BR112021018204A2 - Forma cristalina a de análogo de nucleosídeo 2?-fluoro-4?-substituído i e método de preparação do mesmo e uso do mesmo - Google Patents

Forma cristalina a de análogo de nucleosídeo 2?-fluoro-4?-substituído i e método de preparação do mesmo e uso do mesmo

Info

Publication number
BR112021018204A2
BR112021018204A2 BR112021018204A BR112021018204A BR112021018204A2 BR 112021018204 A2 BR112021018204 A2 BR 112021018204A2 BR 112021018204 A BR112021018204 A BR 112021018204A BR 112021018204 A BR112021018204 A BR 112021018204A BR 112021018204 A2 BR112021018204 A2 BR 112021018204A2
Authority
BR
Brazil
Prior art keywords
crystalline form
fluoro
nucleoside analog
substituted nucleoside
preparation
Prior art date
Application number
BR112021018204A
Other languages
English (en)
Inventor
Chang Junbiao
Du Jinfa
Ge Dongxu
Original Assignee
Henan Genuine Biotech Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Henan Genuine Biotech Co Ltd filed Critical Henan Genuine Biotech Co Ltd
Publication of BR112021018204A2 publication Critical patent/BR112021018204A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/073—Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C07H1/06—Separation; Purification
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

trata-se de uma forma cristalina a de um análogo de nucleosídeo 2?-fluoro-4?-substituído i, em que a mesma está dentro do campo de química farmacêutica. a forma cristalina a tem a seguinte estrutura: (i). o padrão de xrpd de cuka da forma cristalina a do composto i é conforme mostrado na figura 2, em que a forma cristalina a tem uma estabilidade satisfatória e pode ser fácil e uniformemente misturada com materiais auxiliares. a forma cristalina a do composto i é misturada com os materiais auxiliares, de modo que a uniformidade dos mesmos em comprimidos seja aumentada, e a mesma é condutora para controlar a qualidade de fármaco e garantir a eficácia de fármaco. a forma cristalina a é usada para preparar fármacos anti-hbv ou anti-hcv ou anti-hiv ou fármacos antitumorais.
BR112021018204A 2019-03-15 2019-04-18 Forma cristalina a de análogo de nucleosídeo 2?-fluoro-4?-substituído i e método de preparação do mesmo e uso do mesmo BR112021018204A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201910197742 2019-03-15
PCT/CN2019/083217 WO2020186588A1 (zh) 2019-03-15 2019-04-18 2'-氟-4'-取代核苷类似物i的晶型a及其制备方法和应用

Publications (1)

Publication Number Publication Date
BR112021018204A2 true BR112021018204A2 (pt) 2021-11-16

Family

ID=67191814

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021018204A BR112021018204A2 (pt) 2019-03-15 2019-04-18 Forma cristalina a de análogo de nucleosídeo 2?-fluoro-4?-substituído i e método de preparação do mesmo e uso do mesmo

Country Status (9)

Country Link
US (1) US20220002333A1 (pt)
EP (1) EP3939984A4 (pt)
JP (1) JP2022525818A (pt)
KR (1) KR102546496B1 (pt)
CN (1) CN110016068B (pt)
AU (1) AU2019435643B2 (pt)
BR (1) BR112021018204A2 (pt)
CA (1) CA3133415C (pt)
WO (1) WO2020186588A1 (pt)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116478223A (zh) * 2022-01-17 2023-07-25 河南真实生物科技有限公司 4’-取代核苷的晶体、其制备方法、组合物和用途
CN115093453A (zh) * 2022-07-30 2022-09-23 汉瑞药业(荆门)有限公司 阿滋福啶的晶型ⅰ及其制备方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK11922002A3 (sk) 2000-02-18 2003-06-03 Shire Biochem Inc. Použitie analógov nukleozidov na liečenie alebo prevenciu infekcií spôsobených flavivírusom
EP1646654A1 (en) 2003-07-08 2006-04-19 Genesto A/S BINDING MEMBER TOWARDS PNEUMOCOCCUS SURFACE ADHESIN A PROTEIN (PsaA)
CN100532388C (zh) 2007-07-16 2009-08-26 郑州大学 2’-氟-4’-取代-核苷类似物、其制备方法及应用
US20090318380A1 (en) * 2007-11-20 2009-12-24 Pharmasset, Inc. 2',4'-substituted nucleosides as antiviral agents
CN102000103B (zh) * 2009-12-21 2011-12-21 郑州大学 2’-氟-4’-叠氮-核苷类似物或其盐的药物应用
CN103709220B (zh) * 2014-01-13 2016-02-17 河南省科学院高新技术研究中心 3-甲基尿苷及4-甲基胞苷核苷类化合物、合成方法及其药物用途
CN108503681B (zh) * 2018-05-19 2019-06-04 河南省医药科学研究院 白桦脂酸衍生物及其合成方法和应用

Also Published As

Publication number Publication date
CA3133415A1 (en) 2020-09-24
WO2020186588A1 (zh) 2020-09-24
AU2019435643A1 (en) 2021-10-07
KR20210139355A (ko) 2021-11-22
KR102546496B1 (ko) 2023-06-21
JP2022525818A (ja) 2022-05-19
AU2019435643B2 (en) 2022-06-09
EP3939984A1 (en) 2022-01-19
US20220002333A1 (en) 2022-01-06
CN110016068B (zh) 2021-12-14
CA3133415C (en) 2023-12-19
AU2019435643A8 (en) 2021-10-14
CN110016068A (zh) 2019-07-16
EP3939984A4 (en) 2022-05-04

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Legal Events

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B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]