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1. WO2020087947 - METHOD FOR MODIFICATION OF POLYPETIDE AND USES

Publication Number WO/2020/087947
Publication Date 07.05.2020
International Application No. PCT/CN2019/092232
International Filing Date 21.06.2019
IPC
C07K 1/107 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
107by chemical modification of precursor peptides
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
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
A61K 47/60 2017.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
59obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
60the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 25/28 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 3/04 2006.01
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
CPC
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
A61K 47/60
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
59obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
60the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
C07K 14/605
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
605Glucagons
Applicants
  • 中南大学湘雅医院 XIANGYA HOSPITAL, CENTRAL SOUTH UNIVERSITY [CN]/[CN]
Inventors
  • 陈永恒 CHEN, Yongheng
  • 周展 ZHOU, Zhan
  • 陈主初 CHEN, Zhuchu
  • 李俊 LI, Jun
Agents
  • 北京品源专利代理有限公司 BEYOND ATTORNEYS AT LAW
Priority Data
201811283889.331.10.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) METHOD FOR MODIFICATION OF POLYPETIDE AND USES
(FR) PROCÉDÉ DE MODIFICATION DE POLYPEPTIDES ET UTILISATIONS
(ZH) 一种多肽的修饰方法及应用
Abstract
(EN)
Provided are a method for the modification of a polypeptide and uses. The method comprises the following steps: (1) introducing an X into the N-terminus of the polypeptide, thereby obtaining X-polypeptide; (2) oxidizing the X into an aldehyde group; (3) adding a reducing agent, and covalently coupling the oxidation product obtained in step (2) with PEG, thereby obtaining a PEG-modified polypeptide, wherein X is threonine or serine. In the present application, a single component of PEG-modified polypeptide is obtained by introducing a threonine or serine into the N-terminus of the polypeptide, and deriving the amino alcohol structure at the ortho-position of the N-terminus of the polypeptide as an aldehyde group by using a high-specificity oxidation method and covalently coupling the aldehyde group with PEG. The method has a strong universality and a wide range of application, and the method for separating the modified polypeptide is simple and convenient, thereby improving the stability and the circulating half-life of the polypeptide.
(FR)
L'invention concerne un procédé de modification d'un polypeptide et des utilisations. Le procédé comporte les étapes suivantes consistant à : (1) introduire un X dans l'extrémité N-terminale d'un polypeptide, un X-polypeptide étant obtenu; (2) réaliser une oxydation du X dans un groupe aldéhyde; (3) ajouter un agent réducteur, et coupler de manière covalente le produit d'oxydation obtenu à l'étape (2) avec du PEG, ce qui permet d'obtenir un polypeptide modifié par PEG, X étant thréonine ou sérine. La présente invention permet d'obtenir un composant unique d'un polypeptide modifié par PEG, l'invention consiste à introduire une thréonine ou une sérine dans l'extrémité N-terminale d'un polypeptide, dériver la structure d'amino-alcool en position ortho de l'extrémité N-terminale du polypeptide en tant que groupe aldéhyde à l'aide d'un procédé d'oxydation à haute spécificité et coupler de manière covalente le groupe aldéhyde avec le PEG. Le procédé a une grande universalité et une large gamme d'utilisation, le procédé de séparation du polypeptide modifié étant simple et pratique, permettant ainsi d'améliorer la stabilité et la demi-vie en circulation du polypeptide.
(ZH)
本申请提供了一种多肽的修饰方法及应用,所述方法包括以下步骤:(1)向多肽的N端引入X,获得X-多肽;(2)将所述X氧化为醛基;(3)加入还原剂,将步骤(2)获得的氧化产物与PEG进行共价偶联,得到PEG修饰的多肽;其中,所述X为苏氨酸或丝氨酸。本申请向多肽的N端引入一个苏氨酸或一个丝氨酸,并采用高度特异性的氧化方法将多肽N端的临位氨基醇结构衍生为醛基,与PEG共价偶联后得到成分单一的PEG修饰多肽,方法通用性强,应用范围广,修饰后的多肽分离方法简便,提高了多肽的稳定性和循环半衰期。
Also published as
Latest bibliographic data on file with the International Bureau