Salt of cephalosporin derivative, crystalline solid form of same and method for producing same

A technology for crystalline solids and sodium salts, applied in the field of salts of cephalosporin derivatives, can solve the problems of sodium salts, acid addition salts and solvates that have not been specifically disclosed, and achieve good solubility, good stability, and easy operation excellent effect

Active Publication Date: 2017-05-31
SHIONOGI & CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] (hereinafter also referred to as compound (IA)), but there is no specific disclosure about its sodium salt, acid addition salt and solvate

Method used

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  • Salt of cephalosporin derivative, crystalline solid form of same and method for producing same
  • Salt of cephalosporin derivative, crystalline solid form of same and method for producing same
  • Salt of cephalosporin derivative, crystalline solid form of same and method for producing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0191] The present invention is illustrated in more detail by the following examples. The present invention is not limited to these examples. With regard to numerical values ​​(such as amounts, temperatures, etc.), efforts have been made to be correct, but a certain degree of error and deviation should be taken into account. Unless otherwise indicated, % means the weight % of the component and the weight % of the total weight of the composition, and the equivalent means the molar equivalent of the component. Pressure is at or near atmospheric pressure. The meanings of other abbreviations used in this manual are as follows: g means gram, L means liter, mg means milligram, mL means milliliter, EDC means 1-ethyl-3-(3-dimethylaminopropyl)carbodiyl imine.

[0192] (Measurement of Powder X-ray Diffraction Pattern)

[0193] The powder X-ray diffraction measurement of the crystalline solid obtained in each example was performed under any one of the following measurement conditions...

Synthetic example 1

[0272] Synthesis of compound (IA)

[0273] Compound (IA) was adjusted according to the method described in International Publication No. 2010 / 050468, and the pKa of compound (IA) was measured, and the results were pKa1 = 4.2, pKa2 = 7.2.

Embodiment 1

[0275]

[0276] Compound (IA) (100 mg) was dissolved in 1.0 mol / L p-toluenesulfonic acid aqueous solution (2 mL) at room temperature using ultrasonic waves, and allowed to stand at 4° C. for 4 days. The precipitate was filtered to obtain seed crystal A (73 mg). Confirmed by microscopy as needle-like crystals.

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Abstract

The invention discloses a salt of cephalosporin derivative, a crystalline solid form of the same and a method for producing the same. The present invention provides an acid addition salt or sodium salt of a compound represented by formula (IA) (as shown in the description), a hydrate of the salt or a stable crystalline solid form of the salt. The salt or the crystalline solid form thereof is extremely useful as an active ingredient for the production of a pharmaceutical product.

Description

technical field [0001] The present invention relates to a salt of a cephalosporin derivative which is excellent in storage stability, solubility, formulation or process operability, its crystalline solid and its production method. Background technique [0002] The industry expects to provide salts or crystal forms with excellent chemical or physical properties in the manufacturing process of pharmaceuticals. [0003] The applicant of this case records in Patent Document 1 that cephalosporin derivatives having a catechol group have a broad antibacterial spectrum, especially exhibit strong antibacterial activity against β-lactamase-producing bacteria, so they are used as a treatment for infectious diseases. Or prophylactics are useful. The following compound (I-12) in the form of betaine is described in Example 12 of this document: [0004] [chemical formula 1] [0005] [0006] (hereinafter also referred to as compound (IA)), but there is no specific disclosure about it...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/46A61K9/19A61K31/546A61K47/02A61P31/04
CPCA61K9/19A61K31/185A61K31/546A61K47/02A61K2300/00A61K2800/84A61P31/04A61P31/10C07D227/06C07D501/16C07D501/46C07D513/04
Inventor 松原文彦栗田贵教永松大树
Owner SHIONOGI & CO LTD
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