Salt of naphthyridine carboxylic acid derivative
AssigneeLG Life Sciences Ltd.
InventorsAe Ri Kim, Jin Hwa Lee, Ki Sook Park, Jong Ryoo Choi, Tae Hee Lee, Jay Hyok Chang, Do Hyun Nam, Hoon Choi
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Abstract
7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.
Claims33
A crystal form of 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate.nH2O, wherein n is in the range of from 1 to 4.
A solvate comprising a crystal form of 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and at least one organic solvent.
A process for preparing a solvate of 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate with at least one organic solvent, comprising:
- dissolving 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate anhydrate in a mixture of ethanol and water to form a solution;
- heating the solution to 50° C.;
- cooling the solution to −3° C.;
- allowing the solution to stand at −3° C., wherein a solid solvate forms;
- filtering the solid solvate;
- and
- washing the solid solvate with a mixture of ethanol and water.
Dependencies are inferred from the claim text.