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Novel crystal form of ibrutinib and preparation method thereof

A technology of ibrutinib and crystal form, which is applied in the field of medicinal chemistry and can solve problems affecting the quality of drugs

Inactive Publication Date: 2015-11-25
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because drug polymorphism is a common phenomenon in drug research and development, it is an important factor affecting drug quality.

Method used

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  • Novel crystal form of ibrutinib and preparation method thereof
  • Novel crystal form of ibrutinib and preparation method thereof
  • Novel crystal form of ibrutinib and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0028] In the first aspect, the inventor developed a crystal form of ibrutinib through research, which is called crystal form A2.

[0029] The crystal form A2 of ibrutinib has the following characteristics: its differential scanning calorimetry curve (DSC) has an endothermic peak at 185°C-210°C.

[0030] In some embodiments, the differential scanning calorimetry curve (DSC) of the crystalline form A2 of ibrutinib has an endothermic peak at 190°C-205°C. In some embodiments, the differential scanning calorimetry curve (DSC) of the crystalline form A2 of ibrutinib has an endothermic peak at 194°C-204°C. In some embodiments, the peak value of the endothermic peak of the differential scanning calorimetry curve (DSC) of the crystalline form A2 of ibrutinib is about 201.3°C. In some embodiments, the differential scanning calorimetry curve (DSC) of the crystalline form A2 of ibrutinib is as follows: figure 1 shown.

[0031] The above crystal form A2 of ibrutinib also has the follow...

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Abstract

The present invention relates to a novel crystal form of ibrutinib and a preparation method thereof, and belongs to the technical field of pharmacy. The differential scanning calorimetry curve of the novel crystal form has endothermic peak at 194-204 DEG C; and the novel crystal form has good physical and chemical properties, is conducive to the production operation, and can be used in the preparation of pharmaceutical preparations.

Description

technical field [0001] The invention relates to a new crystal form of ibrutinib and a preparation method thereof, belonging to the field of medicinal chemistry. Background technique [0002] Ibrutinib (English name Ibrutinib), chemical name 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d ]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one, an irreversible Bruton's tyrosine kinase (BTK, Bruton'styrosinekinase) inhibitor capable of inhibiting malignant B cells Proliferation, survival, can be used for the treatment of diseases such as chronic lymphocytic leukemia (CLL) and small cell lymphocytic lymphoma; Its structure is as shown in formula (1): [0003] [0004] PCT application WO2013184572 discloses various crystal forms thereof. However, drug polymorphism is a common phenomenon in drug research and development, and it is an important factor affecting drug quality. Different crystal forms of the same drug may have significant differences in physical and chemical pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/519A61P35/00A61P35/02
CPCC07D487/04
Inventor 罗真秀张洽洪陈勇
Owner SUNSHINE LAKE PHARM CO LTD
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