Nitrogen-containing macrocyclic conjugates as radiopharmaceuticals
AssigneeClarity Pharmaceuticals Ltd
InventorsPaul Stephen Donnelly, Michelle Therese Ma, Denis Bernard Scanlon
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Abstract
The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.
Claims11
A compound of formula (I),
- wherein:
- L is a nitrogen containing macrocyclic metal ligand of the formula
- V is selected from the group consisting of N and CR4;
- each Rx and Ry are independently selected from the group consisting of H, CH3, CO2H, NO2, CH2OH, H2PO4, HSO3, CN, CONH2 and CHO;
- each p is independently an integer selected from the group consisting of 2, 3, and 4;
- R4 is selected from the group consisting of H, OH, halogen, NO2, NH2, optionally substituted C1-C12alkyl, optionally substituted C6-C18aryl, cyano, CO2R5, NHR5, N(R5)2 and a group of the formula:
- wherein
- X1 is a linking moiety;
- Y1 is selected from the group consisting of OR6,SR7, N(R8)2 and a molecular recognition moiety;
- wherein R5 is H or C1-C12alkyl;
- R6 is selected from the group consisting of H, halogen, an oxygen protecting group, optionally substituted C1-C12alkyl, optionally substituted C2-C12alkenyl, optionally substituted C2-C12alkynyl and optionally substituted C2-C12 heteroalkyl;
- R7 is selected from the group consisting of H, halogen, a sulfur protecting group, optionally substituted C1-C12alkyl, optionally substituted C2-C-12alkenyl, optionally substituted C2-C12alkynyl and optionally substituted C2-C12 heteroalkyl;
- each R8 is independently selected from the group consisting of H, a nitrogen protecting group, optionally substituted C1-C12alkyl, optionally substituted C2-C12alkenyl, optionally substituted C2-C12alkynyl and optionally substituted C2-C12 heteroalkyl;
- X is a linking moiety;
- Y is a molecular recognition moiety, wherein the molecular recognition moiety is a cyclic RGD or a portion thereof;
- or
- a pharmaceutically acceptable salt or complex thereof.
Dependencies are inferred from the claim text.