113028-17-4Relevant articles and documents
Ulifloxacin hydrochloride crystal and its preparation method and use
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Paragraph 0061; 0062, (2018/03/01)
The invention provides an ulifloxacin hydrochloride crystal. The X-ray powder diffraction pattern of the ulifloxacin hydrochloride crystal under Cu-K alpha radiation has peaks at 2 theta angles of 8.362+/-0.2 degrees, 9.513+/-0.2 degrees, 12.663+/-0.2 degrees, 21.253+/-0.2 degrees and 24.129+/-0.2 degrees. The invention provides a preparation method of the crystal, a pharmaceutical composition comprising the crystal and a pharmaceutical use of the crystal and the pharmaceutical composition. The ulifloxacin hydrochloride crystal has good reproducibility. The preparation method is simple and reduces the dosage of the organic solvent. Experiments prove that the novel crystal and the mother crystal of ulifloxacin hydrochloride have significant effects in the aspects of solubility, stability, hygroscopicity and in-vivo therapeutic effects. The novel crystal can be processed into a variety of dosage forms and has good clinical application potential.
CRYSTALLINE FORM OF PRULIFLOXACIN AND PROCESSES FOR ITS PREPARATION
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Page/Page column 21-22, (2012/01/14)
The present invention relates to a crystalline polymorphic form of 6-fluoro-1-methyl-7- {4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]piperazin-1-yl}-4-oxo-4H-[1,3]-thiazeto-[3,2- a]-quinoline-3-carboxylic acid (prulifloxacin). More specifically, the invention relates to a crystalline form of prulifloxacin (herein referred to as Form A), and a method for preparing the crystalline Form A. The present invention further provides a pharmaceutical formulation comprising the novel form of prulifloxacin.
STUDIES ON PYRIDONECARBOXYLIC ACIDS. 1. SYNTHESIS AND ANTIBACTERIAL EVALUATION OF 7-SUBSTITUTED-6-HALO-4-OXO-4H-THIAZETOQUINOLINE-3-CARBOXYLIC ACIDS
Segawa, Jun,Kitano, Masahiko,Kazuno, Kenji,Matsuoka, Masato,Shirahase, Ichiro,et al.
, p. 4727 - 4738 (2007/10/02)
A series of thiazetoquinoline-3-carboxylic acids and their esters were prepared and evaluated for antibacterial activity.The derivatives with a hydrogen or methyl group at C-1, fluorine at C-6, and piperazinyl or 4-methyl-1-piperazinyl group at C-7 showed superior in vitro antibacterial activity, and the derivatives with 4-methyl-1-piperazinyl group at C-7 had potent in vivo activity.Compound 29a (NM394) showed excellent in vitro antibacterial activity and low toxicity but poor absorption from the gastrointestinal tract.Compound 29ee (NM441), an N- derivative of 29a, was found to possess a favorable pharmacokinetic profile and oral activity superior to that of ciprofloxacin in experimental animals.