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Details for Patent: 8,524,883

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Details for Patent: 8,524,883

Title:Monohydrate of (1-{9-[4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopu- rin-2-yl}pyrazol-4-yl)-N-methylcarboxamide
Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A.sub.2A-adenosine receptor agonist, namely, (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide. Also, disclosed are polymorphs of this compound and methods for isolating a specific polymorph. Also, disclosed are pharmaceutical compositions and methods for preparing pharmaceutical compositions.
Inventor(s): Zablocki; Jeff (Foster City, CA), Elzein; Elfatih (Foster City, CA), Seemayer; Robert (Foster City, CA), Lemons; Travis (Foster City, CA)
Assignee: Gilead Sciences, Inc. (Foster City, CA)
Filing Date:Dec 21, 2011
Application Number:13/333,872
Claims:1. A method of preparing a pharmaceutical composition comprising combining a monohydrate 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 with at least one pharmaceutically acceptable carrier.

2. The method of claim 1, wherein the pharmaceutically acceptable carrier comprises a buffered aqueous solution.

3. The method of claim 2, wherein the monohydrate is a crystalline monohydrate that is substantially free of 2-hydrazinoadenosine.

4. The method of claim 3, wherein the monohydrate is substantially free of other forms of the compound.

5. The method of claim 4, wherein the monohydrate has a purity of at least about 99.6%.
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