| 主权项 |
1. A maytansine-containing conjugate of the general formula:
(((Dq-Lk1)m-P)p-Lk2-Lk3)n-Ab (I) in which D represents a maytansine moiety; q represents an integer from 1 to 10; Lk1 represents a linker; m represents an integer from 1 to 10; P represents a bond or a z-valent group —P1—NH— where z is from 2 to 11 and P1 is a group containing at least one ethylene unit —CH2—CH2— or ethylene glycol unit —O—CH2—CH2—; p represents an integer from 1 to 10; Lk2 represents a bond or a y-valent linker where y is from 2 to 11 and which consists of from 1 to 9 aspartate and/or glutamate residues; Lk3 represents a linker of the general formula:
—CO-Ph-X—Y— (II) in which Ph is an optionally substituted phenyl group; X represents a CO group or a CH.OH group; and Y represents a group of formula: in which each of A and B represents a C1-4alkylene or alkenylene group; Ab represents a binding protein or peptide capable of binding to a binding partner on a target, said binding protein or peptide being bonded to Lk3 via two sulfur atoms derived from a disulfide bond in the binding protein or peptide; and n represents an integer from 1 to s where s is the number of disulfide bonds present in the binding protein or peptide prior to conjugation to Lk3; the meanings of m, n, p, q, y and z being chosen such that the conjugate contains from 1 to 10 D groups. |
