Generated: May 24, 2017
|Title:||Polymorphs of the prodrug 6-N-(L-ALA-L-ALA)-trovafloxacin|
|Abstract:||The invention relates to a monohydrate polymorph PII.M of a compound of the formula ##STR1## exhibiting the following X-ray powder diffraction pattern The invention also relates to methods of preparing the above compound, pharmaceutical compositions containing the above compound, and methods of treating bacterial infections by administering the above compound.|
|Inventor(s):||Norris; Timothy (Gales Ferry, CT), McGarry; James J. (Ledyard, CT), Allen; Douglas J. M. (New London, CT)|
|Assignee:||Pfizer Inc. (New York, NY)|
1. A monohydrate polymorph PII.M of a compound of the formula ##STR6## exhibiting the following X-ray powder diffraction pattern
2. A process for preparing prodrug polymorph monohydrate PII.M, of trovafloxacin, for the formula of claim 1, which comprises
(a) preparing polymorph PII exhibiting the X-ray powder diffraction pattern
by treating the prodrug polymorph PI exhibiting the X-ray powder diffraction pattern.
3. The process of claim 2 step b) wherein said organic solvent is selected from the group consisting of (C.sub.1 -C.sub.6)alkyl esters of (C.sub.1 -C.sub.6)alkanoic acids and (C.sub.1 -C.sub.6)alkanols.
4. The process of claim 3 wherein said solvent is ethyl acetate.
5. A process for preparing prodrug polymorph monohydrate PII.M of claim 1 exhibiting the X-ray diffraction pattern described as follows:
which comprises treating the prodrug polymorph PI exhibiting the X-ray diffraction pattern described as follows:
with an organic solvent containing water.
6. The process of claim 5 wherein said organic solvent is a C.sub.1 -C.sub.6 alkyl ester of a C.sub.1 -C.sub.6 alkanoic acid or a C.sub.1 -C.sub.6 alkanol.
7. The process of claim 6 wherein said solvent is ethyl acetate.
8. A method for treating bacterial infection in a mammal in need thereof which comprises administering to said mammal a bacterial infection treating effective amount of the prodrug of claim 1.
9. A pharmaceutical composition for treating bacterial infection in a mammal comprising a bacterial infection treating effective amount of the prodrug of claim 1 and a pharmaceutically acceptable carrier.
10. The compound of claim 1 having a water content of about 2.7%.
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