Flumatinib mesylate crystal form B and preparation method and use thereof

A technology of flumatinib mesylate and crystal form, which is applied in the field of preparation of drugs for the treatment of chronic myeloid leukemia, and can solve problems such as structural changes, failure to combine with Gleevec, and occurrence of chronic myeloid leukemia patients

Active 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 B and preparation method and use thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Put 1.0 g of flumatinib mesylate and 100.0 ml of ethyl acetate in a reaction flask, heat to reflux until completely dissolved, naturally cool to room temperature under stirring conditions, stir for 24 hours, precipitate solids, filter, and vacuum dry to obtain Form B.

Embodiment 2

[0018] Put 100 g of flumatinib mesylate and 2,000 ml of isopropanol in a reaction flask, heat to reflux until solid forms an oily substance, naturally cool to room temperature under stirring conditions, stir vigorously for 48 hours, and the oily substance turns into a solid, Filter and dry in vacuo to obtain Form B.

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Abstract

The invention relates to flumatinib mesylate crystal form B and a preparation method and the use thereof. 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 present 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 a medicine for treating chronic myeloid 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 ...

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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