Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof

摘要

Disclosed is a compound of the formula T ( L C)m, wherein: T is a transportophore; L is a bond or a linker having a molecular weight up to 240 dalton; C is a non-antibiotic therapeutic agent; and m is 1, 2, 3, 4, 5, 6, 7 or 8; in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2, wherein T ( L C)m is of the formula (I): wherein X is selected from N(R7)-CH2, CH2-N(R7), C(=O), C(=NOR8), CH(OR9), CH(NR10R11), C(=NR12), OC(=O) and C(=O)O; and the remaining substituents are as defined in the specification. Also disclosed is the use of the compounds in the manufacture of medicaments for the treatment of diseases commensurate with the known uses of the therapeutic agents.