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Crystal form of icotinib maleate and its use

A technology of icotinib and maleic acid, which is applied in the field of treatment of cancer and cancer-related diseases, can solve problems such as the impossibility of predicting the crystal structure and properties, and the inability to predict the formation of different crystal forms of organic pharmaceutical compounds

Active Publication Date: 2016-03-23
BETTA PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is often impossible to predict whether a particular organic pharmaceutical compound will form different crystalline forms, let alone the structure and properties of the crystalline forms themselves

Method used

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  • Crystal form of icotinib maleate and its use
  • Crystal form of icotinib maleate and its use
  • Crystal form of icotinib maleate and its use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Example 1. Preparation of Form I (the first preparation method of Form I)

[0066] 100g of icotinib hydrochloride was dissolved in a mixture of 300ml of ethanol and 200ml of water. A solution prepared by dissolving 11.2 g of sodium hydroxide in 100 ml of water was added dropwise to the solution of icotinib hydrochloride at 60° C. until the pH value of the resulting reaction solution reached 13. The reaction solution was stirred for 1 hour and cooled to room temperature to form a precipitate. The precipitate was filtered out, washed with pure water, and dried under vacuum at a temperature lower than 60° C. for 8 hours to obtain 90 g of icotinib.

[0067]

[0068]Form I of icotinib maleate was obtained by reacting icotinib solution with maleic acid solution (1:1 molar ratio) in tetrahydrofuran (THF) at room temperature. Specifically, 10 mg of icotinib was first dissolved in 1 ml of THF to obtain an icotinib solution. In addition, 34.82 mg of maleic acid was also dis...

Embodiment 2

[0070] Example 2. Preparation of Form I

[0071] The second example of the preparation method of Form I is by changing the molar ratio of maleic acid and icotinib in the reaction mixture to 2:1 and following the same steps as described in Example 1 and keeping the same reaction conditions preparation. The melting point of this crystalline form is 173-176°C.

Embodiment 3

[0072] Example 3. Preparation of Form I

[0073] A third example of a preparation method for Form I is by changing the molar ratio of maleic acid and icotinib in the reaction mixture to 1.5:1 (i.e., 3:2) and following the same procedure as described in Example 1. Steps and keep the same reaction conditions for the preparation. The melting point of this crystalline form is 173-176°C.

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Abstract

Provided are Icotinib maleate(the compound of Formula I) and polymorph forms thereof, and methods of preparing and using them.

Description

technical field [0001] The present invention relates to icotinib maleate and new crystal forms thereof, methods for preparing these new crystal forms, pharmaceutical compositions comprising the above-mentioned new crystal forms, and the new crystal forms and pharmaceutical compositions thereof for the treatment of cancer and with Uses in cancer-related diseases. Background technique [0002] Tyrosine kinase receptors are transmembrane proteins that respond to extracellular stimuli and propagate signaling cascades to control cell proliferation, angiogenesis, apoptosis, and other important functions of cell growth. One such class of receptors is the epidermal growth factor receptor (EGFR) tyrosine kinases. These receptors are overexpressed in many tumors in humans, including those of the brain, lung, liver, bladder, breast, head and neck, esophagus, gastrointestinal tract, ovary, cervix, or thyroid. [0003] EGFR is expressed in many types of tumor cells and binds to the ext...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D491/056A61K31/519A61P35/00
CPCC07D491/056A61K31/517A61K31/519A61K45/06C07B2200/13C07C57/145
Inventor 胡邵京龙伟王飞王印祥丁列明
Owner BETTA PHARM CO LTD