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A kind of ubenimex hydrochloride compound

A technology of urbenex hydrochloride and compound, which is applied in the separation/purification of carboxylic acid amide, organic chemistry, drug combination, etc., to achieve the effect of good chemical stability and improved safety

Active Publication Date: 2015-08-26
西安万隆制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But it is not the crystal form of ubenimex hydrochloride;

Method used

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  • A kind of ubenimex hydrochloride compound
  • A kind of ubenimex hydrochloride compound
  • A kind of ubenimex hydrochloride compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The preparation of embodiment 1 ubenimex hydrochloride crystal form

[0029] preparation:

[0030] Add 0.5 g of ubenimex hydrochloride to 22 mL of a mixed solvent of isopropyl acetate: dimethylformamide with a volume ratio of 10:1, heat slightly to dissolve, stir for 1.5 h, filter, and store in a static state. Three days later, the solvent was completely evaporated, and the solid was crushed, left to dry at room temperature for 6 hours, and samples were collected to obtain 0.45 g of crystalline form of ubenimex hydrochloride.

[0031] Measured under the above-mentioned instrument and condition, obtain as figure 1 with figure 2 The shown XRD-powder diffraction pattern and infrared spectrum.

Embodiment 2

[0032] The preparation of embodiment 2 ubenimex hydrochloride crystal form

[0033] Add 1.0 g of ubenimex hydrochloride to 30 mL of a mixed solvent of isopropyl acetate: dimethylformamide with a volume ratio of 14:1, heat slightly to dissolve, stir for 1.5 h, filter, and keep it standing for three After a few days, the solvent was completely evaporated, and the solid was crushed, left to dry at room temperature for 5 hours, and samples were collected to obtain 0.88 g of crystalline form of Ubenimex hydrochloride.

[0034] Carry out the mensuration as embodiment 1, obtained result is consistent with embodiment 1.

Embodiment 3

[0035] The preparation of embodiment 3 ubenimex hydrochloride crystal form

[0036] Add 1.0 g of ubenimex hydrochloride to 40 mL of a mixed solvent of isopropyl acetate: dimethylformamide with a volume ratio of 19:1, heat slightly to dissolve, stir for 2 hours, filter, and keep it standing for three days. The solvent was completely evaporated, the solid was crushed, and left to dry at room temperature for 6 hours, and the sample was collected to obtain 0.93 g of crystalline form of Ubenimex hydrochloride.

[0037] Carry out the mensuration as embodiment 1, obtained result is consistent with embodiment 1.

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Abstract

The invention provides an ubenimex hydrochloride crystal-form compound. The ubenimex hydrochloride crystal-form compound has good dissolvability and stability. The invention also provides a preparation method of the ubenimex hydrochloride crystal-form compound and a pharmaceutical composition containing the ubenimex hydrochloride crystal-form compound. The ubenimex hydrochloride crystal-form compound can be processed to form any dosage forms such as tablets, capsules, an injection, pills, particles and drop pills. The invention also provides a use of the ubenimex hydrochloride crystal-form compound in preparation of drugs for treating cancers.

Description

technical field [0001] The invention relates to the field of chemical synthesis and specifically designs a new crystal form compound of ubenimex hydrochloride. Background technique [0002] Ubenimex is a compound isolated from the culture medium of Streptomyces, which can competitively inhibit aminopeptidase B (aminopeptidase B) and leucine aminopeptidase (leucineaminopeptidase), enhance the function of T cells, and make NK cells Its killing activity is enhanced, and it can increase the synthesis of colony-stimulating factor and stimulate the regeneration and differentiation of bone marrow cells. Ubenimex has the function of enhancing immunity and is the only CD13 antagonist in clinical practice. It can comprehensively block the occurrence and development of various tumor cells, thereby inhibiting tumor metastasis and recurrence, inhibiting tumor angiogenesis and tumor cell proliferation, and promoting tumor growth. Apoptosis, can be used in combination with chemotherapy, r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C237/20C07C231/24A61K31/198A61P35/00
Inventor 王震於长权温锦荣
Owner 西安万隆制药股份有限公司
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