(Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

Patent metadata

Field	Value
Publication number	US-9650370-B2
Application number	US-201414891051-A
Country	US
Kind code	B2
Filing date	May 16, 2014
Priority date	May 17, 2013
Publication date	May 16, 2017
Grant date	May 16, 2017

Abstract

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazolesand-[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

First claim

The invention claimed is:

1. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 , wherein the compound is

4. The compound of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition comprising a compound according to claim 1 in admixture with a pharmaceutically acceptable adjuvant, diluent, and/or carrier.

6. A pharmaceutical composition comprising a compound according to claim 2 in admixture with a pharmaceutically acceptable adjuvant, diluent, and/or carrier.

7. A pharmaceutical composition comprising a compound according to claim 3 in admixture with a pharmaceutically acceptable adjuvant, diluent, and/or carrier.

8. A pharmaceutical composition comprising a compound according to claim 4 in admixture with a pharmaceutically acceptable adjuvant, diluent, and/or carrier.

9. A method of treating a disease or disorder selected from the group consisting of pain, osteoarthritis, and diabetic neuropathy, comprising administering to a human being an effective amount of a compound selected from the group consisting of

or a pharmaceutically acceptable salt thereof, to treat the disease or disorder.

10. The method of claim 9 , wherein the disease or disorder is pain.

11. The method of claim 10 , wherein the pain is low back pain, hip pain, or leg pain.

12. The method of claim 10 , wherein the pain is due to fibromyalgia.

13. The method of claim 10 , wherein the pain is due to trigeminal neuralgia, complex regional pain syndrome Type I, or complex regional pain syndrome Type II.

14. The method of claim 10 , wherein the pain is due to diabetic neuropathy.

15. The method of claim 10 , wherein the pain is acquired immune deficiency syndrome (AIDS) related neuropathic pain.

16. The method of claim 10 , wherein the pain is post-stroke pain, pain due to central nervous system injury, or pain due to multiple sclerosis.

17. The method of claim 10 , wherein the pain is tumour pain, pain due to carpal tunnel syndrome, pain due to irritable bowel, or pain due to osteoarthritis.

18. The method of claim 9 , wherein the disease or disorder is osteoarthritis or diabetic neuropathy.

19. The method of claim 9 , wherein the compound is a compound of claim 2 .

20. The method of claim 10 , wherein the compound is a compound of claim 2 .

21. The method of claim 11 , wherein the compound is a compound of claim 2 .

22. The method of claim 12 , wherein the compound is a compound of claim 2 .

23. The method of claim 13 , wherein the compound is a compound of claim 2 .

24. The method of claim 14 , wherein the compound is a compound of claim 2 .

25. The method of claim 15 , wherein the compound is a compound of claim 2 .

26. The method of claim 16 , wherein the compound is a compound of claim 2 .

27. The method of claim 17 , wherein the compound is a compound of claim 2 .

28. The method of claim 18 , wherein the compound is a compound of claim 2 .

29. The method of claim 10 , wherein the pain is chronic back pain.

30. The method of claim 29 , wherein the compound is a compound of claim 2 .

31. A method of treating irritable bowel syndrome, comprising administering to a human being an effective amount of a compound selected from the group consisting of

or a pharmaceutically acceptable salt thereof, to treat the irritable bowel syndrome.

32. The method of claim 31 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

Assignees

• Centrexion Therapeutics Corp

Inventors

• Riether Doris
• Binder Florian Paul Christian
• Doobs Henri
• Mueller Stephan Georg
• Nicholson Janet Rachel
• Sauer Achim

Classifications

• A61P39/00

  General protective or antinoxious agents · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P25/02

  for peripheral neuropathies · CPC title

• A61P25/04

  Centrally acting analgesics, e.g. opioids · CPC title