| abstract |
Disclosed is a bridge linker compound of Formula (I) for conjugating a drug to a cell-binding molecule: (see formula I) wherein: - represents an optional single bond; - represents either a single bond or a double bond; provided that when - represents a single bond, both U and U' are not H; and when = represents a double bond, either U or U' can be H, but are not H at the same time; and wherein the component , ( see above formula) can be a 2,3-disubstituted succinic group, or a 2-monosubstituted or 2,3-disubstituted fumaric or maleic group for conjugation of two or more compounds/cytotoxic agents per linker to the cell-binding molecule through bridge linking pairs of thiols on the cell-binding molecule. Also disclosed are methods of making such linkers, of using such linkers in making homogeneous conjugates, and of application of the conjugates in the treatment of cancers, infections and autoimmune disorders. |