Details for Patent: 8,524,883
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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%. |