use in medicine as allosteric adenosine A1 receptor enhancers and uses including treatment of pain, for example, persistent chemical pain, meuropathic pain and acute pain states such as that induced by chemical irritation, gastrointestinal disturbance, migraine and all forms of headache.

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: Tumor growth and metastasis can be inhibited by administration of adenosine A1 and/or A3 antagonists, preferably A3 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 A2a 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.