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Claims for Patent: 7,531,623

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Claims for Patent: 7,531,623

Title:Hydrochloride salts of a glycopeptide phosphonate derivative
Abstract:Disclosed are hydrochloride salts of telavancin having a chloride ion content of from about 2.4 wt. % to about 4.8 wt. %. The disclosed salts have improved stability during storage at ambient temperatures compared to other hydrochloride salts. Also disclosed are processes for preparing such salts.
Inventor(s): Liu; Jyanwei (Sunnyvale, CA), Lee; Junning (El Granada, CA)
Assignee: Theravance, Inc. (South San Francisco, CA)
Application Number:10/970,128
Patent Claims: 1. A hydrochloride salt of telavancin having a chloride ion content of from about 3.7 wt. % to about 4.4 wt. %.

2. The hydrochloride salt of claim 1, wherein the chloride ion content is from about 3.9 wt. % to about 4.4 wt. %.

3. The hydrochloride salt of claim 1, wherein the chloride ion content is from about 3.7 wt. % to about 3.9 wt. %.

4. A process for preparing a hydrochloride salt of telavancin having a chloride ion content of from about 3.7 wt. % to about 4.4 wt. % the process comprising the steps of: (a) providing a composition comprising a hydrochloride salt of telavancin having a chloride ion content greater than about 4.8 wt. % and an aqueous solvent system, wherein the composition has a pH of less than or equal to about 2.0; (b) adjusting the pH of the composition to from about 3.5 to about 4.5 to form a hydrochloride salt of telavancin having a chloride ion content of from about 3.7 wt. % to about 4.4 wt. %; and (c) isolating the hydrochloride salt of telavancin produced in step (b).

5. The process of claim 4, wherein in step (b) the pH of the composition is adjusted to a range of from about 3.5 to about 4.0.

6. The process of claim 4, wherein in step (b) the pH of the composition is adjusted to a range of from about 4.0 to about 4.5.

7. The process of claim 4, wherein the aqueous solvent system of step (a) comprises acetonitrile and water.

8. The process of claim 4, wherein in step (b), the pH is adjusted using an alkali hydroxide.

9. The process of claim 4, wherein in step (c), the hydrochloride salt of telavancin is isolated by precipitation and filtration.

10. An isolated hydrochloride salt of telavancin having a chloride ion content of from about 3.7 wt. % to about 4.4 wt. %.

11. The hydrochloride salt of claim 10, wherein the chloride ion content is from about 3.9 wt. % to about 4.4 wt. %.

12. The hydrochloride salt of claim 10, wherein the chloride ion content is from about 3.7 wt. Va to about 3.9 wt. %.

13. A hydrochloride salt of telavacin having about 2 molar equivalents of hydrochloride per molar equivalent of telavancin.
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