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Last Updated: December 23, 2024

Claims for Patent: 8,106,183

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Summary for Patent: 8,106,183

Title:	Process for preparing an A.sub.2A-adenosine receptor agonist and its polymorphs
Abstract:	Disclosed is a synthesis suitable for large scale manufacture of an A.sub.2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
Inventor(s):	Zablocki; Jeff (Mountain View, CA), Elzein; Elfaith (Fremont, CA)
Assignee:	Gilead Sciences, Inc. (Foster City, CA)
Application Number:	12/765,623
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,106,183
Patent Claims:	1. A monohydrate of (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, which monohydrate is in a crystalline form. 2. The monohydrate of claim 1, wherein the crystalline form has a X-ray diffraction pattern as shown in FIG. 3. 3. The monohydrate of claim 1, wherein the crystalline form has a thermogravimetric analysis pattern and a differential scanning calorimetry pattern as shown in FIG. 2. 4. The monohydrate of claim 1, wherein the crystalline form is obtainable by a method comprising crystallizing (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide in an aqueous protic solvent or an aqueous polar solvent. 5. The monohydrate of claim 1, wherein the crystalline form is obtainable by a method comprising crystallizing (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide in a solvent selected from a mixture of ethanol and water and a mixture of dimethylsulfoxide and water. 6. A method for preparing the monohydrate of claim 1, comprising crystallizing (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-methylcarboxamide in an aqueous protic solvent or an aqueous polar solvent. 7. The method of claim 6, wherein the aqueous protic solvent or the aqueous polar solvent is selected from a mixture of ethanol and water and a mixture of dimethylsulfoxide and water. 8. The monohydrate of claim 1, wherein the crystalline form has a .sup.1H NMR spectrum as shown in FIG. 1. 9. The monohydrate of claim 1, wherein the crystalline form is free of any impurity represented by the following structure: ##STR00024##

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