Crystalline alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid and methods for preparing thereof
AssigneeTheravance, Inc.
InventorPaul R. Fatheree
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Abstract
The invention provides a micronized 4′-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid having improved stability. The invention also provides pharmaceutical compositions comprising the stable micronized compound, processes for preparing the stable micronized compound, and methods of using the stable micronized compound to treat diseases such as hypertension.
Claims17
Stable micronized 4′-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid, where the amount of 4′-{2-ethoxy-4-ethyl-5-[(2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid ethyl ester within the stable micronized acid imidazole does not increase by more than about 0.1% AUC by HPLC relative to the initial amount of acid imidazole, when the stable micronized acid imidazole is maintained at a temperature of about 40° C. for at least 2 weeks.
Dependencies are inferred from the claim text.