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Flumatinib mesylate crystal form A and preparation method and use thereof

A technology of flumatinib mesylate and its crystal form is applied in the application field of preparing medicines for the treatment of chronic myeloid leukemia, and can solve the problems of inability to combine with Gleevec, structural changes, and the occurrence of chronic myeloid leukemia patients.

Inactive Publication Date: 2012-12-12
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, many chronic myeloid leukemia patients taking Gleevec have been found to develop drug resistance in recent years
In most cases, resistance arises because of a mutation in BCR-ABL that changes the structure of the enzyme so that Gleevec cannot bind to it

Method used

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  • Flumatinib mesylate crystal form A and preparation method and use thereof

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Experimental program
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Effect test

Embodiment 1

[0016] Put 1.0 g of flumatinib mesylate and 8.0 ml of isopropanol in a reaction flask, heat to reflux, and dissolve completely quickly, then naturally cool to room temperature under stirring conditions, stir for 24 hours, precipitate a solid, filter, Drying in vacuo yielded Form A.

Embodiment 2

[0018] Put 100g of flumatinib mesylate and 800ml of isopropanol in a reaction flask, heat to reflux, dissolve completely quickly, cool to room temperature naturally under stirring conditions, stir for 24 hours, precipitate solid, filter, and vacuum dry Form A was obtained.

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Abstract

The invention relates to flumatinib mesylate crystal form A and a preparation method and the use thereof. Specifically, one crystal form of the flumatinib mesylate, the preparation method thereof, medicine combination of the compound and with treatment effective quantity and application of the crystal form in preparation of medicine for treating chronic myelogenous leukemia are further provided.

Description

technical field [0001] The invention relates to a crystal form of flumatinib mesylate and a preparation method thereof, a pharmaceutical composition containing a therapeutically effective amount of the compound, and an application thereof in preparing medicines for treating chronic myelogenous leukemia. Background technique [0002] More than 95% of patients with chronic myelogenous leukemia are due to chromosomal translocation to produce BCR-ABL fusion protein, resulting in high expression of ABL tyrosine activating enzyme activity and a large number of abnormal white blood cells. [0003] In the prior art, drugs used to treat chronic myelogenous leukemia include recombinant interferon α-2a, cytarabine, homoharringtonine and imatinib. Gleevec (imatinib) is the main drug for the treatment of chronic myelogenous leukemia. The therapeutic mechanism is to inhibit the proliferation of cancer cells by inhibiting the activity of BCR-ABL, and at the same time induce apoptosis of ca...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61K31/506A61P35/02
Inventor 何雷杨宝海张亮
Owner JIANGSU HANSOH PHARMA CO LTD
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