Compounds for Positron Emission Tomography

Patent metadata

Field	Value
Publication number	US-2016287731-A1
Application number	US-201415035936-A
Country	US
Kind code	A1
Filing date	Nov 13, 2014
Priority date	Nov 14, 2013
Publication date	Oct 6, 2016
Grant date	—

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.

First claim

1 - 19 . (canceled)

20 . 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 of an imaging agent or radiotherapy agent, such as a radionuclide or radionuclide containing group, or a precursor thereof, or a radical of a compound capable of binding a radionuclide or radionuclide containing group, such as a metal chelating group.

21 . The conjugate of claim 20 comprising folate-Asp,

22 . The conjugate of claim 20 comprising folate-Arg.

23 . The conjugate of claim 20 wherein the linker comprises a polypeptide comprising lysine, arginine, or aspartic acid, or a combination thereof.

24 . The conjugate of claim 20 wherein the linker does not include a diradical of the formula NH—(CH 2 ) 2 —NH,

25 . The conjugate of claim 20 comprising the formula

or a derivative thereof comprising a chelated metal.

26 . The conjugate of claim 20 comprising folate-PEG.

27 . The conjugate of claim 26 comprising the formula

or a derivative thereof comprising a chelated metal.

28 . The conjugate of claim 26 comprising the formula

or a derivative thereof comprising a chelated metal.

29 . The conjugate of claim 20 wherein the targeting agent is a radical of a PSMA binding ligand or PSMA inhibitor.

30 . The conjugate of claim 29 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.

31 . The conjugate of claim 29 wherein the linker comprises a polypeptide comprising phenylalanine, lysine, arginine, or aspartic acid, or a combination thereof.

32 . The conjugate of claim 29 comprising the formula

or a derivative thereof comprising a chelated metal.

33 . The conjugate of claim 29 comprising the formula

where n is an integer selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

34 . The conjugate of claim 29 wherein the linker comprises the formula

35 . The conjugate of claim 29 wherein the linker comprises the formula

36 . The conjugate of claim 33 comprising the formula

or a derivative thereof comprising a chelated metal.

37 . The conjugate of claim 20 , wherein the radionuclide is a positron-emitting radionuclide.

38 . The conjugate of claim 37 , wherein the positron-emitting radionuclide 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.

39 . The conjugate of claim 20 wherein the radionuclide is a radiotherapy agent.

Assignees

• Endocyte Inc
• Purdue Research Foundation

Inventors

• Vlahov Iontcho R
• Leamon Christopher P
• Low Philip S
• Parham Garth L
• Chen Qingshou

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61P13/08

  of the prostate · CPC title

• G01N2800/00

  Detection or diagnosis of diseases · CPC title

• A61K51/0459

  having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine · CPC title

• A61K51/0497 Primary

  conjugates with a carrier being an organic compounds · CPC title