Baricitinib polymorph A and preparation method thereof

A baricitinib and crystal form technology, applied in the field of baricitinib crystal form A and its preparation, can solve the instability of baricitinib, unfavorable crystal form transformation, strong hygroscopicity, etc. problem, to achieve the effect of good bioavailability and excellent high temperature stability

Inactive Publication Date: 2016-06-22
SHANGHAI SUNTRONG BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The problem to be solved by the present invention is to solve the existing baricitinib instability, strong hygroscopicity and easy crystal transformation, etc., which are unfavorable for its u

Method used

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  • Baricitinib polymorph A and preparation method thereof
  • Baricitinib polymorph A and preparation method thereof
  • Baricitinib polymorph A and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 6

[0035] Embodiments 1 to 6 Preparation of Baricitinib A Crystal Form

[0036] Weigh 800mg of baricitinib raw material into a container, add 1.5mL N,N dimethylformamide to completely dissolve it. Slowly add 50 mL of the solvent in Table 1 (analytical grade, water is deionized water) to the obtained solution respectively, let stand overnight, filter and vacuum dry to obtain an off-white solid. Weigh and calculate its yield, and the results are shown in Table 1.

[0037] Table 1 Preparation of baricitinib A crystal form

[0038] Example

Embodiment 7 to 12

[0039] Examples 7 to 12 Preparation of crystal form A of baricitinib

[0040] Weigh 1.0 g of baricitinib raw material into a container, add 1.0 mL of N,N dimethylformamide to completely dissolve it. Slowly add 60 mL of the solvent in Table 1 (analytical grade, water is deionized water) to the obtained solution respectively, let it stand overnight, filter, and vacuum-dry to obtain an off-white solid.

Embodiment 13 to 18

[0041] Examples 13 to 18 Preparation of crystal form A of baricitinib

[0042] Weigh 100mg of baricitinib raw material into a container, add 0.5mL N,N dimethylformamide to completely dissolve it. Slowly add 10 mL of the solvent in Table 1 (analytical grade, water is deionized water) to the obtained solution respectively, let stand overnight, filter and vacuum dry to obtain an off-white solid.

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PUM

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Abstract

The invention provides a baricitinib polymorph A. The baricitinib polymorph A is characterized in that diffraction peaks are arranged on an XRPD (X Ray Powder Diffraction) map when values of 2 theta are equal to 12.46, 13.921, 14.94, 15.359, 16.26, 16.639, 17.36, 19.08, 20.321, 21.961, 22.381, 24.118, 25.42, 27.441, 28.381, 29.321, 29.799, 32.675, 33.14, 33.563, 33.923 and 41.6, wherein an error range of the values of the 2 theta is +/- 0.2. The baricitinib polymorph A provided by the invention has good high-temperature stability, good high-humidity stability and good illumination stability, can be applied to medicine for treating or preventing diseases related to JAK (Janus Kinase) and has better biological availability; meanwhile, provided qualitative and quantitative information has important significance in further studying the therapeutic effect of such solid medicine.

Description

technical field [0001] The present invention relates to a polymorphic form of baricitinib as a JAK inhibitor, in particular to a polymorphic form of baricitinib A and a preparation method thereof. Background technique [0002] JAK is Janus Kinase, which is a non-receptor tyrosine protein kinase and a non-transmembrane tyrosine kinase. This is because JAK can not only phosphorylate the cytokine receptors associated with it, but also phosphorylate multiple signaling molecules containing specific SH2 domains. The JAK protein family includes 4 members: JAK1, JAK2, JAK3 and TYK2, which have 7 JAK homology domains (JAKhomology domain, JH) in their structure, of which the JH1 domain is the kinase domain and the JH2 domain is the "false" The kinase domain, JH6 and JH7 are receptor binding domains. [0003] TYK2 is a potential target for immunoinflammatory diseases, which has been confirmed by human genetics and mouse knockout studies (Levy D. and Loomis C., New England Journal of ...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/519A61P29/00A61P37/00A61P37/06A61P35/00
CPCC07D487/04C07B2200/13
Inventor 任国宾弋东旭陈金姚
Owner SHANGHAI SUNTRONG BIOTECH
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