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Crystal form of dimaleate of tyrosine kinase inhibitor and preparation method thereof

A technology of crystal form and solvent, which is applied in the field of crystal form of dimaleate of tyrosine kinase inhibitors and its preparation, which can solve the problems of easy agglomeration, poor fluidity, and poor product stability, etc.

Inactive Publication Date: 2019-01-15
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Generally speaking, amorphous pharmaceutical products have no regular crystal structure and often have other defects, such as poor product stability, difficult filtration, easy agglomeration, poor fluidity, etc.

Method used

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  • Crystal form of dimaleate of tyrosine kinase inhibitor and preparation method thereof
  • Crystal form of dimaleate of tyrosine kinase inhibitor and preparation method thereof
  • Crystal form of dimaleate of tyrosine kinase inhibitor and preparation method thereof

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Embodiment Construction

[0024] In the specification and claims of the present application, unless otherwise specified, the scientific and technical terms used herein have the meanings commonly understood by those skilled in the art. However, for a better understanding of the present invention, definitions and explanations of some related terms are provided below. In addition, when the definitions and explanations of terms provided in this application are inconsistent with the meanings commonly understood by those skilled in the art, the definitions and explanations of terms provided in this application shall prevail.

[0025] "C" described in the present invention 1-6 "Alkyl" means a linear or branched alkyl group containing 1-6 carbon atoms. Specific examples include, but are not limited to: methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, isopentyl, 2-methylbutyl, neopentyl, 1-ethylpropyl, n-hexyl, isohexyl, 3-methylpentyl, 2-methyl Amylpentyl, 1-methylpenty...

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Abstract

The invention relates to a crystal form of dimaleate of a tyrosine kinase inhibitor and a preparation method thereof. Specifically, the invention relates to an II crystal form of dimaleate of an epidermal growth factor receptor (EGFR) inhibitor and a preparation method thereof. The II crystal form has good chemical stability and crystal form stability, and can be better used in clinical treatment.

Description

technical field [0001] The invention relates to a crystal form of dimaleate salt of a tyrosine kinase inhibitor and a preparation method thereof. Background technique [0002] Studies have shown that more than 50% of proto-oncogenes and oncogene products have tyrosine kinase activity, and their abnormal expression will lead to tumorigenesis. Tyrosine kinase inhibitors have been on the market since 2001, and have become a new type of anticancer drug that has sprung up. [0003] Epidermal growth factor receptor (EGFR) is a member of the receptor tyrosine kinase family. The EGFR pathway plays a very important role in the occurrence and development of tumors, and has become the most important research and development topic in the field of tumor treatment. One of the development targets. Such drugs that are already on the market include erlotinib, gefitinib, and lapatinib (lapatinb, Tykerb, GW572016). [0004] WO2011029265A1 (publication date 2011.03.17) discloses an epidermal...

Claims

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Application Information

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IPC IPC(8): C07D401/14A61K31/4709A61P35/00
CPCC07D401/14A61P35/00C07B2200/13
Inventor 曹笑立王立坤杜振兴
Owner JIANGSU HENGRUI MEDICINE CO LTD
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