IP Library › Granted Patent US 11,759,528
Granted Patent B2
US 11,759,528 · App. 16/213,485 · Granted Sep 19, 2023

Peg linker and ligand drug conjugate

Inventors: Yanping Song (Beijing, CN); Wen Li (Beijing, CN); Jinliang Wang (Beijing, CN); Yan Liu (Beijing, CN); Kun Zheng (Beijing, CN); Meina Lin (Beijing, CN); Zhen Wei (Beijing, CN); Zewang Feng (Beijing, CN); Xuan Zhao (Beijing, CN)
Assignee: JENKEM TECHNOLOGY CO., LTD. (BEIJING)
A61K47/6855A61K31/436A61K31/4745A61K47/10A61K47/34A61K47/60A61K47/6803A61K47/6849A61K47/6883A61P31/00A61P35/00A61P37/02C07C59/125C07C69/708C07C247/04C07C309/65C07D207/452C07D207/46C07K16/2809C07K16/32C08G65/334C08G65/3332C08G65/3344C08G65/33303C08G65/33317C08G65/48C07K2317/94
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Quick Facts
Patent No.
US 11,759,528
App. No.
16/213,485
Granted
Sep 19, 2023
Kind
B2
Abstract

A PEG linker as represented by formula (I), wherein n and m are respectively an integer from 1 to 7, providing the PEG linker with 1 to 49 linking sites. A ligand drug conjugate as represented by formula (II). The conjugate uses the PEG linker to increase a drug loading capacity and drug loading diversity, thereby improving pharmaceutical efficacy. Y1-PEG1-{R 1 -PEG2-{Y4} n } m   (I) TM-{R 2 -PEG1-{R 1 -PEG2-{R 3 -A′-drug} n } m } l   (II)

Claims (4)

1. A ligand drug conjugate or a pharmaceutically acceptable salt thereof

wherein,

the ligand drug conjugate is selected from the group consisting of APEGA-2, APEGA-4, APEGA-5 and APEGA-6, each having the structural formula shown below:

wherein, Val is proline; Iri is irinotecan; h is the same or not the same, and each independently is an integer selected from 1 to 240; TM is a ligand unit, the TM ligand unit is selected from the group consisting of a monoclonal antibody and a polyclonal antibody.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 29, 2022
From: SONG, YANPING; LI, WEN; WANG, JINLIANG; LIU, YAN; ZHENG, KUN; LIN, MEINA; WEI, ZHEN; FENG, ZEWANG; ZHAO, XUAN
To: JENKEM TECHNOLOGY CO., LTD. (BEIJING)
Reel/Frame 060351/0946 →
Priority Claims (1)
CN 201610398765.4 · Jun 7, 2016 · national
Continuity (2)
Continuation PCTCN2016090397 · Jul 19, 2016
Related Publication 20190117790A1 · Apr 25, 2019