Bausch-Lomb Incorporated

Harry M King, Jr

Eric Phillips

Mohannad Shawer

Disclosed herein is a molecular crystal form of (R)-(+)-7-(3-amino-2,3,4,5,6,7-hexahydro-1H-azepin-1-yl)-1-cyclopropyl-8-chloro-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid. The molecular crystal is characterized by at least one of: (a) an X-ray powder diffraction ('XRPD') spectrum that comprises peaks at 2&#x3b8; angles of 10.6, 15, 19.7, 21.1, and 22&#xb0;&#xb1;0.2&#xb0;; (b) a DSC melting peak at 288&#xb0; C.; (c) aC NMR spectrum having peaks at 23.3, 27.7, 41.1, 54.5, 116.6, and 153.5 ppm; and (d) pKa values of 5.65 and 9.91. The compound belongs to the class of fluoroquinolones and is useful as an antibacterial agent.

Fluoroquinolone carboxylic acid molecular crystals

Amorphous solid-state form of (R)-(+)-7-(3-amino-2,3,4,5,6,7-hexahydro-1H-azepin-1-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid is characterized by at least one of: (a) an X-ray powder diffraction ('XRPD') spectrum that comprises peaks at 2&#x3b8; angles of 6.9-7.1, 9.4, 10.6-10.7, and 13.4-13.7&#xb0;&#xb1;0.2&#xb0;, and a diffuse halo pattern at 11-30&#xb0;; and (b) a DSC (differential scanning calorimetry) melting peak at about 267-272&#xb0; C. The amorphous solid is prepared by rapid precipitation from a saturated or supersaturated solution of besifloxacin free base in a solvent comprising at least benzyl alcohol.

Amorphous besifloxacin solid

Disclosed herein is a molecular crystal form of the compound (R)-(+)-7-(3-amino-2,3,4,5,6,7-hexahydro-1H-azepin-1-yl)-1-cyclopropyl-8-chloro-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid. The molecular crystal is characterized by at least one of: (a) an X-ray powder diffraction ('XRPD') spectrum that comprises peaks at 2&#x3b8; angles of 10.6, 15, 19.7, 21.1, and 22&#xb0;&#xb1;0.2&#xb0;; (b) a DSC melting peak at 288&#xb0; C.; (c) aC NMR spectrum having peaks at 23.3, 27.7, 41.1, 54.5, 116.6, and 153.5 ppm; and (d) pKa values of 5.65 and 9.91. The compound belongs to the class of fluoroquinolones and is useful as an antibacterial agent.

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Webster, NY, United States of America

Harry M King, Jr