US 2020/0046842 A1 · MULTI-DRUG-LOADING-SITE, HIGH DRUG-LOADING CAPACITY LIGAND-DRUG CONJUGATE

Abstract

The present invention provides a multi-drug-loading site and high drug-loading capacity ligand-drug conjugate. The ligand-drug conjugate has a structure of general formula (I). The ligand-drug conjugate has the characteristics of high loading capacity, high drug efficacy, low toxicity, and low risks. The ligand-drug conjugate can be used particularly to connect to a low toxicity chemical molecule, thereby extending a therapeutic window. Furthermore, the present invention provides an antibody-drug conjugate molecule. The antibody-drug conjugate molecule has the characteristics of multiple drug-loading ability and high drug-loading capacity, such that the antibody-drug conjugate can carry a large amount of a low toxicity chemical molecule and achieve a therapeutic effect without depending on antibody targeting or high toxicity chemicals. TM-{R2-PEG1-[R1-PEG2-(R3-A′-D)n]m}l (I

Claims20

Dependent claims

A ligand drug conjugate, having a structure represented by general formula I:

TM-{R2-PEG1-[R1-PEG2-(R3-A′-D)n]m}l (I)
wherein:
TM is a ligand unit;
PEG1 and PEG2 are the same or different polyethylene glycol residues;
l is an integer from 11 to 500;
m is an integer from 1 to 7;
n is an integer from 1 to 7;
A′ is a spacer which is optionally present;
R1 is a linking unit linking PEG1 and PEG2;
R2 is a ligand unit linking the ligand unit and PEG1;
R3 is a linking unit linking PEG2 and spacer A′ or a drug;
and
D is a drug,
or a pharmaceutically acceptable salt thereof.

11 more elements

Dependencies are inferred from the claim text.

Facts

Application

16/588,010Filed 30 Sep 2019

Priority

CN 201710197518.229 Mar 2017

Published

13 Feb 2020

Term ends

Not estimatedThe source records don’t support an estimate.

Classification21 codes

A61K 31/436
Ortho- or peri-condensed with heterocyclic ring systems: the heterocyclic ring system containing a six-membered ring having oxygen as a ring…
A61K 47/60
Obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes: the organic…
A61K 47/65
The modifying agent being a protein, peptide or polyamino acid: peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
A61K 47/68037
Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates: the drug being a camptothecin [CPT] or derivatives

Multi-drug-loading-site, high drug-loading capacity ligand-drug conjugate

Life of this patent

Multi-drug-loading-site, high drug-loading capacity ligand-drug conjugate

Life of this patent

Abstract

Claims20