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1. WO2021060439 - HETEROBIFUNCTIONAL MONODISPERSED POLYETHYLENE GLYCOL HAVING PEPTIDE LINKER

Publication Number WO/2021/060439
Publication Date 01.04.2021
International Application No. PCT/JP2020/036195
International Filing Date 25.09.2020
IPC
C08G 65/323 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
65Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
02from cyclic ethers by opening of the heterocyclic ring
32Polymers modified by chemical after-treatment
321with inorganic compounds
323containing halogens
C07K 5/06 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
C07K 5/08 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
08Tripeptides
C07K 5/10 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
10Tetrapeptides
C07K 16/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
16Immunoglobulins, e.g. monoclonal or polyclonal antibodies
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
Applicants
  • 日油株式会社 NOF CORPORATION [JP]/[JP]
Inventors
  • 松野 佑紀 MATSUNO, Yuki
  • 吉岡 宏樹 YOSHIOKA, Hiroki
  • 鈴木 輝 SUZUKI, Akira
Agents
  • 高島 一 TAKASHIMA, Hajime
Priority Data
2019-17606626.09.2019JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) HETEROBIFUNCTIONAL MONODISPERSED POLYETHYLENE GLYCOL HAVING PEPTIDE LINKER
(FR) POLYÉTHYLÈNE GLYCOL MONODISPERSÉ HÉTÉROBIFONCTIONNEL AYANT UN LIEUR PEPTIDIQUE
(JA) ペプチドリンカーを有するヘテロ二官能性単分散ポリエチレングリコール
Abstract
(EN)
The present invention addresses the problem of providing: a heterobifunctional monodispersed polyethylene glycol having two adjacent monodispersed polyethylene glycol side chains which can sustainedly release a drug upon the decomposition of a peptide linker by an enzyme in cells and, at the same time, which can effectively block the hydrophobicity of the drug; and an antibody-drug conjugate in which an antibody is conjugated with a drug using the heterobifunctional monodispersed polyethylene glycol. This heterobifunctional monodispersed polyethylene glycol is represented by formula (1). [In formula (1), each symbol is as defined in the description.]
(FR)
La présente invention aborde le problème de la fourniture : d'un polyéthylène glycol monodispersé hétérobifonctionnel ayant deux chaînes latérales adjacentes de polyéthylène glycol monodispersé, qui peut libérer de manière prolongée un médicament lors de la décomposition d'un lieur peptidique par une enzyme dans des cellules et, dans le même temps, qui peut bloquer efficacement l'hydrophobicité du médicament ; et un conjugué anticorps-médicament dans lequel un anticorps est conjugué à un médicament à l'aide du polyéthylène glycol monodispersé hétérobifonctionnel. Le polyéthylène glycol monodispersé hétérobifonctionnel est représenté par la formule (1). [Dans la formule (1), chaque symbole est tel que défini dans la description.]
(JA)
細胞内の酵素によりペプチドリンカーが分解して薬物を徐放し、かつ薬物の疎水性を効果的に遮蔽する近接した二本の単分散ポリエチレングリコール側鎖を有するヘテロ二官能性単分散ポリエチレングリコール、およびこれを用いて抗体と薬物を結合した抗体-薬物複合体を提供すること。式(1)で示される、ヘテロ二官能性単分散ポリエチレングリコール。 (式(1)中、各記号は明細書中で定義した通りである。)
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