Claims for Patent: 11,951,190

Summary for Patent: 11,951,190

Title:	Use of labeled inhibitors of prostate specific membrane antigen (PSMA), as agents for the treatment of prostate cancer
Abstract:	The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).
Inventor(s):	Matthias Eder, Klaus Kopka, Martin Schäfer, Ulrike BAUDER-WÜST, Michael Eisenhut, Walter Mier, Martina BENESOVA
Assignee:	Novartis AG
Application Number:	US17/143,280
Patent Claims:	1. A method of treating prostate cancer and/or a metastasis thereof, comprising administering to a patient a therapeutically effective amount of a compound of the formula: and/or a salt thereof, wherein R′ is a chelator of the formula: wherein a radionuclide is complexed to the chelator. 2. The method of treating prostate cancer and/or a metastasis thereof according to claim 1, wherein the radionuclide is chosen from 90Y, 177Lu, 67Cu, 149Tb, 161Tb, 213Bi, 225Ac, 230U, 223Ra, or 131I. 3. The method of treating prostate cancer and/or a metastasis thereof according to claim 1, wherein the radionuclide is chosen from 67Cu, 177Lu, 90Y, or 225Ac. 4. The method of treating prostate cancer and/or a metastasis thereof according to claim 1, wherein the radionuclide is chosen from 177Lu or 225Ac. 5. The method of treating prostate cancer and/or a metastasis thereof according to claim 1, wherein the radionuclide is 177Lu. 6. The method of treating prostate cancer and/or a metastasis thereof according to claim 1, wherein the radionuclide is 225Ac. 7. The method of treating prostate cancer and/or a metastasis thereof according to claim 1, wherein the radionuclide is 67Cu. 8. The method of treating prostate cancer and/or a metastasis thereof according to claim 1, wherein the radionuclide is 90Y. 9. The method of treating prostate cancer and/or a metastasis thereof according to claim 1, comprising administering the compound and/or salt thereof by intravenous, intramusclular, intraarterial, intrathecal, intracapsular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subcuticular, intraarticluare, subcapsular, subarachnoid, intraspinal, or intrasternal injection means, or by infusion. 10. The method of treating prostate cancer and/or a metastasis thereof according to claim 1, comprising administering the compound and/or salt thereof intravenously. 11. The method of treating prostate cancer and/or a metastasis thereof according to claim 2, comprising administering the compound and/or salt thereof by intravenous, intramusclular, intraarterial, intrathecal, intracapsular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subcuticular, intraarticluare, subcapsular, subarachnoid, intraspinal, or intrasternal injection means, or by infusion. 12. The method of treating prostate cancer and/or a metastasis thereof according to claim 2, comprising administering the compound and/or salt thereof intravenously. 13. A method of treating prostate cancer and/or a metastasis thereof, comprising administering to a patient a therapeutically effective amount of a composition comprising: (1) a compound of the formula: and/or a salt thereof, wherein R′ is a chelator of the formula: wherein a radionuclide is complexed to the chelator, and (2) optionally a pharmaceutically acceptable carrier. 14. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, wherein the composition further comprises an excipient, and wherein the excipient is different from said pharmaceutically acceptable carrier. 15. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, wherein the radionuclide is chosen from 90Y, 177Lu, 67Cu, 149Tb, 161Tb, 213Bi, 225Ac, 230U, 223Ra, or 131I. 16. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, wherein the radionuclide is chosen from chosen from 67Cu, 177Lu, 90Y, or 225Ac. 17. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, wherein the radionuclide chosen from 177Lu or 225Ac. 18. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, wherein the radionuclide is 177Lu. 19. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, wherein the radionuclide is 225Ac. 20. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, wherein the radionuclide is 67Cu. 21. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, wherein the radionuclide is 90Y. 22. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, wherein the pharmaceutically acceptable carrier is selected from mannitol, lactose, glucose, and albumin. 23. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, comprising administering the composition by intravenous, intramusclular, intraarterial, intrathecal, intracapsular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subcuticular, intraarticluare, subcapsular, subarachnoid, intraspinal, or intrasternal injection means, or by infusion. 24. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, comprising administering the composition intravenously. 25. The method of treating prostate cancer and/or a metastasis thereof according to claim 15, comprising administering the composition by intravenous, intramusclular, intraarterial, intrathecal, intracapsular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subcuticular, intraarticluare, subcapsular, subarachnoid, intraspinal, or intrasternal injection means, or by infusion. 26. The method of treating prostate cancer and/or a metastasis thereof according to claim 15, comprising administering the composition intravenously. 27. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, wherein the radionuclide is chosen from 90Y, 177Lu, 67Cu, 149Tb, 161Tb, 213Bi, 225Ac, 230U, 223Ra, or 131I. 28. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, wherein the radionuclide is chosen from 67Cu, 177Lu, 90Y, or 225Ac. 29. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, wherein the radionuclide is chosen from 177Lu or 225Ac. 30. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, wherein the radionuclide is 177Lu. 31. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, wherein the radionuclide is 225Ac. 32. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, wherein the radionuclide is 67Cu. 33. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, wherein the radionuclide is 90Y. 34. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, wherein the pharmaceutically acceptable carrier is selected from mannitol, lactose, glucose, and albumin. 35. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, comprising administering the composition by intravenous, intramusclular, intraarterial, intrathecal, intracapsular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subcuticular, intraarticluare, subcapsular, subarachnoid, intraspinal, or intrasternal injection means, or by infusion. 36. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, comprising administering the composition intravenously. 37. The method of treating prostate cancer and/or a metastasis thereof according to claim 13, wherein the composition is a buffered solution. 38. The method of treating prostate cancer and/or a metastasis thereof according to claim 14, wherein the composition is a buffered solution. 39. The method of treating prostate cancer and/or a metastasis thereof according to claim 15, wherein the composition is a buffered solution. 40. The method of treating prostate cancer and/or a metastasis thereof according to claim 22, wherein the composition is a buffered solution. 41. The method of treating prostate cancer and/or a metastasis thereof according to claim 23, wherein the composition is a buffered solution. 42. The method of treating prostate cancer and/or a metastasis thereof according to claim 24, wherein the composition is a buffered solution. 43. The method of treating prostate cancer and/or a metastasis thereof according to claim 25, wherein the composition is a buffered solution. 44. The method of treating prostate cancer and/or a metastasis thereof according to claim 26, wherein the composition is a buffered solution. 45. The method of treating prostate cancer and/or a metastasis thereof according to claim 27, wherein the composition is a buffered solution. 46. The method of treating prostate cancer and/or a metastasis thereof according to claim 34, wherein the composition is a buffered solution. 47. The method of treating prostate cancer and/or a metastasis thereof according to claim 35, wherein the composition is a buffered solution. 48. The method of treating prostate cancer and/or a metastasis thereof according to claim 36, wherein the composition is a buffered solution. 49. The method of treating prostate cancer and/or a metastasis thereof according to claim 5, comprising administering the compound and/or salt thereof by intravenous, intramusclular, intraarterial, intrathecal, intracapsular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subcuticular, intraarticluare, subcapsular, subarachnoid, intraspinal, or intrasternal injection means, or by infusion. 50. The method of treating prostate cancer and/or a metastasis thereof according to claim 5, comprising administering the compound and/or salt thereof intravenously. 51. The method of treating prostate cancer and/or a metastasis thereof according to claim 6, comprising administering the compound and/or salt thereof by intravenous, intramusclular, intraarterial, intrathecal, intracapsular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subcuticular, intraarticluare, subcapsular, subarachnoid, intraspinal, or intrasternal injection means, or by infusion. 52. The method of treating prostate cancer and/or a metastasis thereof according to claim 6, comprising administering the compound and/or salt thereof intravenously. 53. The method of treating prostate cancer and/or a metastasis thereof according to claim 18, comprising administering the composition and/or salt thereof by intravenous, intramusclular, intraarterial, intrathecal, intracapsular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subcuticular, intraarticluare, subcapsular, subarachnoid, intraspinal, or intrasternal injection means, or by infusion. 54. The method of treating prostate cancer and/or a metastasis thereof according to claim 18, comprising administering the composition and/or salt thereof intravenously. 55. The method of treating prostate cancer and/or a metastasis thereof according to claim 19, comprising administering the composition and/or salt thereof by intravenous, intramusclular, intraarterial, intrathecal, intracapsular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subcuticular, intraarticluare, subcapsular, subarachnoid, intraspinal, or intrasternal injection means, or by infusion. 56. The method of treating prostate cancer and/or a metastasis thereof according to claim 19, comprising administering the composition and/or salt thereof intravenously. 57. The method of treating prostate cancer and/or a metastasis thereof according to claim 30, wherein the composition is a buffered solution. 58. The method of treating prostate cancer and/or a metastasis thereof according to claim 31, wherein the composition is a buffered solution. 59. A method of treating prostate cancer and/or a metastasis thereof, comprising administering to a patient a therapeutically effective amount of a compound of the formula: and/or a salt thereof, wherein R′ is a chelator of the formula: wherein a radionuclide is complexed to the chelator. 60. A method of treating prostate cancer and/or a metastasis thereof, comprising administering to a patient a therapeutically effective amount of a composition comprising: (1) a compound of the formula: and/or a salt thereof, wherein R′ is a chelator of the formula: wherein a radionuclide is complexed to the chelator, and (2) optionally a pharmaceutically acceptable carrier. 61. A method of treating prostate cancer and/or a metastasis thereof, comprising administering to a patient a therapeutically effective amount of a compound of the formula: and/or a salt thereof, wherein R′ is a chelator of the formula: wherein a radionuclide is complexed to the chelator. 62. A method of treating prostate cancer and/or a metastasis thereof, comprising administering to a patient a therapeutically effective amount of a composition comprising: (1) a compound of the formula: and/or a salt thereof, wherein R′ is a chelator of the formula: wherein a radionuclide is complexed to the chelator, and (2) optionally a pharmaceutically acceptable carrier.