.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 8,481,526

« Back to Dashboard

Claims for Patent: 8,481,526

Title:Fluoroquinolone carboxylic acid molecular crystals
Abstract: 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.theta. angles of 10.6, 15, 19.7, 21.1, and 22.degree..+-.0.2.degree.; (b) a DSC melting peak at 288.degree. C.; (c) a .sup.13C 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.
Inventor(s): King, Jr.; Harry M. (Webster, NY)
Assignee: Bausch & Lomb Incorporated (Rochester, NY)
Application Number:12/723,047
Patent Claims: 1. 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 characterized by an X-ray powder diffraction ("XRPD") spectrum that comprises peaks at 2.theta. angles of 10.6, 15, 19.7, 21.1, and 22.degree..+-.0.2.degree..

2. 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 characterized by a differential scanning calorimetry ("DSC") melting peak at 288.degree. C.

3. 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 characterized by .sup.13C NMR spectrum having peaks at 23.3, 27.7, 41.1, 54.5, 116.6, and 153.5 ppm.

4. 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 characterized by pKa values of 5.65 and 9.91.

5. 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 characterized by an X-ray powder diffraction ("XRPD") spectrum that comprises peaks at 2.theta. angles of 10.6, 15, 19.7, 21.1, and 22.degree..+-.0.2.degree.; a DSC melting peak at 288.degree. C.; a .sup.13C NMR spectrum having peaks at 23.3, 27.7, 41.1, 54.5, 116.6, and 153.5 ppm; and by pKa values of 5.65 and 9.91.

6. A method of making a molecular crystal of besifloxacin ((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), comprising: (a) solubilizing a desired amount of a soluble salt of besifloxacin in a solvent (such as water) to form a solution; (b) adjusting the pH of the solution to a value in the range from about 6.2 to about 6.8; and (c) allowing a time sufficient to form the molecular crystal of besifloxacin.

7. The method of claim 6, further comprising recovering the molecular crystal of besifloxacin.

8. The method of claim 7, further comprising subjecting the recovered molecular crystal to a step of size reduction to nanometer- or micrometer-sized particles.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

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.

`abc