Benzimidazole compounds having nociceptin receptor affinity

• US 20020128288A1
• Filed: 12/06/2000
• Published: 09/12/2002
• Est. Priority Date: 12/06/1999
• Status: Active Grant

• Current Assignee: Purdue Pharma L.P.
• Original Assignee: Purdue Pharma L.P.
• Inventors: Kyle, Donald, Shao, Bin, Goehring, R. Richard
• Granted Patent: US 7,456,198 B2
• Time in Patent Office: Days
• US Class Current: 514/322
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 29/02 without antiinflammatory effect
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 401/04 directly linked by a ring-member-to-ring-member bond

Abstract

Disclosed are compounds of the formula (I)

wherein A, R₁, R₂, R₃, R₄ and X₁ are as disclosed herein. The compounds have affinity for the ORL1 receptor and are useful in the treatment of chronic and acute pain.

Claims

16-1. A pharmaceutical composition comprising a compound of claim 1 and at least one pharmaceutically acceptable excipient.

19. A method of modulating a response from opioid receptors comprising administering a compound having a binding affinity for the ORL1 receptor of less than 500 K_i (nM) and a binding affinity for the mu receptor of less than 25 K_i (nM).

20. A method of reducing side effects associated with the administration of opioid analgesics in a human patient comprising administering to said human patient an analgesically effective amount of a non-opioid compound which exhibits a binding affinity for the ORL1 receptor of less than 500 K_i (nM).

21. The method of claim 20 wherein said compound has a binding affinity for the mu receptor of less than 25 K_i (nM).