Imaging composition and uses thereof

Patent metadata

Field	Value
Publication number	US-9980930-B2
Application number	US-201515518333-A
Country	US
Kind code	B2
Filing date	Oct 16, 2015
Priority date	Oct 16, 2014
Publication date	May 29, 2018
Grant date	May 29, 2018

Abstract

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

First claim

The invention claimed is:

1. A radionuclide complex of a compound of formula (I):

or a pharmaceutically acceptable salt thereof, wherein L is a leaving group selected from azide, halogen, cyanate and OR, wherein R is selected from C 1 to C 10 alkyl, C 1 to C 10 heteroalkyl, C 2 to C 10 alkene, C 2 to C 10 alkyne, and aryl, each of which is optionally substituted.

2. The radionuclide complex of claim 1 , wherein R is C 1 to C 6 alkyl.

3. The radionuclide complex of claim 1 , wherein L is selected from O-p-toluenesulfonate, O-methanesulfonate, O-trifluoromethanesulfonate, O-benzenesulfonate, and O-m-nitrobenzenesulfonate.

4. The radionuclide complex of claim 1 wherein the radionuclide is selected from radioisotopes of zirconium, gallium, lutetium, holmium, scandium, titanium, indium and niobium.

5. The radionuclide complex of claim 4 wherein the radionuclide is a radioisotope of zirconium, gallium or indium.

6. The radionuclide complex of claim 1 further conjugated to a target molecule to form a radionuclide-labelled conjugate.

7. The radionuclide-labelled conjugate of claim 6 , wherein the target molecule is a polypeptide.

8. A method of imaging a patient, the method including:
administering to a patient the radionuclide-labelled conjugate of claim 6 ; and
imaging said patient.

9. The method of claim 8 , wherein the target molecule serves to target the conjugate to a desired site in vivo.

10. The method of claim 9 , wherein the desired site is a tumour.

11. A method of imaging a cell or in vitro biopsy sample, the method including:
administering to a cell or in vitro biopsy sample the radionuclide-labelled conjugate of claim 6 ; and
imaging the cell or in vitro biopsy sample.

12. The radionuclide complex of claim 2 , wherein R is methyl or ethyl.

Assignees

• Univ Melbourne

Inventors

• Donnelly Paul Stephen
• Rudd Stacey Erin
• Williams Spencer John

Classifications

• C07C309/14

  containing amino groups bound to the carbon skeleton · CPC title

• C07D213/89

  with hetero atoms directly attached to the ring nitrogen atom · CPC title

• C07C311/46

  Y being a hydrogen or a carbon atom · CPC title

• C07D413/12

  linked by a chain containing hetero atoms as chain links · CPC title

• A61K51/1051

  the tumor cell being from breast, e.g. the antibody being herceptin · CPC title