US 10,864,279 B2 · Linker-drug and antibody-drug conjugate (ADC) employing the same

Abstract

A linker-drug represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof is provided. In formula (I), C is a conjugator, L is a linker unit, D is a toxin unit, and n is an integer ranging from 1 to 4. The structure of the conjugator is represented by formula (II). In formula (II), X is a leaving group, each of R1 and R2 is independently a single bond or —NH—, and Z is substituted aryl, heteroaryl, linear alkyl, cycloalkyl, heterocycloalkyl, or a combination thereof. The antibody is conjugated to the linker unit through a cysteine residue of the antibody. An antibody-drug conjugate (ADC) employing the above linker-drug is also provided.

Claims16

Dependent claims

A linker-drug represented by formula (IA) or formula (IA′):

wherein C is a conjugating linker;
L is a linker unit;
Do, Dp and Dq are drug units;
and m is an integer of 1;
o is an integer ranging from 1 to 4;
p is an integer ranging from 1 to 4;
and q is an integer ranging from 1 to 4;
wherein the structure of the conjugating linker is represented by formula (IIa), formula (IIb), or formula (IIc):
wherein X is a leaving group,
wherein the wave line of formula (IIa), formula (IIb), or formula (IIc) indicates the covalent attachment site to L.

7 more elements

Dependencies are inferred from the claim text.

Facts

Application

15/830,272Filed 4 Dec 2017 · us provisional application

Priority

16 Dec 2016

Published

US 2018/0169262 A121 Jun 2018

Granted

15 Dec 2020

Term ends

Not estimatedThe source records don’t support an estimate.

Classification13 codes

A61K 47/6889
The modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment: conjugates wherein the antibody being the…
A61K 31/4745
Ortho- or peri-condensed with heterocyclic ring systems: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
A61K 47/64
The modifying agent being a protein, peptide or polyamino acid: drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying…
A61K 47/68031
Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates: the drug being an auristatin

Linker-drug and antibody-drug conjugate (ADC) employing the same

Life of this patent

Linker-drug and antibody-drug conjugate (ADC) employing the same

Life of this patent

Abstract

Claims16