PSMA ligands for imaging and endoradiotherapy
The present invention relates to compounds which bind and/or inhibit prostate-specific membrane antigen (PSMA) comprising at least one group electron dense substituent (EDS), and at least one moiety which is amenable to radiolabeling; and therapeutic and diagnostic uses thereof.
1. A compound or salt that comprises a structure of one of the following formulae:
2. A compound of claim 1 that comprises a structure of the following formula:
or salt thereof.
3. A compound of claim 1 that comprises a structure of the following formula:
or salt thereof.
4. A compound of claim 1 that comprises a structure of the following formula:
or salt thereof.
5. A compound of claim 1 that comprises a structure of the following formula:
or salt thereof.
6. A compound of claim 1 comprising a radioactive cation.
7. A compound of claim 6 comprising 177 Lu.
8. A compound of claim 2 comprising a radioactive cation.
9. A compound of claim 8 comprising 177 Lu.
10. A compound of claim 3 comprising a radioactive cation.
11. A compound of claim 10 comprising 177 Lu.
12. A compound of claim 4 comprising a radioactive cation.
13. A compound of claim 12 comprising 177 Lu.
14. A compound of claim 5 comprising a radioactive cation.
15. A compound of claim 14 comprising 177 Lu.
16. A pharmaceutical composition comprising one or more compounds or salts of claim 1 .
17. A pharmaceutical composition comprising one or more compounds or salts of claim 6 .
18. A method for treating prostate-specific membrane antigen (PSMA)-associated cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 6 .
19. A method for treating prostate-specific membrane antigen (PSMA)-associated cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 7 .
20. A method for treating prostate-specific membrane antigen (PSMA)-associated cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 8 .
21. A method for treating prostate-specific membrane antigen (PSMA)-associated cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 9 .
22. A method for treating prostate-specific membrane antigen (PSMA)-associated cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 10 .
23. A method for treating prostate-specific membrane antigen (PSMA)-associated cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 11 .
24. A method for treating prostate-specific membrane antigen (PSMA)-associated cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 12 .
25. A method for treating prostate-specific membrane antigen (PSMA)-associated cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 13 .
26. A method for treating prostate-specific membrane antigen (PSMA)-associated cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 14 .
27. A method for treating prostate-specific membrane antigen (PSMA)-associated cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 15 .
28. A method for treating prostate cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 6 .
29. A method for treating prostate cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 7 .
30. A method for treating prostate cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 8 .
31. A method for treating prostate cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 9 .
32. A method for treating prostate cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 10 .
33. A method for treating prostate cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 11 .
34. A method for treating prostate cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 12 .
35. A method for treating prostate cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 13 .
36. A method for treating prostate cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 14 .
37. A method for treating prostate cancer in a subject, comprising administering to the subject an effective amount of the composition of claim 15 .