IP Library Granted Patent US 10,239,870
Granted Patent B2
US 10,239,870 · App. 15/975,466 · Granted Mar 26, 2019

Dopamine D3 receptor antagonists

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Quick Facts
Patent No.
US 10,239,870
App. No.
15/975,466
Granted
Mar 26, 2019
Kind
B2
Abstract

The disclosure is directed to novel dopamine D3 receptor antagonists, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, including treating drug dependency and psychosis.

Claims (40)

1. A compound or a pharmaceutically acceptable salt thereof, wherein the compound is:

2. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.

3. A method of modulating dopamine D 3 receptors in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 1 to modulate the dopamine D 3 receptors.

4. The method of claim 3 , wherein the method of modulating dopamine D 3 receptors is a method for treating Parkinson's disease; neuroleptic-induced parkinsonism; tardive dyskinesia; depression; anxiety; a cognitive impairment; Alzheimer's disease; an eating disorder; a sexual dysfunction; a sleep disorder; emesis; a movement disorder; obsessive-compulsive disorder; amnesia; aggression; autism; vertigo; dementia; a circadian rhythm disorder; a gastric motility disorder, or a gambling disorder.

5. A method for treating a psychotic condition in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 1 to treat the psychotic condition.

6. A method for treating opioid use disorder in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 1 to treat the opioid use disorder.

7. A method for treating schizophrenia in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 1 to treat the schizophrenia.

8. A method of treating a substance-related disorder in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 1 to treat the substance-related disorder.

9. A compound or a pharmaceutically acceptable salt thereof, wherein the compound is:

10. A pharmaceutical composition comprising the compound of claim 9 and a pharmaceutically acceptable carrier.

11. A method of modulating dopamine D 3 receptors in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 9 to modulate the dopamine D 3 receptors.

12. The method of claim 11 , wherein the method of modulating dopamine D 3 receptors is a method for treating Parkinson's disease; neuroleptic-induced parkinsonism; tardive dyskinesia; depression; anxiety; a cognitive impairment; Alzheimer's disease; an eating disorder; a sexual dysfunction; a sleep disorder; emesis; a movement disorder; obsessive-compulsive disorder; amnesia; aggression; autism; vertigo; dementia; a circadian rhythm disorder; a gastric motility disorder, or a gambling disorder.

13. A method for treating a psychotic condition in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 9 to treat the psychotic condition.

14. A method for treating opioid use disorder in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 9 to treat the opioid use disorder.

15. A method for treating schizophrenia in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 9 to treat the schizophrenia.

16. A method of treating a substance-related disorder in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 9 to treat the substance-related disorder.

17. A compound or a pharmaceutically acceptable salt thereof, wherein the compound is:

18. A pharmaceutical composition comprising the compound of claim 17 and a pharmaceutically acceptable carrier.

19. A method of modulating dopamine D 3 receptors in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 17 to modulate the dopamine D 3 receptors.

20. The method of claim 19 , wherein the method of modulating dopamine D 3 receptors is a method for treating Parkinson's disease; neuroleptic-induced parkinsonism; tardive dyskinesia; depression; anxiety; a cognitive impairment; Alzheimer's disease; an eating disorder; a sexual dysfunction; a sleep disorder; emesis; a movement disorder; obsessive-compulsive disorder; amnesia; aggression; autism; vertigo; dementia; a circadian rhythm disorder; a gastric motility disorder, or a gambling disorder.

21. A method for treating a psychotic condition in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 19 to treat the psychotic condition.

22. A method for treating opioid use disorder in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 19 to treat the opioid use disorder.

23. A method for treating schizophrenia in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 19 to treat the schizophrenia.

24. A method of treating a substance-related disorder in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 19 to treat the substance-related disorder.

25. A compound or a pharmaceutically acceptable salt thereof, wherein the compound is:

26. A pharmaceutical composition comprising the compound of claim 25 and a pharmaceutically acceptable carrier.

27. A method of modulating dopamine D 3 receptors in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 25 to modulate the dopamine D 3 receptors.

28. The method of claim 27 , wherein the method of modulating dopamine D 3 receptors is a method for treating Parkinson's disease; neuroleptic-induced parkinsonism; tardive dyskinesia; depression; anxiety; a cognitive impairment; Alzheimer's disease; an eating disorder; a sexual dysfunction; a sleep disorder; emesis; a movement disorder; obsessive-compulsive disorder; amnesia; aggression; autism; vertigo; dementia; a circadian rhythm disorder; a gastric motility disorder, or a gambling disorder.

29. A method for treating a psychotic condition in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 25 to treat the psychotic condition.

30. A method for treating opioid use disorder in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 25 to treat the opioid use disorder.

31. A method for treating schizophrenia in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 25 to treat the schizophrenia.

32. A method of treating a substance-related disorder in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 25 to treat the substance-related disorder.

33. A compound or a pharmaceutically acceptable salt thereof, wherein the compound is:

34. A pharmaceutical composition comprising the compound of claim 33 and a pharmaceutically acceptable carrier.

35. A method of modulating dopamine D 3 receptors in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 33 to modulate the dopamine D 3 receptors.

36. The method of claim 35 , wherein the method of modulating dopamine D 3 receptors is a method for treating Parkinson's disease; neuroleptic-induced parkinsonism; tardive dyskinesia; depression; anxiety; a cognitive impairment; Alzheimer's disease; an eating disorder; a sexual dysfunction; a sleep disorder; emesis; a movement disorder; obsessive-compulsive disorder; amnesia; aggression; autism; vertigo; dementia; a circadian rhythm disorder; a gastric motility disorder, or a gambling disorder.

37. A method for treating a psychotic condition in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 33 to treat the psychotic condition.

38. A method for treating opioid use disorder in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 33 to treat the opioid use disorder.

39. A method for treating schizophrenia in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 33 to treat the schizophrenia.

40. A method of treating a substance-related disorder in a mammal in need thereof, the method comprising administering to the mammal an effective amount of the compound of claim 33 to treat the substance-related disorder.

Assignments (7)
RELEASE OF SECURITY INTEREST Recorded Mar 18, 2026
From: PIPER SANDLER FINANCE, LLC
To: INDIVIOR INC.; INDIVIOR UK LIMITED
Reel/Frame 074114/0582 →
SECURITY INTEREST Recorded Nov 13, 2024
From: INDIVIOR INC.; INDIVIOR UK LIMITED
To: PIPER SANDLER FINANCE LLC, AS COLLATERAL AGENT
Reel/Frame 069254/0413 →
TERMINATION AND RELEASE OF SECURITY INTEREST Recorded Nov 11, 2024
From: MORGAN STANLEY SENIOR FUNDING, INC.
To: INDIVIOR UK LIMITED (F/K/A RB PHARMACEUTICALS LIMITED)
Reel/Frame 069316/0760 →
NOTICE OF GRANT OF SECURITY INTEREST IN PATENTS AND TRADEMARKS Recorded Aug 28, 2019
From: INDIVIOR UK LIMITED (FORMERLY KNOWN AS RB PHARMACEUTICALS LIMITED)
To: MORGAN STANLEY SENIOR FUNDING INC., AS COLLATERAL AGENT
Reel/Frame 050196/0961 →
CHANGE OF ASSIGNEE ADDRESS Recorded May 21, 2019
From: INDIVIOR UK LIMITED
To: INDIVIOR UK LIMITED
Reel/Frame 049246/0785 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 19, 2018
From: MICHELI, FABRIZIO; CREMONESI, SUSANNA; SEMARARO, TERESA; TARSI, LUCA
To: APTUIT, SRL
Reel/Frame 047816/0915 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 19, 2018
From: APTUIT, SRL
To: INDIVIOR UK LIMITED
Reel/Frame 047817/0049 →