IP Library Granted Patent US 9,789,082
Granted Patent B2
US 9,789,082 · App. 15/157,624 · Granted Oct 17, 2017

Somatostatin receptor subtype 4 (SSTR4) agonists

Inventors: Riccardo Giovannini (Verona, IT); Yunhai Cui (Biberach an der Riss, DE); Henri Doods (Warthausen, DE); Marco Ferrara (San Donato, IT); Stefan Just (Biberach an der Riss, DE); Raimund Kuelzer (Mittelbiberach, DE); Iain Lingard (Monza, IT); Rocco Mazzaferro (San Giuliano, IT); Klaus Rudolf (Warthausen, DE)
Assignee: Centrexion Therapeutics Corporation
A61K31/403A61K31/416A61K31/4155A61K31/423A61K31/426A61K31/429A61K31/437A61K31/4375A61K31/4439A61K31/4709A61K31/4725A61K31/497A61K31/501A61K31/502A61K31/506A61K31/5025A61K31/517A61K31/519C07D209/52C07D401/12C07D403/12C07D405/12C07D413/12C07D417/12C07D471/04C07D487/04
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,789,082
App. No.
15/157,624
Granted
Oct 17, 2017
Kind
B2
Abstract

3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.

Claims (49)

1. A method for the treatment of pain which comprises administering to a host suffering from pain a therapeutically effective amount of a compound of Formula I to treat the pain, wherein Formula I is represented by:

or a salt thereof, wherein:

A is selected from the group consisting of H and C 1-6 -alkyl;

R 1 and R 2 are independently selected from the group consisting of H, C 1-6 -alkyl and C 3-6 -cycloalkyl, wherein at least one of R 1 or R 2 is C 1-6 -alkyl or C 3-6 -cycloalkyl, and the C 1-6 -alkyl or the C 3-6 -cycloalkyl is optionally substituted with halogens or MeO—;

W is a mono- or bicyclic heteroaryl, each of which is optionally substituted with one or more R 3 , and wherein the heteroaryl comprises up to 4 heteroatoms and one or two 5- or 6-membered ring(s);

R 3 is independently selected from the group consisting of C 1-6 -alkyl, C 1-6 -alkyl-O—, halogen, HO—, and NC—; and

Y is selected from the group consisting of a bond, —CH 2 —, —CH 2 CH 2 —, and —CH 2 O—.

2. The method of claim 1 , wherein A is H; and R 1 and R 2 are C 1-6 alkyl.

3. The method of claim 2 , wherein W is selected from the group consisting of

wherein each of these ring systems are optionally substituted with one or more R 3 .

4. The method of claim 2 , wherein Y is —CH 2 O—; and W is

optionally substituted with one R 3 .

5. The method of claim 2 , wherein Y is a bond; and W is

optionally substituted with one R 3 .

6. The method of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

7. The method of claim 1 , wherein the compound is a pharmaceutically acceptable salt of

8. The method of claim 1 , wherein the compound is

9. The method of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

10. The method of claim 1 , wherein the compound is

11. The method of claim 3 , wherein the pain is neuropathic pain.

12. The method of claim 6 , wherein the pain is neuropathic pain.

13. The method of claim 7 , wherein the pain is neuropathic pain.

14. The method of claim 9 , wherein the pain is neuropathic pain.

15. The method of claim 11 , wherein the neuropathic pain is post-stroke pain, pain due to central nervous system injury, or pain due to multiple sclerosis.

16. The method of claim 6 , wherein the pain is low back pain.

17. The method of claim 7 , wherein the pain is low back pain.

18. The method of claim 9 , wherein the pain is low back pain.

19. The method of claim 6 , wherein the pain is chronic back pain.

20. The method of claim 7 , wherein the pain is chronic back pain.

21. The method of claim 6 , wherein the pain is fibromyalgia.

22. The method of claim 7 , wherein the pain is fibromyalgia.

23. The method of claim 6 , wherein the pain is caused by irritable bowel or diabetic neuropathy.

24. The method of claim 7 , wherein the pain is caused by irritable bowel or diabetic neuropathy.

25. The method of claim 6 , wherein pain is trigeminal neuralgia, complex regional pain syndrome Type I, or complex regional pain syndrome Type II.

26. The method of claim 7 , wherein pain is trigeminal neuralgia, complex regional pain syndrome Type I, or complex regional pain syndrome Type II.

27. The method of claim 6 , wherein the pain is caused by osteoarthritis.

28. The method of claim 6 , wherein the pain is tumour pain.

29. The method of claim 3 , wherein the pain is chronic pain.

30. The method of claim 6 , wherein the pain is chronic pain.

31. The method of claim 3 , wherein the pain is inflammatory pain.

32. The method of claim 6 , wherein the pain is inflammatory pain.

33. The method of claim 12 , wherein the host is a human being.

34. The method of claim 16 , wherein the host is a human being.

35. The method of claim 21 , wherein the host is a human being.

36. The method of claim 23 , wherein the host is a human being.

37. The method of claim 25 , wherein the host is a human being.

38. The method of claim 30 , wherein the host is a human being.

Assignments (5)
RELEASE OF SECURITY INTEREST Recorded Nov 21, 2025
From: AVENUE VENTURE OPPORTUNITIES FUND, L.P., AS AGENT
To: CENTREXION THERAPEUTICS CORPORATION
Reel/Frame 073683/0099 →
SECURITY INTEREST Recorded Nov 21, 2025
From: CENTREXION THERAPEUTICS CORPORATION
To: ANKURA TRUST COMPANY, LLC, AS ADMINISTRATIVE AND COLLATERAL AGENT
Reel/Frame 073683/0108 →
SECURITY INTEREST Recorded Jul 12, 2023
From: CENTREXION THERAPEUTICS CORPORATION
To: AVENUE VENTURE OPPORTUNITIES FUND, L.P., AS AGENT
Reel/Frame 064256/0125 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2017
From: GIOVANNINI, RICCARDO; CUI, YUNHAI; DOODS, HENRI; FERRARA, MARCO; JUST, STEFAN; KUELZER, RAIMUND; LINGARD, IAIN; MAZZAFERRO, ROCCO; RUDOLF, KLAUS
To: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Reel/Frame 043513/0820 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 12, 2017
From: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
To: CENTREXION THERAPEUTICS CORPORATION
Reel/Frame 042359/0109 →
Priority Claims (1)
EP 13168224 · May 17, 2013 · regional
Continuity (2)
Continuation 14275879 · May 12, 2014
Related Publication 20170014381A1 · Jan 19, 2017