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1. WO2020181687 - PREPARATION METHOD FOR AND INTERMEDIATE OF DRUG-LINKER FOR ANTIBODY DRUG CONJUGATE MC-MMAF

Publication Number WO/2020/181687
Publication Date 17.09.2020
International Application No. PCT/CN2019/092950
International Filing Date 26.06.2019
IPC
C07K 5/062 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
062the side chain of the first amino acid being acyclic, e.g. Gly, Ala
C07K 5/027 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
02containing at least one abnormal peptide link
027in which at least a gamma-amino acid is involved, e.g. statine
C07K 1/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
06using protecting groups or activating agents
A61K 47/68 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
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/65 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
62the modifying agent being a protein, peptide or polyamino acid
65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
CPC
A61K 47/65
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
62the modifying agent being a protein, peptide or polyamino acid
65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
A61K 47/68
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
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 1/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
06using protecting groups or activating agents
Applicants
  • 联宁(苏州)生物制药有限公司 LEVENA BIOPHARMA CO., LTD. [CN]/[CN]
Inventors
  • 许喆 XU, Zhe
  • 李海泓 LI, Haihong
  • 郭茂君 GUO, Maojun
  • 李辉 LI, Hui
Agents
  • 苏州瑞光知识产权代理事务所(普通合伙) SUZHOU RUNSUN INTELLECTUAL PROPERTY AGENCY
Priority Data
201910178142.X08.03.2019CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PREPARATION METHOD FOR AND INTERMEDIATE OF DRUG-LINKER FOR ANTIBODY DRUG CONJUGATE MC-MMAF
(FR) PROCÉDÉ DE PRÉPARATION ET INTERMÉDIAIRE DE MÉDICAMENT-LIEUR POUR UN CONJUGUÉ ANTICORPS-MÉDICAMENT MC-MMAF
(ZH) 一种用于抗体药物偶联物的药物-连接子MC-MMAF的制备方法及其中间体
Abstract
(EN)
A preparation method for and an intermediate of a drug-linker for an antibody drug conjugate MC-MMAF. The reaction activity of the N-terminus is improved, so that the occurrence of a racemic reaction is effectively controlled. The toxin MMAF is not directly used and a fragment peptide having low toxicity is used, so that an operation difficulty in mass production is reduced. No reverse-phase preparation is required so that the operations are simple.
(FR)
L'invention concerne un procédé de préparation et un intermédiaire d'un médicament-lieur pour un conjugué anticorps-médicament MC-MMAF. L'activité de réaction de l'extrémité N-terminale est améliorée, de telle sorte que l'apparition d'une réaction racémique est contrôlée de manière efficace. La toxine MMAF n'est pas directement utilisée et un peptide fragment ayant une faible toxicité est utilisé, ce qui permet de réduire la difficulté de fonctionnement en production de masse. L'invention ne nécessite pas de préparation en phase inverse de sorte que les fonctionnements sont simples.
(ZH)
一种用于抗体偶联药物的药物-连接子MC-MMAF的制备方法及其中间体。提高了N端的反应活性,从而有效的控制了消旋反应的发生;不直接使用毒素MMAF,而采用毒性较低的片段肽,降低了大量生产时的操作难度;无需反相制备,操作简便。
Also published as
Latest bibliographic data on file with the International Bureau