Triazacyclononane-based phosphinate ligand and its use for molecular imaging

Patent metadata

Field	Value
Publication number	US-9260483-B2
Application number	US-201213978859-A
Country	US
Kind code	B2
Filing date	Jan 5, 2012
Priority date	Jan 10, 2011
Publication date	Feb 16, 2016
Grant date	Feb 16, 2016

Abstract

The present invention relates to the field of molecular imaging, i.e. nuclear and fluorescent imaging using metal ion radionuclides in combination with chelates highly functionalized with peptidic, nonpeptidic or protein ligands or additional signalling moieties.

First claim

The invention claimed is:

1. A chelate ligand having one of the following formulae

2. A chelate comprising at least one chelate ligand as defined in claim 1 and at least one metal or radiometal.

3. The chelate according to claim 2 , wherein the at least one metal or radiometal is selected from the group consisting of La 3+ , Ce 3+ , Pr 3+ , Nd 3+ , Sm 3+ , Eu 2+ , Gd 3+ , Tb 3+ , Dy 3+ , Ho 3+ , Er 3+ , Tm 3+ , Yb 3+ , Lu 3+ , Sc 3+ , Y 3′ , Al 3+ , Ga 3+ , Ge 4+ , In 3+ , As 3+ , Sn 2+ , Sn 4+ , Sc 3+ , Ti 4+ , V 5+ , Cr 3+ , Mn 2+ , Fe 3+ , Co 2+ , Co 3+ , Ni 2+ , Cu 1+ , Cu 2+ , Zn 2+ , Cd 2+ and mixtures thereof.

4. The chelate according to claim 2 or 3 , wherein the at least one radiometal is selected from the group consisting of 44 Sc, 46 Sc, 55 Co, 99m Tc, 203 Pb, 66 Ga, 67 Ga, 68 Ga, 72 As, 111 In, 113m In, 114m In, 97 Ru, 62 Cu, 64 Cu, 52 Fe, 52m Mn, 51 Cr, 186 Re, 188 Re, 77 As, 90 Y, 67 Cu, 169 Er, 117m Sn, 121 Sn, 127 Te, 142 Pr, 143 Pr, 198 Au, 199 Au, 149 Tb, 161 Tb, 109 Pd, 165 Dy, 149 Pm, 51 Pm, 153 Sm, 157 Gd, 166 Ho, 172 Tm, 169 Yb, 175 Yb, 177 Lu, 105 Rh, 111 Ag and mixtures thereof, preferably selected from the group consisting of 44 Sc, 99m Tc, 67 Ga, 68 Ga, 111 In, 64 Cu, 188 Re, 90 Y, 177 Lu and mixtures thereof.

5. A method of molecular imaging comprising administering a chelate ligand or chelate, according to either claim 2 or claim 3 , to a patient and performing an imaging step.

6. The method according to claim 5 , wherein said molecular imaging is multimodal molecular imaging of the distribution of said chelate ligand or chelate in said patient.

Assignees

• Notni Johannes
• Wester Hans-Jürgen
• Univ Muenchen Tech

Inventors

• Notni Johannes
• Wester Hans-Jürgen

Classifications

• G01N21/75

  Systems in which material is subjected to a chemical reaction, the progress or the result of the reaction being investigated (systems in which material is burnt in a flame or plasma G01N21/72, G01N21/73) · CPC title

• C07F9/65586

  at least one of the hetero rings does not contain nitrogen as ring hetero atom · CPC title

• C07F9/65583

  each of the hetero rings containing nitrogen as ring hetero atom · CPC title

• C07F9/6515

  having three nitrogen atoms as the only ring hetero atoms · CPC title

• A61K51/0482

  chelates from cyclic ligands, e.g. DOTA · CPC title