US 2021/0275686 A1 · BINDER/ACTIVE AGENT CONJUGATES DIRECTED AGAINST CXCR5, HAVING ENZYMATICALLY CLEAVABLE LINKERS AND IMPROVED ACTIVITY PROFILE

Abstract

The invention relates to a new binder-drug conjugates with improved properties, to active metabolites of said ADCs and to processes for the preparation thereof. The invention particularly relates to antibody-drug conjugates (ADCs) with CXCR5 antibodies and selected KSP inhibitors. The present invention further relates to the use of said conjugates for the treatment and/ore prevention of diseases and to the use of said conjugates for the production of medicaments for the treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases.

Claims23

Dependent claims

Binder/active agent conjugates of general formula (I)

in which
X1 represents N,
X2 represents N and
X3 represents C;
or
X1 represents CH or CF,
X2 represents C and
X3 represents N;
or
X1 represents NH,
X2 represents C and
X3 represents C,
or
X1 represents CH,
X2 represents N and
X3 represents C,
R1 represents hydrogen or methyl,
R2 represents methyl, ethyl, —CH2—CH(CH3)2, —CH2—C(═O)OH or isopropyl,
R3 represents methyl, ethyl, —CH2—CH(CH3)2 or —CH2—C(═O)—NH2,
M represents the group
#—C(═O)—CH(CH3)—NH—C(═O)—(CH2)2-8—C(═O)-### or
#—C(═O)— (CH2)3—C(═O)-###,
n represents a number from 1 to 50,
AK2 represents a binder or a derivative thereof, preferably an antibody or an antigen-binding fragment
# represents the bond to the active agent and
### represents the bond to an N atom of a lysine side chain of the binder,
as well as their salts and solvates thereof and their salts of these solvates.

24 more elements

Dependencies are inferred from the claim text.

Binder/active agent conjugates directed against cxcr5, having enzymatically cleavable linkers and improved activity profile

Life of this patent

Binder/active agent conjugates directed against cxcr5, having enzymatically cleavable linkers and improved activity profile

Life of this patent

Abstract

Claims23