WO2023093708A1 - Inhibiteur de fusion membranure anti-virus syncytial - Google Patents

Inhibiteur de fusion membranure anti-virus syncytial Download PDF

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Publication number
WO2023093708A1
WO2023093708A1 PCT/CN2022/133459 CN2022133459W WO2023093708A1 WO 2023093708 A1 WO2023093708 A1 WO 2023093708A1 CN 2022133459 W CN2022133459 W CN 2022133459W WO 2023093708 A1 WO2023093708 A1 WO 2023093708A1
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WO
WIPO (PCT)
Prior art keywords
compound
preparation
formula
lys
glu
Prior art date
Application number
PCT/CN2022/133459
Other languages
English (en)
Chinese (zh)
Inventor
于海宁
周述靓
王鹏
Original Assignee
成都奥达生物科技有限公司
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 成都奥达生物科技有限公司 filed Critical 成都奥达生物科技有限公司
Publication of WO2023093708A1 publication Critical patent/WO2023093708A1/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/06—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/10—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using coupling agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Definitions

  • the scientific research team of the present invention has been committed to the research and development of viral membrane fusion inhibitor drugs, and has developed a series of polypeptide membrane fusion inhibitors with strong inhibitory activity against syncytial virus (RSV), and they can also effectively inhibit RSV.
  • RSV syncytial virus
  • Infection see Chinese patent CN202010108065.3 for details, because the purpose of this invention patent is to provide a lead compound for the further development of RSV therapeutic drugs.
  • the patented compound has high gelation characteristics, and is extremely difficult to dissolve in water and has poor druggability.
  • the present invention also provides the application of the compound and/or the compound prepared by the preparation method in the preparation of medicine or medicine combination for preventing and/or treating diseases.
  • the present invention also provides a method for preventing and/or treating syncytial virus pneumonia, which comprises administering any of the following items to a subject:
  • the present invention firstly provides a compound represented by formula I, the pharmaceutically acceptable salt, solvate, chelate or non-covalent complex formed by the compound, the prodrug based on the compound, or the above-mentioned Any mixture of forms.
  • the present invention also provides a pharmaceutical combination comprising the compound according to the present invention, and the use of the pharmaceutical combination of the compound of the present invention for preparing a medicine for treating diseases.
  • the preparation method of the present invention comprises: adopting the solid-phase polypeptide synthesis method to prepare the peptide resin, and the peptide resin is subjected to acid hydrolysis to obtain a crude product, and finally the crude product is purified to obtain a pure product; wherein the step of preparing the peptide resin by the solid-phase polypeptide synthesis method is on the carrier resin
  • the corresponding protected amino acids or fragments in the polypeptide sequence are sequentially inserted into the peptide resin by solid-phase coupling synthesis.
  • the chromatographic filling material for purification is the reverse phase C18 of 10 ⁇ m
  • mobile phase system is 0.1% TFA/water solution-0.1% TFA/acetonitrile solution
  • the chromatographic column flow rate of 77mm * 250mm is 90mL/min (can be Use chromatographic columns of different specifications for purification; according to different specifications of chromatographic columns, adjust the corresponding flow rate), use a gradient system for elution, cycle sample purification, take the crude product solution and load it on the chromatographic column, start the mobile phase elution, After collecting the main peak and evaporating acetonitrile, the concentrated solution of the purified intermediate was obtained;

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Virology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La présente invention concerne le domaine de la synthèse de médicaments. L'invention concerne un inhibiteur de fusion membranaire anti-virus respiratoire syncytial (VRS). L'inhibiteur de fusion membranaire anti-virus syncytial de la présente invention est utilisé pour préparer une composition pharmaceutique pour le traitement de maladies. L'invention concerne également une utilisation de la composition pharmaceutique dans la préparation d'un médicament pour le traitement de la pneumonie à virus syncytial.
PCT/CN2022/133459 2021-11-24 2022-11-22 Inhibiteur de fusion membranure anti-virus syncytial WO2023093708A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN202111403215.4A CN116162136A (zh) 2021-11-24 2021-11-24 一种抗合胞病毒膜融合抑制剂
CN202111403215.4 2021-11-24

Publications (1)

Publication Number Publication Date
WO2023093708A1 true WO2023093708A1 (fr) 2023-06-01

Family

ID=86409954

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2022/133459 WO2023093708A1 (fr) 2021-11-24 2022-11-22 Inhibiteur de fusion membranure anti-virus syncytial

Country Status (2)

Country Link
CN (1) CN116162136A (fr)
WO (1) WO2023093708A1 (fr)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1310626A (zh) * 1998-05-20 2001-08-29 特莱默里斯公司 具有增强药物动力特性的杂合肽
CN1373669A (zh) * 1999-07-09 2002-10-09 特莱默里斯公司 增强了药动学性质的杂合多肽

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1310626A (zh) * 1998-05-20 2001-08-29 特莱默里斯公司 具有增强药物动力特性的杂合肽
CN1373669A (zh) * 1999-07-09 2002-10-09 特莱默里斯公司 增强了药动学性质的杂合多肽

Also Published As

Publication number Publication date
CN116162136A (zh) 2023-05-26

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