Novel crystal of cephalosporin compound
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsKohji Kawabata, Takeshi Terasawa, Ayako Ohki, Fumiyuki Shirai, Hirofumi Yamamoto, Ryoichi Kawakami, Chiaki Hamaguchi
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Abstract
A novel crystal of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof. Said compound is a cephalosporin antibiotic having very strong antibacterial activity which exhibits superior characteristics physically, chemically and pharmaceutically.
Claims25
A crystal of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof.
The crystal of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof characterized in that which is crystallized from solution containing 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof under acidic conditions at cooled temperature, room temperature or elevated temperature.
The crystal of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof, wherein the solution containing 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof contains a lower alcohol and water.
A process for producing crystals of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof characterized in that which is crystallized from solution containing 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof under acidic conditions at cooled temperature, room temperature or elevated temperature.
A crystal of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid which shows peaks at the following diffraction angles in its a powder x-ray diffraction pattern:
- ca. 7.5°, ca. 11.3°, ca. 19.5°, ca.21.3°, ca. 24.5°, ca. 25.9°, ca. 29.0°.
A process for producing 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof hydrate crystals characterized in that 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof solvate crystals containing water and organic solvent are subjected to treatment for removal of the organic solvent.
Dependencies are inferred from the claim text.