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1. WO2022001710 - INTERMEDIATE FOR PREPARING ANTIBODY-DRUG CONJUGATE (ADC), PREPARATION METHOD THEREFOR, AND USE THEREOF

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Publication Number WO/2022/001710
Publication Date 06.01.2022
International Application No. PCT/CN2021/101061
International Filing Date 18.06.2021
IPC
A61K 47/68 2017.1
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 47/54 2017.1
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
54the modifying agent being an organic compound
A61K 31/337 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
337having four-membered rings, e.g. taxol
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 37/02 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
CPC
A61K 31/337
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
337having four-membered rings, e.g. taxol
A61K 47/54
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
54the modifying agent being an organic compound
A61K 47/545
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
54the modifying agent being an organic compound
545Heterocyclic compounds
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
A61K 47/6803
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
6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
A61K 47/6889
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
6889Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
Applicants
  • 达石药业（广东）有限公司 DARTSBIO PHARMACEUTICALS LTD. [CN]/[CN]
Inventors
  • 王春河 WANG, Chunhe
  • 邵婷 SHAO, Ting
  • 陈田志 CHEN, Tianzhi
  • 王琪 WANG, Qi
  • 陈艺丽 CHEN, Yili
  • 林以均 LIN, Yijun
Agents
  • 北京金信知识产权代理有限公司 KINGSOUND & PARTNERS
Priority Data
202010601915.328.06.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) INTERMEDIATE FOR PREPARING ANTIBODY-DRUG CONJUGATE (ADC), PREPARATION METHOD THEREFOR, AND USE THEREOF
(FR) INTERMÉDIAIRE POUR PRÉPARER UN CONJUGUÉ ANTICORPS-MÉDICAMENT (ADC), SA MÉTHODE DE PRÉPARATION ET SON UTILISATION
(ZH) 用于抗体与药物偶联体(ADC)制备的中间体及其制备方法和应用
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Abstract
(EN) Provided are an intermediate (connexon and load combination) for preparing an antibody-drug conjugate (ADC), a preparation method therefor, and the use thereof. The connexon and load combination has a structure as represented by formula I. Formula I can be used for coupling highly hydrophobic compound loads, such as paclitaxel (PTX'), and a prepared ADC molecule has good hydrophilicity and thermal stability and can achieve a higher drug-to-antibody ratio.
(FR) L'invention concerne un intermédiaire (connexon et combinaison de charge) pour préparer un conjugué anticorps-médicament (ADC), sa méthode de préparation et son utilisation. Le connexon et la combinaison de charge ont une structure telle que représentée par la formule I. La formule I peut être utilisée pour coupler des charges de composés hautement hydrophobes, telles que le paclitaxel (PTX'), et une molécule d'ADC préparée présente une bonne hydrophilie et une bonne stabilité thermique et peut atteindre un rapport médicament/anticorps plus élevé.
(ZH) 一种用于抗体与药物偶联体（ADC）制备的中间体（连接子与载荷组合）及其制备方法和应用，连接子与载荷组合具有式I结构。式I可用于紫杉醇类（PTX'）等不易被偶联的高疏水性化合物载荷的偶联，制备的ADC分子具有良好的亲水性和热稳定性，并且可以达到较高的药物与抗体比例值。
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