IP Library › Granted Patent US 10,398,791

Granted Patent B2

US 10,398,791 · App. 16/114,988 · Granted Sep 3, 2019

Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

Inventors: Matthias Eder (Mannheim, DE); Klaus Kopka (Dossenheim, DE); Martin Schäfer (Neckarsteinach, DE); Ulrike Bauder-Wüst (Schriesheim, DE); Uwe Haberkorn (Schwetzingen, DE); Michael Eisenhut (Heidelberg, DE); Walter Mier (Bensheim, DE); Martina Benesova (Heidelberg, DE)

Assignees: DEUTSCHES KREBSFORSCHUNGSZENTRUM; RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG

A61K51/0482 C07B59/002 C07D257/02 C07D295/145

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Quick Facts

Patent No.: US 10,398,791
App. No.: 16/114,988
Granted: Sep 3, 2019
Kind: B2

External Links

USPTO Patent Center↗ Full Patent PDF↗

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).

Claims (66)

1. A compound of the formula:

or a salt thereof.

2. The compound or salt thereof according to claim 1 , wherein the compound or salt is lyophilized.

3. A composition comprising:

(1) the compound and/or a salt thereof according to claim 1 ; and

(2) optionally a pharmaceutically acceptable carrier.

4. The composition of claim 3 ,

wherein the composition further comprises an excipient, and

wherein the excipient is different from said pharmaceutically acceptable carrier.

5. The composition of claim 3 , wherein the composition is a buffered solution.

6. The composition of claim 3 , wherein the compound and/or a salt thereof, and optionally the pharmaceutically acceptable carrier, are lyophilized.

7. A compound of the formula:

or a salt thereof.

8. The compound or salt thereof according to claim 7 , wherein the compound or salt is lyophilized.

9. A composition comprising:

(1) the compound and/or a salt thereof according to claim 7 ; and

(2) optionally a pharmaceutically acceptable carrier.

10. The composition of claim 9 ,

wherein the composition further comprises an excipient, and

wherein the excipient is different from said pharmaceutically acceptable carrier.

11. The composition of claim 9 , wherein the composition is a buffered solution.

12. A compound of the formula:

or a salt thereof,

wherein R′ is a chelator of the formula:

wherein 177 Lu is complexed to the chelator.

13. A composition comprising:

(1) the compound and/or a salt thereof according to claim 12 ; and

(2) optionally a pharmaceutically acceptable carrier.

14. The composition of claim 13 ,

wherein the composition further comprises an excipient, and

wherein the excipient is different from said pharmaceutically acceptable carrier.

15. The composition of claim 13 , wherein the composition is a buffered solution.

16. A compound of the formula:

or a salt thereof,

wherein R′ is a chelator of the formula:

wherein 177 Lu is complexed to the chelator.

17. A composition comprising:

(1) the compound and/or a salt thereof according to claim 16 ; and

(2) optionally a pharmaceutically acceptable carrier.

18. The composition of claim 17 ,

wherein the composition further comprises an excipient, and

wherein the excipient is different from said pharmaceutically acceptable carrier.

19. The composition of claim 17 , wherein the composition is a buffered solution.

20. The composition of claim 9 , wherein the compound and/or a salt thereof, and optionally the pharmaceutically acceptable carrier, are lyophilized.

21. The compound of claim 7 having the formula:

or a salt thereof.

22. The compound or salt thereof according to claim 21 , wherein the compound or salt is lyophilized.

23. A composition comprising:

(1) the compound and/or a salt thereof according to claims 21 ; and

(2) optionally a pharmaceutically acceptable carrier.

24. The composition of claim 23 ,

wherein the composition further comprises an excipient, and

wherein the excipient is different from said pharmaceutically acceptable carrier.

25. The composition according to claim 23 , wherein the composition is a buffered solution.

26. The composition of claim 23 , wherein the compound and/or a salt thereof, and optionally the pharmaceutically acceptable carrier, are lyophilized.

27. The compound of claim 16 having the formula:

or a salt thereof,

wherein R′ is a chelator of the formula:

wherein 177 Lu is complexed to the chelator.

28. A composition comprising:

(1) the compound and/or a salt thereof according to claims 27 ; and

(2) optionally a pharmaceutically acceptable carrier.

29. The composition of claim 28 ,

wherein the composition further comprises an excipient, and

wherein the excipient is different from said pharmaceutically acceptable carrier.

30. The composition of claim 28 , wherein the composition is a buffered solution.

Assignments (10)

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 3, 2023

From: NOVARTIS PHARMA AG

To: NOVARTIS AG

Reel/Frame 064482/0485 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 3, 2023

From: DEUTSCHES KREBSFORSCHUNGSZENTRUM; RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG

To: NOVARTIS PHARMA AG

Reel/Frame 064482/0290 →

DECLARATION OF BRENDA HERSCHBACH JARRELL Recorded Apr 12, 2022

From: RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG; DEUTSCHES KREBSFORSCHUNGSZENTRUM

To: RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG; DEUTSCHES KREBSFORSCHUNGSZENTRUM

Reel/Frame 059690/0222 →

SECOND DECLARATION TO CORRECT ASSIGNMENT RECORD AFTER ATTEMPT BY A THIRD PARTY TO RECORD AN IMPROPER ASSIGNMENT IN APPLICATION NO. 16/114,988 AT REEL 051989/FRAME 0918 Recorded Nov 20, 2021

From: RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG; DEUTSCHES KREBSFORSCHUNGSZENTRUM

To: RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG; DEUTSCHES KREBSFORSCHUNGSZENTRUM

Reel/Frame 058573/0601 →

DECLARATION TO CORRECT ASSIGNMENT RECORD FOLLOWING DECLARATION RECORDED ON NOVEMBER 12, 2019 IN APPLICATION NO. 16/114,988 Recorded Feb 21, 2020

From: MOLECULAR INSIGHT PHARMACEUTICAL, INC.; UNIVERSITY OF HEIDELBERG

To: MOLECULAR INSIGHT PHARMACEUTICAL, INC.; UNIVERSITY OF HEIDELBERG

Reel/Frame 051989/0918 →

DECLARATION TO CORRECT ASSIGNMENT RECORD AFTER ATTEMPT BY A THIRD PARTY TO RECORD AN IMPROPER ASSIGNMENT IN APPLICATION NO. 16/114,988 AT REEL 047972/FRAME 0664 Recorded Nov 12, 2019

From: RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG; DEUTSCHES KREBSFORSCHUNGSZENTRUM

To: RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG; DEUTSCHES KREBSFORSCHUNGSZENTRUM

Reel/Frame 050994/0511 →

CONFIRMATION OF OWNERSHIP (AS FILING RELATES TO COMPOUNDS THAT ARE "DERIVATIVES") Recorded Dec 20, 2018

From: UNIVERSITY OF HEIDELBERG

To: MOLECULAR INSIGHT PHARMACEUTICAL, INC.

Reel/Frame 047972/0664 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2018

From: KRATOCHWIL, CLEMENS

To: RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG

Reel/Frame 047146/0613 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 28, 2018