Last Updated: June 9, 2026

Claims for Patent: 5,763,454

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Summary for Patent: 5,763,454

Title:	Crystal form of anhydrous 7-( 1α,5α,6α!-6-amino-3-azabicyclo 3.1.0!hex-3-yl)-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8 naphthyridine-3-carboxylic acid, methanessulfonic acid salt
Abstract:	PCT No. PCT/US95/07211 Sec. 371 Date May 21, 1997 Sec. 102(e) Date May 21, 1997 PCT Filed Jun. 6, 1995 PCT Pub. No. WO96/39406 PCT Pub. Date Dec. 12, 1996The anhydrate of 7-([1 alpha ,5 alpha ,6 alpha ]-6-amino-3-azabicyclo[3.1.0]hex-3-yl)-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, methanesulfonic acid salt has advantageous stability for formulation as an antibacterial agent.
Inventor(s):	Lynne A. Handanyan, Thomas A. Morris, Robert L. Hendrickson, Phillip J. Johnson, Timothy Norris
Assignee:	Pfizer Inc
Application Number:	US08/849,300
Patent Claims:	1. 7-( 1.alpha.,5α,6α!-6-amino-3-azabicyclo 3.1.0!hex-3-yl)-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, methanesulfonic acid salt characterized by the following major peaks in its X-ray powder diffraction pattern ______________________________________ Peak no. 1 2 3 4 5 6 7 8 ______________________________________ 2θ(°) Cu 4.5 7.7 9.1 13.6 15.0 18.2 18.6 22.8 d space 19.5 11.5 9.7 6.5 5.9 4.9 4.8 3.9 ______________________________________ 2. A process for preparing the compound according to claim 1, which comprises heating 7-( 1α,5α,6α!-6-amino-3-azabicyclo 3.1.0!hex-3-yl)-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, methanesulfonic acid salt or its derived monohydrate in the presence of an alcohol or mixture thereof with an aprotic co-solvent. 3. A pharmaceutical composition having antibacterial activity, which comprises crystalline 7-( 1α,5α,6α!-6-amino-3-azabicyclo 3.1.0!hex-3-yl)-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, methanesulfonic acid salt characterized by the following major peaks in its X-ray powder diffraction pattern ______________________________________ Peak no. 1 2 3 4 5 6 7 8 ______________________________________ 2θ(°) Cu 4.5 7.7 9.1 13.6 15.0 18.2 18.6 22.8 d space 19.5 11.5 9.7 6.5 5.9 4.9 4.8 3.9 ______________________________________ 4. A method of treating a bacterial infection, which comprises administering to a subject in need of treatment an antibacterial amount of crystalline 7-( 1α,5α,6α!-6-amino-3-azabicyclo 3.1.0!hex-3-yl)-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, methanesulfonic acid salt characterized by the following major peaks in its X-ray powder diffraction pattern ______________________________________ Peak no. 1 2 3 4 5 6 7 8 ______________________________________ 2θ(°) Cu 4.5 7.7 9.1 13.6 15.0 18.2 18.6 22.8 d space 19.5 11.5 9.7 6.5 5.9 4.9 4.8 3.9 ______________________________________

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