| 主权项 |
1. An antibody-drug conjugate represented by Formula (I)
Ab-(L-D)p, Ab is an antibody; L is a peptidomimetic linker represented by the following formula
-Str-(PM)-Sp- wherein Str is a stretcher unit covalently attached to Ab; Sp is a bond or spacer unit covalently attached to a drug moiety; PM is a non-peptide chemical moiety selected from the group consisting of: W is —NH-heterocycloalkyl- or heterocycloalkyl; Y is heteroaryl, aryl, —C(O)C1-C6alkylene, C1-C6alkenyl, C1-C6alkylene or —C1-C6alkylene-NH—; each R1 is independently C1-C10alkyl, C1-C10alkenyl, (C1-C10alkyl)NHC(NH)NH2 or (C1-C10alkyl)NHC(O)NH2; R3 and R2 are each independently H, C1-C10alkyl, C1-C10alkenyl, arylalkyl or heteroarylalkyl, or R3 and R2 together may form a C3-C7cycloalkyl; R4 and R5 are each independently C1-C10alkyl, C1-C10alkenyl, arylalkyl, heteroarylalkyl, (C1-C10alkyl)OCH2—, or R4 and R5 together may form a C3-C7cycloalkyl ring; p is an integer from 1 to 8; D is a drug moiety of Formula (Ia) or (Ib) represented by the following structures: wherein R11 is a hydrogen atom, hydroxy or methoxy group, and R22 is a C1-C5 alkoxy group, or a pharmaceutically acceptable salt thereof. |
