IP Library Granted Patent US 11,046,706
Granted Patent B2
US 11,046,706 · App. 16/233,315 · Granted Jun 29, 2021

CCR2 receptor antagonists and uses thereof

Inventors: Heiner Ebel (Biberach an der Riss, DE); Sara Frattini (Castelleone, IT); Kai Gerlach (Mittelbiberach, DE); Riccardo Giovannini (Verona, IT); Christoph Hoenke (Biberach an der Riss, DE); Rocco Mazzaferro (San Giuliano Milanese, IT); Marco Santagostino (Mittelbiberach, DE); Stefan Scheuerer (Warthausen, DE); Christofer Tautermann (Biberach, DE); Thomas Trieselmann (Mettenberg, DE)
Assignee: Centrexion Therapeutics Corporation
C07D491/107A61P25/00A61P25/02A61P25/04A61P29/00C07D405/14
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Quick Facts
Patent No.
US 11,046,706
App. No.
16/233,315
Granted
Jun 29, 2021
Kind
B2
Abstract

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

Claims (27)

1. A method for treating a neurologic disease selected from inflammatory and neuropathic pain, comprising administering to a patient in need thereof an effective amount of a pharmaceutical formulation containing a compound of Formula I, to treat the neurologic disease, wherein Formula I is

or a salt thereof.

2. The method of claim 1 , wherein the neurologic disease is inflammatory pain.

3. The method of claim 1 , wherein the neurologic disease is neuropathic pain.

4. The method of claim 3 , wherein the neuropathic pain is low back pain.

5. The method of claim 3 , wherein the neuropathic pain is trigeminal neuralgia.

6. The method of claim 3 , wherein the neuropathic pain is hip pain, leg pain, non-herpetic neuralgia, post herpetic neuralgia, diabetic neuropathy, nerve injury-induced pain, phantom limb pain, post-surgical pain, or stump pain.

7. The method of claim 1 , wherein the neurologic disease is neuropathic pain due to chemotherapy caused nerve injury.

8. The method of claim 2 , wherein the pharmaceutical formulation is administered orally to the patient.

9. The method of claim 3 , wherein the pharmaceutical formulation is administered orally to the patient.

10. The method of claim 4 , wherein the pharmaceutical formulation is administered orally to the patient.

11. The method of claim 5 , wherein the pharmaceutical formulation is administered orally to the patient.

12. A method for treating a neurologic disease selected from inflammatory and neuropathic pain, comprising administering to a patient in need thereof an effective amount of pharmaceutical formulation containing a compound of Formula I, to treat the neurologic disease, wherein Formula I is an acid addition salt formed by a pharmacologically acceptable acid and the following compound:

13. The method of claim 12 , wherein the neurologic disease is inflammatory pain.

14. The method of claim 12 , wherein the neurologic disease is neuropathic pain.

15. The method of claim 14 , wherein the neuropathic pain is low back pain.

16. The method of claim 14 , wherein the neuropathic pain is trigeminal neuralgia.

17. The method of claim 14 , wherein the neuropathic pain is hip pain, leg pain, non-herpetic neuralgia, post herpetic neuralgia, diabetic neuropathy, nerve injury-induced pain, phantom limb pain, post-surgical pain, or stump pain.

18. The method of claim 12 , wherein the neurologic disease is neuropathic pain due to chemotherapy caused nerve injury.

19. The method of claim 13 , wherein the pharmaceutical formulation is administered orally to the patient.

20. The method of claim 14 , wherein the pharmaceutical formulation is administered orally to the patient.

21. The method of claim 15 , wherein the pharmaceutical formulation is administered orally to the patient.

22. The method of claim 16 , wherein the pharmaceutical formulation is administered orally to the patient.

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

24. The method of claim 3 , wherein the neuropathic pain is nerve injury-induced pain.

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

26. The method of claim 14 , wherein the neuropathic pain is nerve injury-induced pain.

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 Feb 7, 2020
From: EBEL, HEINER; FRATTINI, SARA; GERLACH, KAI; GIOVANNINI, RICCARDO; HOENKE, CHRISTOPH; MAZZAFERRO, ROCCO; SANTAGOSTINO, MARCO; SCHEUERER, STEFAN; TAUTERMANN, CHRISTOFER; TRIESELMANN, THOMAS
To: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Reel/Frame 051757/0967 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 7, 2020
From: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
To: CENTREXION THERAPEUTICS CORPORATION
Reel/Frame 051759/0879 →
Priority Claims (2)
EP 09179555 · Dec 17, 2009 · regional
EP 10162621 · May 12, 2010 · regional
Continuity (4)
Continuation 15606749 · May 26, 2017
Continuation 14260552 · Apr 24, 2014
Division 12969745 · Dec 16, 2010
Related Publication 20190300541A1 · Oct 3, 2019
Cited By (1)
US 12,209,094