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Baricitinib trifluoroacetate crystal forms A and B and preparation method thereof

A technology of trifluoroacetate and crystal form of baricitinib, applied in the field of crystal form A and crystal form B of baricitinib trifluoroacetate and its preparation, can solve the problem of affecting bioavailability, baricitinib The stability of nitrifluoroacetate needs to be improved to achieve the effect of high stability

Active Publication Date: 2016-05-11
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 the problem that the stability of the existing baricitinib trifluoroacetate needs to be improved to affect the bioavailability. At the same time, it is hoped that a new crystal form of baricitinib trifluoroacetate can be sought, Provide more qualitative and quantitative information for the efficacy research of solid drugs

Method used

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  • Baricitinib trifluoroacetate crystal forms A and B and preparation method thereof
  • Baricitinib trifluoroacetate crystal forms A and B and preparation method thereof
  • Baricitinib trifluoroacetate crystal forms A and B and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1 Preparation of crystal form A of baricitinib trifluoroacetate

[0060] Add 400 mg of baricitinib trifluoroacetate semi-crystals into 4 mL of acetone to prepare a solution at 50 ° C, and the solution is rapidly cooled to 15 ° C under ultrasonic conditions, then filtered, dried to obtain a solid, and the weight of the solid is weighed is 106mg.

Embodiment 2

[0061] Example 2 Preparation of crystal form A of baricitinib trifluoroacetate

[0062] Add 400 mg of baricitinib trifluoroacetate semi-crystals into 3.3 mL of acetone to prepare a solution at 54°C. The solution is rapidly cooled to 0°C under ultrasonic conditions, filtered, and dried to obtain a solid. Weigh the solid The weight is 113mg.

Embodiment 3

[0063] Example 3 Preparation of crystal form A of baricitinib trifluoroacetate

[0064] Add 400 mg of baricitinib trifluoroacetate semi-crystals into 5 mL of acetone to prepare a solution at 52 °C, and then quickly cool the solution to 20 °C under ultrasonic conditions, then filter, dry to obtain a solid, and weigh the weight of the solid is 97mg.

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Abstract

The invention provides Baricitinib trifluoroacetate crystal forms A and B in the formula (I) (please see the formula in the description). The XRPD atlas of the crystal form A has diffraction peaks at the positions representing that 2theta equals to 8.60, 10.12, 10.72, 14.02, 16.66, 17.24, 17.84, 18.90, 19.54, 20.26, 21.54, 21.94, 23.40, 23.78, 24.66, 25.64, 25.98, 26.32, 27.12, 28.16, 30.34 and 31.12, and the XRPD atlas of the crystal form B has diffraction peaks at the positions representing that 2theta equals to 5.34, 9.00, 10.08, 10.70, 16.12, 17.44, 17.80, 18.92, 19.48, 20.22, 21.56, 22.68, 23.42, 23.98, 25.84, 27.22, 28.76, 29.46 and 32.66, wherein the error range of 2theta is + / -0.2. The stability of the Baricitinib trifluoroacetate crystal forms A and B is better than that of a Baricitinib trifluoroacetate semi-crystal, and the medicine processing of the crystal forms A and B and the application of the crystal forms A and B in a medicine composition are facilitated. The Baricitinib trifluoroacetate crystal forms A and B can be applied in medicine for treating immunity diseases, inflammatory diseases or cancers; meanwhile, qualitative and quantitative information is provided, and important significance is achieved for further studying the treatment effect of such type of solid medicine.

Description

technical field [0001] The present invention relates to polymorphic forms of baricitinib trifluoroacetate salt as a JAK inhibitor, in particular, to baricitinib trifluoroacetic acid salt A crystal form and B crystal form 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 knocko...

Claims

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Application Information

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IPC IPC(8): C07D487/04
CPCC07B2200/13C07D487/04
Inventor 任国宾弋东旭陈金姚
Owner SHANGHAI SUNTRONG BIOTECH
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