Compounds for Positron Emission Tomography
Abstract
Described herein are compounds, compositions, and methods for diagnosing and/or monitoring pathogenic disease using positron emission tomography. Also described are conjugates of the formula B-L-P, wherein B is a radical of a targeting agent selected from vitamin receptor binding ligands (such as folate), PSMA binding ligands, or PSMA inhibitors; L is a divalent linker comprising aspartic acid, lysine, or arginine, and P is a radical of an imaging agent or radiotherapy agent, such as a radionuclide or radionuclide containing group, or a radical of a compound capable of binding a radionuclide, such as a metal chelating group.
Claims
exact text as granted — not AI-modified1 . A conjugate of the formula
B-L-P
or a pharmaceutically acceptable salt thereof, wherein B is a radical of a targeting agent selected from vitamin receptor binding ligands, PSMA binding ligands, and PSMA inhibitors, L is a divalent linker, and P is a radical comprising a formula chosen from the group consisting of:
2 . The conjugate of claim 1 comprising folate-Asp.
3 . The conjugate of claim 1 comprising folate-Arg.
4 . The conjugate of claim 1 , wherein the divalent linker L comprises a polypeptide comprising phenylalanine, lysine, arginine, or aspartic acid, or a combination thereof.
5 . The conjugate of claim 1 wherein the divalent linker L does not include a diradical of the formula *NH—(CH 2 ) 2 —NH*.
6 . The conjugate of claim 1 , wherein P comprises:
or a derivative thereof comprising a chelated metal.
7 . The conjugate of claim 1 comprising folate-PEG.
8 . The conjugate of claim 1 , wherein P comprises:
or a derivative thereof comprising a chelated metal.
9 . The conjugate of claim 1 , wherein P comprises:
or a derivative thereof comprising a chelated metal.
10 . The conjugate of claim 1 wherein the targeting agent is a radical of a PSMA binding ligand or PSMA inhibitor.
11 . The conjugate of claim 10 comprising the formula
where n is an integer selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10; or
where n is an integer selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10; or
where W is O or S.
12 . The conjugate of claim 10 wherein the linker comprises a polypeptide comprising phenylalanine, lysine, arginine, or aspartic acid, or a combination thereof.
13 . The conjugate of claim 1 , wherein P comprises:
or a derivative thereof comprising a chelated metal.
14 . The conjugate of claim 10 comprising the formula
where n is an integer selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.
15 . The conjugate of claim 10 wherein the divalent linker L comprises the formula
16 . The conjugate of claim 10 wherein the divalent linker L comprises the formula
17 . The conjugate of claim 1 , wherein P comprises:
or a derivative thereof comprising a chelated metal.
18 . The conjugate of claim 1 , further comprising a positron-emitting radionuclide or radionuclide containing group.
19 . The conjugate of claim 18 wherein the radionuclide is a radiotherapy agent.
20 . The conjugate of claim 18 , wherein the positron-emitting radionuclide or radionuclide containing group is selected from the group consisting of 89 Zr, 45 Ti, 51 Mn, 64 Cu, 61 Cu, 63 Zn, 82 Rb, 68 Ga, 66 Ga, 11 C, 13 N, 15 O, 124 I, 34 Cl, 18 F, and 19 F.Join the waitlist — get patent alerts
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