CN112752577A - Daprodustat的晶型及其制备方法和用途 - Google Patents

Daprodustat的晶型及其制备方法和用途 Download PDF

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Publication number
CN112752577A
CN112752577A CN201980002213.9A CN201980002213A CN112752577A CN 112752577 A CN112752577 A CN 112752577A CN 201980002213 A CN201980002213 A CN 201980002213A CN 112752577 A CN112752577 A CN 112752577A
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crystalline form
crystal form
hydroxylase inhibitor
inhibitor according
crystal
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CN112752577B (zh
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任国宾
季伟杰
弋东旭
黄嘉骏
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Shenzhen Rentai Pharmaceutical Technology Co Ltd
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Shenzhen Rentai Pharmaceutical Technology Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60—Three or more oxygen or sulfur atoms
    • C07D239/62—Barbituric acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A61K31/515—Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

一种脯氨酸羟化酶抑制剂daprodustat的晶型M，使用Cu‑Kɑ辐射，以2θ角度表示的X‑射线粉末衍射，在4.7±0.2°、6.5±0.2°、6.8±0.2°处有特征峰。晶型M的制备方法和用途。该晶型M具有良好的光照稳定性、高温稳定性和高湿稳定性，良好的溶解性，且纯度较高。

Description

PCT国内申请，说明书已公开。

Claims (15)

  1. PCT国内申请，权利要求书已公开。
CN201980002213.9A 2019-08-20 2019-08-20 Daprodustat的晶型及其制备方法和用途 Active CN112752577B (zh)

Applications Claiming Priority (1)

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PCT/CN2019/101496 WO2021031102A1 (zh) 2019-08-20 2019-08-20 Daprodustat的晶型及其制备方法和用途

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CN112752577A true CN112752577A (zh) 2021-05-04
CN112752577B CN112752577B (zh) 2023-07-07

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Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3221427A1 (en) 2021-06-18 2022-12-22 Nicholas FALCO Novel manufacturing method of daprodustat and precursors thereof
CA3221668A1 (en) 2021-06-25 2022-12-29 Glaxosmithkline Intellectual Property (No.2) Limited Daprodustat for reducing fatigue in a subject with anemia associated with chronic kidney disease
WO2024022998A1 (en) * 2022-07-26 2024-02-01 Inke, S.A. Process for preparing daprodustat and cocrystals thereof
GB202211231D0 (en) 2022-08-02 2022-09-14 Glaxosmithkline Ip No 2 Ltd Novel formulation

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018035112A (ja) * 2016-09-01 2018-03-08 公立大学法人大阪市立大学 抗癌剤の抗腫瘍効果の増強剤、癌治療剤、及び癌治療用医薬組成物。
WO2019052133A1 (zh) * 2017-09-15 2019-03-21 苏州科睿思制药有限公司 Gsk1278863的晶型及其制备方法和制药用途

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR061570A1 (es) * 2006-06-23 2008-09-03 Smithkline Beecham Corp Compuesto de glicina sustituido en el n heteroaromatico composicion farmaceutica que lo comprende, su uso para preparar un medicamento, procedimientos para preparar dicha composicion farmaceutica y para preparar el compuesto

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018035112A (ja) * 2016-09-01 2018-03-08 公立大学法人大阪市立大学 抗癌剤の抗腫瘍効果の増強剤、癌治療剤、及び癌治療用医薬組成物。
WO2019052133A1 (zh) * 2017-09-15 2019-03-21 苏州科睿思制药有限公司 Gsk1278863的晶型及其制备方法和制药用途

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KIMBERLY A等: "An Emerging Treatment Alternative for Anemia in Chronic Kidney Disease Patients: A Review of Daprodustat" *
袁秋慧等: "新型慢性肾脏疾病贫血治疗药物的临床研究进展" *

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CN112752577B (zh) 2023-07-07
WO2021031102A1 (zh) 2021-02-25
US20220169619A1 (en) 2022-06-02

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