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A crystal form of ethanolamine salt of thrombopoietin mimic and its preparation method

A technology of ethanolamine salt and diethanolamine salt is applied in the field of monoethanolamine salt A crystal form and preparation, and can solve the problems affecting the curative effect, stability and bioavailability of drugs and the like

Active Publication Date: 2020-11-17
JIANGSU HENGRUI MEDICINE CO LTD
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  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Different crystal forms of the same drug may have significant differences in stability and bioavailability, which will affect the efficacy of the drug

Method used

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  • A crystal form of ethanolamine salt of thrombopoietin mimic and its preparation method
  • A crystal form of ethanolamine salt of thrombopoietin mimic and its preparation method
  • A crystal form of ethanolamine salt of thrombopoietin mimic and its preparation method

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Embodiment Construction

[0025] 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.

[0026] "X-ray powder diffraction pattern or XRPD" described in the present invention refers to according to Bragg's formula 2d sinθ=nλ (wherein, λ is the wavelength of X-ray, The order n of diffraction is any positive integer, generally take the first-order diffraction peak, n=1), when the X-ray is incident on the crystal or part of the crystal sample at the grazing angle θ (the compl...

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Abstract

The present invention relates to the crystal forms of the ethanolamine salts of thrombopoietin mimetic, and a preparation method thereof, particularly to the crystal form B of the diethanolamine saltof a (Z)-5-(2-hydroxy-3-(2-(3-methyl-5-oxo-1-(5,6,7,8-tetrahydronaphthalene-2-yl)-1H-pyrazole-4(5H)-ylidene)hydrazinyl)phenyl)furan-2-carboxylic acid compound represented by a formula (I), the crystalform A of the monoethanolamine salt of the compound represented by the formula (I), and a preparation method of the crystal forms. According to the present invention, the crystal form B of the diethanolamine salt of compound represented by the formula (I) and the crystal form A of the monoethanolamine salt of compound represented by the formula (I) have advantages in moisture absorption property.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and relates to a chemical named (Z)-5-(2-hydroxyl-3-(2-(3-methyl-5-oxo-1-(5,6,7,8-tetra Diethanolamine salt B crystal form, monoethanolamine salt A crystal form and Preparation. Background technique [0002] Thrombopoietin (TPO) is a hematopoietic growth factor that stimulates platelet production in the body. It can regulate the proliferation, differentiation, and maturation of megakaryocytes by binding to a specific receptor (c-Mpl), thereby forming platelets and increasing the number of platelets in circulating blood. . In November 2008, the world's first small-molecule TPO mimic, eltrombopag, developed by GSK, was approved by the US FDA for marketing, and it was launched in Europe in 2009. [0003] WO2009092276 discloses a new small molecule TPO mimetic, as shown in formula (I), which can significantly activate TPO receptor cMpl; its ability to activate TPO receptor cMpl in mice reaches 2...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D405/12A61K31/4155A61P7/02
CPCA61P7/02C07B2200/13C07D405/12
Inventor 赵苗苗张全良刁艾青杜振兴王立坤
Owner JIANGSU HENGRUI MEDICINE CO LTD
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