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Claims for Patent: 9,085,601

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Claims for Patent: 9,085,601

Title:Process for preparing an A2A-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; Elfatih (Fremont, CA), Seemayer; Robert (Belmont, CA), Lemons; Travis (Los Gatos, CA)
Assignee: Gilead Sciences, Inc. (Foster City, CA)
Application Number:13/970,372
Patent Claims: 1. A pharmaceutical composition prepared from a crystalline monohydrate form of the compound (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide by adding at least one pharmaceutically acceptable carrier.

2. The pharmaceutical composition of claim 1, wherein the monohydrate is substantially free of 2-hydrazinoadenosine.

3. The pharmaceutical composition of claim 2, wherein the monohydrate is substantially free of other hydrates or amorphous form.

4. The pharmaceutical composition of claim 3, wherein the monohydrate has a purity of at least about 99.6%.

5. The pharmaceutical composition of claim 4, wherein the monohydrate exhibits an X-ray powder diffraction pattern having peaks at diffraction angle 2.theta. (.degree.) of about 6, about 9, about 11, about 13, about 14.5, about 16.5, and about 18 as measured by Cu-K.alpha.1 X-ray powder diffractometry.
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