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WO2019037393A1 - Composé polypeptidique ayant une affinité élevée pour le récepteur glp-1, son procédé de préparation et son utilisation - Google Patents

Composé polypeptidique ayant une affinité élevée pour le récepteur glp-1, son procédé de préparation et son utilisation Download PDF

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Publication number
WO2019037393A1
WO2019037393A1 PCT/CN2018/075186 CN2018075186W WO2019037393A1 WO 2019037393 A1 WO2019037393 A1 WO 2019037393A1 CN 2018075186 W CN2018075186 W CN 2018075186W WO 2019037393 A1 WO2019037393 A1 WO 2019037393A1
Authority
WO
WIPO (PCT)
Prior art keywords
glp
evans blue
group
receptor
derivative
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/CN2018/075186
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English (en)
Chinese (zh)
Inventor
陈小元
刘熠
郎立新
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shanghai Theranostics Biotechnology Co Ltd
Original Assignee
Shanghai Theranostics Biotechnology 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 Shanghai Theranostics Biotechnology Co Ltd filed Critical Shanghai Theranostics Biotechnology Co Ltd
Publication of WO2019037393A1 publication Critical patent/WO2019037393A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/57563—Vasoactive intestinal peptide [VIP]; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Definitions

  • Evans Blue also known as Evans Blue, binds to albumin in vitro and in vivo to form EB-albumin complexes, effectively increasing the in vivo half-life of EB molecules.
  • EB-NH 2 amino-functionalized EB molecule
  • the molecules with different functions are covalently modified, for example, the drug molecule, NOTA, DOTA, etc. are modified on the EB, PET imaging and treatment for tumors and lymph nodes.
  • the separation of unreacted material from the lyophilized mixture described in step (3) can be removed by a typical dialysis method, for example, by dissolving the lyophilized mixture in a suitable buffer for dialysis.
  • a suitable buffer for dialysis There is no particular limitation on the buffer.
  • PBS phosphate buffer
  • the selected buffer should match the reaction conditions of Evans blue, depending on the functional group of Evans blue (maleic anhydride requires pH6) .5-7.5; pyridyldithiol or iodoacetyl requires pH alkaline, 7.0-8.5).
  • the reaction system can be isolated and purified using size exclusion chromatography or reversed-phase high performance liquid chromatography.
  • Figure 1 is a graph showing the purity of maleic dimethylenediamine prepared in the step a of Example 1;
  • Figure 3 is a purity diagram of the maleimide Evans blue prepared in the step b of Example 1.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Endocrinology (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Zoology (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Vascular Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La présente invention concerne un composé polypeptidique ayant une affinité élevée pour les récepteurs de GLP -1, la structure moléculaire correspondante étant telle que représentée par la formule suivante (I), R représentant un bleu d'Evans ou un groupe dérivé de celui-ci. Le composé polypeptidique selon la présente invention présente les avantages d'une structure stable, d'une préparation simple, d'un effet thérapeutique significatif, d'une efficacité médicamenteuse à long terme, d'un stockage pratique, etc. La présente invention concerne en outre un procédé de préparation du composé polypeptidique et son utilisation dans la préparation d'un médicament pour le diagnostic, la prévention ou le traitement de maladies associées à la voie du récepteur GLP-1/GLP-1.
PCT/CN2018/075186 2017-08-25 2018-02-03 Composé polypeptidique ayant une affinité élevée pour le récepteur glp-1, son procédé de préparation et son utilisation Ceased WO2019037393A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201710743049.XA CN107365375B (zh) 2017-08-25 2017-08-25 一种对glp-1受体具有高亲和性的多肽化合物及其制备方法和应用
CN201710743049.X 2017-08-25

Publications (1)

Publication Number Publication Date
WO2019037393A1 true WO2019037393A1 (fr) 2019-02-28

Family

ID=60312456

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2018/075186 Ceased WO2019037393A1 (fr) 2017-08-25 2018-02-03 Composé polypeptidique ayant une affinité élevée pour le récepteur glp-1, son procédé de préparation et son utilisation

Country Status (2)

Country Link
CN (1) CN107365375B (fr)
WO (1) WO2019037393A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107365375B (zh) * 2017-08-25 2019-03-01 莎穆(上海)生物科技有限公司 一种对glp-1受体具有高亲和性的多肽化合物及其制备方法和应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000073331A2 (fr) * 1999-06-01 2000-12-07 Amylin Pharmaceuticals, Inc. Utilisation d'exendines et de leurs agonistes pour le traitement du diabete sucre gestationnel
CN104650217A (zh) * 2015-01-26 2015-05-27 汇佳生物科技（上海）有限公司 伊文氏蓝或其衍生物修饰的Exendin-4及其制备方法和应用
CN107365375A (zh) * 2017-08-25 2017-11-21 莎穆(上海)生物科技有限公司 一种对glp‑1受体具有高亲和性的多肽化合物及其制备方法和应用

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000073331A2 (fr) * 1999-06-01 2000-12-07 Amylin Pharmaceuticals, Inc. Utilisation d'exendines et de leurs agonistes pour le traitement du diabete sucre gestationnel
CN104650217A (zh) * 2015-01-26 2015-05-27 汇佳生物科技（上海）有限公司 伊文氏蓝或其衍生物修饰的Exendin-4及其制备方法和应用
CN107365375A (zh) * 2017-08-25 2017-11-21 莎穆(上海)生物科技有限公司 一种对glp‑1受体具有高亲和性的多肽化合物及其制备方法和应用

Also Published As

Publication number Publication date
CN107365375B (zh) 2019-03-01
CN107365375A (zh) 2017-11-21

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