- Ulifloxacin hydrochloride crystal and its preparation method and use
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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.
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Paragraph 0063; 0064
(2018/03/01)
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- Ulifloxacin hydrochloride crystal as well as preparation method and application thereof
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The invention provides an ulifloxacin hydrochloride crystal. The crystal uses an X-ray powder diffraction pattern of Cu-Ka radiation and has following peaks denoted with 2theta angles: 8.859 degrees plus or minus 0.2 degrees, 15.233 degrees plus or minus 0.2 degrees, 15.284 degrees plus or minus 0.2 degrees, 22.153 degrees plus or minus 0.2 degrees, 25.217 degrees plus or minus 0.2 degrees and 26.750 degrees plus or minus 0.2 degrees. The invention also provides a preparation method of the crystal, medicine composition containing the crystal as well as a pharmaceutical application of the crystal and the medicine composition. The provided crystal has good reproducibility, the preparation method is simple, and dosage of an organic solvent is reduced. Experiments prove that the novel crystal and an original ulifloxacin hydrochloride crystal both have a remarkable effect in the aspects of solubility, stability, moisture absorption and in-vivo therapy effect, and the novel crystal can be prepared in multiple dosage forms and has good clinical application potential.
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Paragraph 0057; 0058
(2018/03/24)
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- A method for preparing of plurichari (by machine translation)
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The invention relates to a prepration method of a compound prulifloxacin as shown in the formula (I), wherein the chemical name of prulifloxacin is 6-floro-1-methyl-7-[4-(5-methyl-2-oxo1,3-dioxo hetercyclopentene-4-yl)methyl-1-piperazinyl-4-oxo-4H-[1,3] thiaazacyclobutane[3,2-a] quinoline-3-carboxylic acid. The preparation method provided by the invention is a preparation method of prulifloxacin suitable for industrialized production, simple in process, high in purity and high in yield.
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Paragraph 0024; 0037; 0038; 0039
(2016/10/07)
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- CRYSTALLINE FORM OF PRULIFLOXACIN AND PROCESSES FOR ITS PREPARATION
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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.
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Page/Page column 22
(2012/01/14)
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- PROCESS FOR THE PREPARATION OF HIGHLY PURE PRULIFLOXACIN
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The present invention provides an industrially advantageous process for the preparation of highly pure prulifloxacin of formula I and its pharmaceutically acceptable salts. The present i innvention a also provides a novel process for the purification of prulifloxacin acid addition salt.
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Page/Page column 15
(2009/09/05)
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- PROCESS FOR PREPARATION OF PRULIFLOXACIN USING NOVEL INTERMEDIATES
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The present invention provides a novel process for the preparation of prulifloxacin intermediate, 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid, thereby producing prulifloxacin and its pharmaceutical acceptable acid addition salts thereof in high purity and in high yield using novel intermediates in lesser reaction time. Thus, for example, ethyl 6,7-difluoro-1-methyl-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate is reacted with boric acid in presence of acetic anhydride and acetic acid to give borane compound, which is then condensed with piperazine in presence of acetonitrile and dimethylsulfoxide, followed by treatment with potassium hydroxide solution to give 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid.
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Page/Page column 6-7
(2008/12/05)
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- STUDIES ON PYRIDONECARBOXYLIC ACIDS. 1. SYNTHESIS AND ANTIBACTERIAL EVALUATION OF 7-SUBSTITUTED-6-HALO-4-OXO-4H-THIAZETOQUINOLINE-3-CARBOXYLIC ACIDS
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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.
- Segawa, Jun,Kitano, Masahiko,Kazuno, Kenji,Matsuoka, Masato,Shirahase, Ichiro,et al.
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p. 4727 - 4738
(2007/10/02)
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- Substituted thiazetoquinoline-3-carboxylic acids and pharmaceutically acceptable salts thereof
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Anti-bacterial and anti-fungal compounds of formula I and pharmaceutically acceptable salts thereof: STR1 in which R1 is hydrogen, alkyl or substituted or unsubstituted phenyl; R2 is hydrogen, alkyl, alkoxy, hydroxy, halgen, nitro or substituted or unsubstituted amino; R3 is hydrogen or substituted or unsubstituted alkyl; R4 and R5 are the same or different and are alkyl or hydroxyalkyl or R4 and R5 together with the nitrogen atom to which they are attached form an unsubstituted or substituted heterocyclic ring having the depicted nitrogen atom as the sole heteroatom or which may have nitrogen, oxygen or sulphur atoms as additional heteroatoms; and X is halogen.
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