Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|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%.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.