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Crystal form of hypoxia inducible factor prolyl hydroxylase inhibitor and preparation method thereof

A crystal form, nicotinamide technology, applied in the field of medicinal chemistry, can solve the problems of poor crystallinity of crystal form B, no research work on Vadadustat crystal form screening, poor reproducibility, etc.

Pending Publication Date: 2022-03-01
SUNSHINE LAKE PHARM CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The original research AkIIbia company disclosed Vadadustat crystal forms A, B, and C in WO2015073779A1. Crystal form B may be converted into crystal form A in the slurry at high temperature. Among them, crystal form A is a stable crystal form, but its solubility in water is very poor. Crystal form B Poor crystallinity, poor stability, crystal form C is difficult to reproduce by conventional methods, its preparation conditions are harsh, and the reproducibility is poor
Moreover, the patent WO2015073779A1 did not do more screening research on the crystal form of Vadadustat

Method used

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  • Crystal form of hypoxia inducible factor prolyl hydroxylase inhibitor and preparation method thereof
  • Crystal form of hypoxia inducible factor prolyl hydroxylase inhibitor and preparation method thereof
  • Crystal form of hypoxia inducible factor prolyl hydroxylase inhibitor and preparation method thereof

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Embodiment Construction

[0032] The inventor has developed the crystal form of the compound Vadadustat and its preparation method through research.

[0033] The crystal forms of Vadadustat provided by the present invention are called crystal form II, crystal form H1, crystal form H2, crystal form H3, crystal form H4 or crystal form H5. These crystal forms have good performance, high solubility and high bioavailability ; or / and good in stability, which is conducive to storage, thereby meeting the requirements of drug stability; low hygroscopicity, or / and good performance in terms of static electricity, low static electricity, which is conducive to operation in the production process.

[0034] In a first aspect, the present invention provides a new crystal form of Vadadustat, called Form II.

[0035] The crystal form II of Vadadustat has the following characteristics: its X-ray powder diffraction pattern contains diffraction peaks at 2θ angles of 14.38, 20.80 and 26.85 degrees.

[0036] In some embodim...

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Abstract

The invention relates to the field of medicinal chemistry, in particular to a crystal form of a hypoxia inducible factor prolyl hydroxylase inhibitor and a preparation method of the crystal form. An X-ray powder diffraction pattern of the crystal form comprises diffraction peaks with 2 theta angles of 14.38 degrees, 20.80 degrees and 26.85 degrees. Wherein the crystal form has better performance and can be used for treating or preventing anemia; the preparation method of the crystal form is simple, convenient to operate and mild in condition.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a crystal form of a hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor and a preparation method thereof. Background technique [0002] Vadadustat (CAS No.: 1000025-07-9), whose chemical name is {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, was developed by AkIIbia company and has the effect of treating or preventing anemia Function, the mechanism of action is hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor, which is in the third phase of clinical treatment of anemia caused by secondary chronic kidney disease; its structural formula is as follows: [0003] [0004] The original research AkIIbia company disclosed Vadadustat crystal forms A, B, and C in WO2015073779A1. Crystal form B may be converted to crystal form A in the slurry at high temperature. Among them, crystal form A is a stable crystal form, but its solubility in water is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/81A61K31/44A61P7/06A61P13/12
CPCC07D213/81A61P7/06A61P13/12C07B2200/13
Inventor 叶辉青张娅璇黄河肖清波李亚平陈勇黄芳芳
Owner SUNSHINE LAKE PHARM CO LTD