Maytansinoid Derivatives

摘要

Disclosed herein are maytansinoid drug linker derivatives which can be linked to a antigen binding unit (Abu), and maytansinoid drugs linked with an antigen binding unit (Drug-Linker-Antigen binding Unit: D-L-Abu), for targeted delivery to disease tissues. D-L-Abu, D-L-Abu derivatives, and methods relating to the use of such drug conjugates to treat antigen positive cells in cancers and immunological disorders are provided.

主权项

1. A compound selected from the group consisting of: or a salt thereof, wherein
X is hydrogen or halo;Y is selected from the group consisting of hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, and —C(═O)R5;R1 is selected from the group consisting of hydrogen, —OH, —OC(═O)R5 and —OR5;R2 is hydrogen or C1-C6 alkyl;R3 is methyl, —CH2OH, or —CH2C(═O)R6;R4 is —OH or —SH;R5 is C1-C6 alkyl or benzyl;R6 is C1-C6 alkyl, phenyl or benzyl;R7 is hydrogen, C1-C6 alkyl or an amino acid side chain;R8 is hydrogen or C1-6 alkyl;AA is an amino acid.