ANTIBODY DRUG CONJUGATES

摘要

Drug conjugates of formula [D-(X)b-(AA)w-(L)-]n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, wherein: A is selected from (II) and (III) R1, R2 and R3 is H, ORa, OCORa, OCO—ORa, alkyl, alkenyl, alkynyl, etc; R3′ is, CORa, COORa, CONRaRb, etc; each of R4 to R10 and R12 is alkyl, alkenyl or alkynyl; R11 is H, CORa, COORa, alkyl, alkenyl or alkynyl, or R11 and R12+N+C atoms to which they are attached may form a heterocyclic group; each of R13 and R14 is H, CORa, COORa, alkyl, alkenyl or alkynyl; each Ra and Rb is H, alkyl, alkenyl, alkynyl, etc.; each dotted line represents an optional additional bond; X is an extending group; AA is an amino acid unit; L is a linker group; w is 0 to 12; b is 0 or 1; A bis a moiety comprising at least one antigen binding site, and n is the ratio of the group [D-(X)b-(AA)w-(L)-] to the moiety comprising at least one antigen binding site and is in the range from 1 to 20, are useful in the treatment of cancer.