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1. WO2020134717 - GLUCAGON ANALOGUE, PREPARATION METHOD THEREFOR, AND USE THEREOF

Publication Number WO/2020/134717
Publication Date 02.07.2020
International Application No. PCT/CN2019/119391
International Filing Date 19.11.2019
IPC
C07K 14/605 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
605Glucagons
C07K 19/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
19Hybrid peptides
A61K 38/26 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
26Glucagons
A61P 3/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 38/26
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
26Glucagons
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 3/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
A61P 3/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
Applicants
  • 杭州和泽医药科技有限公司 HANGZHOU HEZE PHARMACEUTICAL TECHNOLOGY CO., LTD. [CN]/[CN]
  • 浙江道尔生物科技有限公司 ZHEJIANG DOER BIOLOGICS CORPORATION [CN]/[CN]
Inventors
  • 黄岩山 HUANG, Yanshan
Agents
  • 上海光华专利事务所(普通合伙) J.Z.M.C. PATENT AND TRADEMARK LAW OFFICE (GENERAL PARTNERSHIP)
Priority Data
201811584730.524.12.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) GLUCAGON ANALOGUE, PREPARATION METHOD THEREFOR, AND USE THEREOF
(FR) ANALOGUE DE GLUCAGON, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 一种胰高血糖素类似物及其制备方法和用途
Abstract
(EN)
A glucagon analogue, a preparation method therefor, and a use thereof. Provided is a glucagon analogue, comprising a glucagon-like polypeptide fragment with a long-acting carrier cross-linked thereon. The polypeptide chain in the glucagon analogue has only 2-3 amino acids mutated on the basis of a natural glucagon sequence, and has an extremely low risk of immunogenicity. Furthermore, introduction of a C-terminal sequence of the marketed drug Exenatide (trade name Bydureon) on this basis increases safety. In addition, the glucagon analogue has extremely high GLP-1R and GCGR agonistic activity, and the glucagon analogue has significant changes in in vitro activity before and after cross-linking of a fatty acid.
(FR)
L'invention concerne un analogue du glucagon, son procédé de préparation et son utilisation. L'invention concerne un analogue du glucagon, comprenant un fragment polypeptidique de type glucagon ayant un support à action prolongée réticulé sur celui-ci. La chaîne polypeptidique dans l'analogue du glucagon ne contient que 2 à 3 acides aminés mutés sur la base d'une séquence de glucagon naturel, et présente un risque d'immunogénicité extrêmement faible. En outre, l'introduction d'une séquence à extrémité C-terminale du médicament commercialisé exénatide (nom commercial "Bydureon") sur cette base augmente la sécurité. De plus, l'analogue de glucagon a une activité agoniste de GLP-1R et GCGR extrêmement élevée, et l'analogue de glucagon a des changements significatifs d'activité in vitro avant et après réticulation d'un acide gras.
(ZH)
一种胰高血糖素类似物及其制备方法和用途,提供一种胰高血糖素类似物,包括类胰高血糖素多肽片段,所述类胰高血糖素多肽片段上交联有长效载体。所述胰高血糖素类似物中的多肽链在天然Glucagon序列的基础上只突变了2-3个氨基酸,免疫原性风险极低,另外在此基础上引入已上市的药物Exenatide(商品名Bydureon)的C末端序列,安全性更高。此外,所述胰高血糖素类似物具有极高的GLP-1R及GCGR激动活性,胰高血糖素类似物在脂肪酸交联前后,体外活性更是具有显著的变化。
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