Patent ID: 9138495
Filing Date: 2015-09-22
Classification: A61K,A61P

Abstract:
1. A bifunctional compound precursor, a bifunctional compound or a bifunctional molecule, wherein: (a) the bifunctional compound precursor is represented by the formula: or salts thereof; wherein one of X and Y is C═O and the other is NR; provided that if one of X and Y is C═O and the other is NR, then m is selected from 0 to 6, and p is selected from 1 to 6; wherein R 1 is a chelating group capable of chelating a radionuclide and is selected from: wherein R, R 2 , R 3 and R 4 are independently hydrogen or an optionally substituted C 1-7 alkyl group; B is a linker group for linking the chelating group to the reactive group, and is represented by the formula: wherein each Q is independently selected from a group consisting of —NR 5 —, —C(O)NR 5 —, —C(O)O—, —NR 5 C(O)NR 5 —, —NR 5 C(S)NR 5 — and —O—, each R 5 is independently hydrogen or an optionally substituted C 1-7 alkyl group, each q and s are independently selected from 0 to 6 and each r is independently selected from 1 to 6; A is a reactive group for coupling to a biological moiety, a targeting group, a protein, a polypeptide or a delivery vehicle; (b) the bifunctional compound is represented by the formula: or salts thereof; wherein one of X and Y is C═O and the other is NR; provided that if one of X and Y is C═O and the other is NR, then m is selected from 0 to 6, and p is selected from 1 to 6; wherein R 1 is a chelating group capable of chelating a radionuclide and is selected from: wherein R, R 2 , R 3 and R 4 are independently hydrogen or an optionally substituted C 1-7 alkyl group; B is a linker group for linking the chelating group to the reactive group, and is represented by the formula: wherein each Q is independently selected from a group consisting of —NR 5 —, —C(O)NR 5 —, —C(O)O—, —NR 5 C(O)NR 5 —, —NR 5 C(S)NR 5 — and —O—, each R 5 is independently hydrogen or an optionally substituted C 1-7 alkyl group, each q and s are independently selected from 0 to 6 and each r is independently selected from 1 to 6; A* is a reacted reactive group that is coupled to T, T being a targeting group capable of binding to a target of interest in a subject; or (c) the bifunctional molecule comprises a bifunctional compound and a radionuclide bound through a chelating group of the bifunctional compound, wherein the bifunctional compound of the bifunctional molecule is represented by the formula: or salts thereof; wherein one of X and Y is C═O and the other is NR; provided that if one of X and Y is C═O and the other is NR, then m is selected from 0 to 6, and p is selected from 1 to 6; wherein R 1 is a chelating group capable of chelating a radionuclide and is selected from: wherein R, R 2 , R 3 and R 4 are independently hydrogen or an optionally substituted C 1-7 alkyl group; B is a linker group for linking the chelating group to the reactive group, and is represented by the formula: wherein each Q is independently selected from a group consisting of —NR 5 —, —C(O)NR 5 —, —C(O)O—, —NR 5 C(O)NR 5 —, —NR 5 C(S)NR 5 — and —O—, each R 5 is independently hydrogen or an optionally substituted C 1-7 alkyl group, each q and s are independently selected from 0 to 6 and each r is independently selected from 1 to 6; A* is a reacted reactive group that is coupled to T, T being a targeting group capable of binding to a target of interest in a subject.