This disclosure relates to an improved process for the preparation of regadenoson pharmaceutically acceptable salts thereof and hydrates thereof and for the preparation of intermediates useful in the synthesis of regadenoson. The disclosure also relates to a new crystalline form of regadenoson. Processes for the preparation of the crystalline form compositions containing the crystalline form and methods of use thereof are also described.

This disclosure relates to an improved process for the preparation of regadenoson, pharmaceutically acceptable salts thereof, and hydrates thereof, and for the preparation of intermediates useful in the synthesis of regadenoson. The disclosure also relates to a new crystalline form of regadenoson. Processes for the preparation of the crystalline form, compositions containing the crystalline form, and methods of use thereof are also described.

This disclosure relates to an improved process for the preparation of regadenoson, pharmaceutically acceptable salts thereof, and hydrates thereof, and for the preparation of intermediates useful in the synthesis of regadenoson. The disclosure also relates to a new crystalline form of regadenoson. Processes for the preparation of the crystalline form, compositions containing the crystalline form, and methods of use thereof are also described.

Myocardial imaging methods that are accomplished by administering doses of a pharmaceutical composition including regadenoson—an adenosine A2A receptor agonist—to a human undergoing myocardial imaging in an amount sufficient to achieve at least a minimal increase in average coronary peak flow velocity.

Myocardial imaging methods are provided that are accomplished by administering doses of a pharmaceutical composition comprising one or more adenosine A2A receptor agonists in particular regadenoson useful for among other indications myocardial imaging and coronary vasodilation in an amount sufficient to achieve at least a minimal increase in average coronary peak flow velocity.

Myocardial imaging methods that are accomplished by administering doses of a pharmaceutical composition including regadenoson—an adenosine A2A receptor agonist—to a human undergoing myocardial imaging in an amount sufficient to achieve at least a minimal increase in average coronary peak flow velocity.

The present invention relates to methods for producing coronary vasodilation with little peripheral vasodilation by administering doses of a pharmaceutical composition including regadenoson named (1-{9-[(4S2R3R5R)-34-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide — an adenosine A2A receptor agonist — to a human in an amount sufficient to increase the average coronary peak flow velocity by at least about 16.5 cm/sec.

The present invention relates to methods for producing coronary vasodilation with little peripheral vasodilation by administering doses of a pharmaceutical composition including regadenoson named (1-{9-[(4S2R3R5R)-34-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide - an adenosine A2A receptor agonist - to a human in an amount sufficient to increase the average coronary peak flow velocity by at least about 16.5 cm/sec.(From US7655636 B2)