Bifunctional linker
AssigneeImmunomedics, Inc.
InventorBoby M. Sundoro
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AssigneeImmunomedics, Inc.
InventorBoby M. Sundoro
Estimating the term…
A selective bifunctional sequential linker has the formula Y.dbd.C.dbd.N--Q--A--C(O)--Z wherein Q is a homoaromatic or heteroaromatic ring system; A is a single bond or an unsubstituted or substituted divalent C.sub.1-30 bridging group; Y is O or S; and Z is Cl, Br, I, N.sub.3, N-succinimidyloxy, imidazolyl, 1-benzotriazolyloxy, OAr where Ar is an electron-deficient activating aryl group, or OC(O)R where R is --A--Q--N.dbd.C.dbd.Y or C.sub.4-20 tertiary-alkyl. A method for activating an amine function towards reaction with a second amine involves reacting the amine with the foregoing linker. The resultant isocyanate or isothiocyanate derivative can then be reacted with a second amine to form a urea or thiourea conjugate. The linker is useful for producing conjugates of ligands with amine-containing polymers and/or proteins, especially for forming antibody conjugates with chelators, drugs, enzymes, detectable labels and the like.
A selective bifunctional sequential linker having the formula
A method for activating a first amine-containing compound having a primary or secondary amine function thereon towards reaction with a second amine-containing compound having a primary or secondary amine function thereon, comprising the step of contacting said first amine-containing compound with at least a stoichiometric equivalent of a selective bifunctional sequential linker having the formula
A derivative of a primary or secondary amine-containing ligand, joined at the amine nitrogen, and having the formula
A conjugate of a first primary or secondary amine-containing ligand and a second primary or secondary amine-containing ligand, each joined at the amine nitrogen, and having the formula
Dependencies are inferred from the claim text.