EPSILON-POLY-L-LYSINE-BASED DRUG CONJUGATE, INTERMEDIATE THEREOF, AND APPLICATION THEREOF

Title:

EPSILON-POLY-L-LYSINE-BASED DRUG CONJUGATE, INTERMEDIATE THEREOF, AND APPLICATION THEREOF

Document Type and Number:

WIPO Patent Application WO/2023/078464

Kind Code:

A1

Abstract:

Disclosed are an epsilon-poly-L-lysine-based drug conjugate, an intermediate thereof, and an application thereof. The present invention provides an epsilon-poly-L-lysine derivative-drug conjugate that has a controllable group coupling number and controllable group coupling sites and that is represented by formula (I). The drug conjugate of the present invention has one or more among the effect advantages of low renal clearance rate, low liver and spleen clearance rate, long plasma half-life, rapid accumulation of effective drug concentration in lesions, and a better therapeutic effect.

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Inventors:

ZHANG FUYAO (CN)
WAN JIAXUN (CN)
HUANG LEI (CN)

Application Number:

PCT/CN2022/130704

Publication Date:

May 11, 2023

Filing Date:

November 08, 2022

Export Citation:

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Assignee:

SHANGHAI BEST LINK BIOSCIENCE LLC (CN)

International Classes:

A61K47/64; A61K45/00; A61K47/54; A61K47/65; A61P35/00; A61P35/02; C08G69/48

Foreign References:

CN110520161A

2019-11-29

Other References:

MEHTA DHARMINI, LEONG NATHANIA, MCLEOD VICTORIA M., KELLY BRIAN D., PATHAK RASHMI, OWEN DAVID J., PORTER CHRISTOPHER J.H., KAMINSK: "Reducing Dendrimer Generation and PEG Chain Length Increases Drug Release and Promotes Anticancer Activity of PEGylated Polylysine Dendrimers Conjugated with Doxorubicin via a Cathepsin-Cleavable Peptide Linker", MOLECULAR PHARMACEUTICS, vol. 15, no. 10, 1 October 2018 (2018-10-01), US , pages 4568 - 4576, XP055795993, ISSN: 1543-8384, DOI: 10.1021/acs.molpharmaceut.8b00581
LISA M. KAMINSKAS, BOYD BEN J., KARELLAS PETER, KRIPPNER GUY Y., LESSENE ROMINA, KELLY BRIAN, PORTER CHRISTOPHER J. H.: "The Impact of Molecular Weight and PEG Chain Length on the Systemic Pharmacokinetics of PEGylated Poly l-Lysine Dendrimers", MOLECULAR PHARMACEUTICS, vol. 5, no. 3, 1 June 2008 (2008-06-01), pages 449 - 463, XP055159689, ISSN: 1543-8384, DOI: 10.1021/mp7001208

Attorney, Agent or Firm:

SHANGHAI BESHINING LAW OFFICE (CN)

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