Claims
- 1. A monohydrate polymorph PII.M of a compound of the formula ##STR6## exhibiting the following X-ray powder diffraction pattern
- ______________________________________Peak No. 1 2 3 4 5 6 7 8______________________________________2.sub.-- .theta..sub.-- (.degree.) Cu 3.6 7.3 13.7 14.5 17.1 21.) 23.6 26.7d space 24.2 12.2 6.5 6.1 5.2 4.2 3.8 3.3______________________________________
- 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
- ______________________________________Peakno. 1 2 3 4 5 6 7 8 9______________________________________2.sub.-- .theta..sub.-- 3.4 6.8 13.5 16.8 19.6 20.3 23.1 25.7 27.8(.degree.) Cud space 26.0 13.1 6.6 5.3 4.5 4.4 3.8 3.5 3.2.______________________________________
- 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:
- ______________________________________Peak no. 1 2 3 4 5 6 7 8______________________________________2.sub.-- .theta..sub.-- (.degree.) Cu 3.6 7.3 13.7 14.5 17.1 21.0 23.6 26.7d space 24.2 12.2 6.5 6.1 5.2 4.2 3.8 3.3______________________________________
- which comprises treating the prodrug polymorph PI exhibiting the X-ray diffraction pattern described as follows:
- ______________________________________PeakNo. 1 2 3 4 5 6 7 8______________________________________2.sub.-- .theta..sub.-- (.degree.) 6.1 7.3 7.9 9.5 11.7 14.2 14.9 15.8Cud space 14.5 12.1 11.2 9.3 7.6 6.2 6.0 5.6______________________________________PeakNo. 9 10 11 12 13 14______________________________________2.sub.-- .theta..sub.-- (.degree.) 16.8 20.1 21.4 22.7 24.9 26.0Cud space 5.3 4.4 4.2 3.9 3.6 3.4______________________________________
- 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%.
Parent Case Info
This application claims benefit of provisional application Ser. No. 60/005,109 filed Aug. 29, 1995.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
102e Date |
371c Date |
PCT/IB96/00653 |
7/5/1996 |
|
|
1/30/1998 |
1/30/1998 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO97/08191 |
3/6/1997 |
|
|
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
5164402 |
Brighty |
Nov 1992 |
|
5229396 |
Brighty |
Jul 1993 |
|