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Crystal form of icotinib phosphate and its use

A technology of icotinib phosphate and crystal form, which can be used in medical preparations containing active ingredients, organic active ingredients, organic chemistry, etc. Different crystalline forms, etc.

Active Publication Date: 2016-07-13
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 phosphate and its use
  • Crystal form of icotinib phosphate and its use
  • Crystal form of icotinib phosphate and its use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Example 1. Preparation of Form I

[0095] 100g of icotinib hydrochloride was dissolved in a mixed solvent of 300ml of ethanol and 200ml of water. A solution formed by dissolving 11.2 g of sodium hydroxide in 100 ml of water was dropped into the above mixed solution at 60° C. until the pH value was 13. The reaction solution was stirred for 1 hour, cooled to room temperature, and a solid precipitated out. Filter and wash with pure water, and vacuum-dry at a temperature lower than 60°C for 8 hours to obtain 90 g of icotinib.

[0096]

[0097] At room temperature, the icotinib solution and phosphoric acid solution (molar ratio 1:1) were reacted in THF to prepare the No. 1 sample of crystal form I of icotinib phosphate. Specific steps: 10 mg icotinib was dissolved in 1 ml THF, and 18.9 μL phosphoric acid solution was added to 3 ml THF to make a 0.1 mol / L phosphoric acid solution. 0.26ml of 0.1mol / L phosphoric acid solution was added to the icotinib solution, and the re...

Embodiment 2

[0099] Example 2. Preparation of Form I

[0100] The preparation steps and conditions of Form I No. 2 sample are the same as in Example 1, except that the molar ratio of phosphoric acid and icotinib in the reaction solution is changed to 1.5:1.

Embodiment 3

[0101] Example 3. Preparation of Form I

[0102] The preparation steps and conditions of Form I No. 3 sample are the same as in Example 1, except that the molar ratio of phosphoric acid and icotinib in the reaction solution is changed to 2:1.

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Abstract

Disclosed is Icotinib phosphate (i.e., 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 new crystal forms of icotinib phosphate, methods for preparing these new crystal forms, pharmaceutical compositions containing the new crystal forms, and the new crystal forms and pharmaceutical compositions for the treatment of cancer and cancer-related diseases use. 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 extracellular domain with its cognate ligan...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519C07D491/056A61P35/00
CPCC07B2200/13C07D491/056
Inventor 胡邵京龙伟王飞王印祥丁列明
Owner BETTA PHARM CO LTD