US2006194739A1PendingUtilityA1

Nociceptin-based analgesics

Individually held — no corporate assignee on recordPriority: Oct 9, 2001Filed: Apr 11, 2006Published: Aug 31, 2006
Est. expiryOct 9, 2021(expired)· nominal 20-yr term from priority
Inventors:Amrit K. Judd
A61K 38/00C07K 14/665
64
PatentIndex Score
0
Cited by
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References
0
Claims

Abstract

The invention relates to a family of hexapeptide compounds exhibiting activity with regard to the ORL-1 receptor. The compounds share a general formula of Arg-Tyr-Tyr-Arg-Trp-Arg, and may be constructed having modifications or substitutions at any position, and may include modifications of the amino- and carboxy-termini of the hexapeptide. These compounds include agents exhibiting agonist activity and antagonist activity when exposed to the human ORL-1 receptor. As such, the hexapeptides may be useful as analgesics, anxiolytics, diuretics, and anti-cancer agents.

Claims

exact text as granted — not AI-modified
1 . A hexapeptide of the formula: 
 Arg-Xaa-Tyr-Arg-Trp-Arg (SEQ ID NO: 17), wherein the hexapeptide binds with the ORL-1 receptor, wherein Xaa is selected from the group consisting of natural amino acids, D-amino acids, non-natural amino acids, modified natural amino acids, and amino acid analogs.    
     
     
         2 . (canceled)  
     
     
         3 . (canceled)  
     
     
         4 . (canceled)  
     
     
         5 . The hexapeptide of  claim 1 , having the formula of SEQ ID NO: 1.  
     
     
         6 . The hexapeptide of  claim 1 , having the formula of SEQ ID NO: 2.  
     
     
         7 . The hexapeptide of  claim 1 , having the formula of SEQ ID NO: 3.  
     
     
         8 . The hexapeptide of  claim 1 , having the formula of SEQ ID NO: 4.  
     
     
         9 . The hexapeptide of  claim 1 , having the formula of SEQ ID NO: 6.  
     
     
         10 . (canceled)  
     
     
         11 . (canceled)  
     
     
         12 . The hexapeptide of  claim 1 , having the formula of SEQ ID NO: 5.  
     
     
         13 . The hexapeptide of  claim 1 , having the formula of SEQ ID NO: 7.  
     
     
         14 . The hexapeptide of  claim 1 , having the formula of SEQ ID NO: 23.  
     
     
         15 . (canceled)  
     
     
         16 . (canceled)  
     
     
         17 . (canceled)  
     
     
         18 . (canceled)  
     
     
         19 . (canceled)  
     
     
         20 . (canceled)  
     
     
         21 . A hexapeptide of the formula: 
 Arg-Tyr-Xaa-Arg-Trp-Arg (SEQ ID NO: 18), wherein the hexapeptide binds with the ORL-1 receptor, wherein Xaa is selected from the group consisting of natural amino acids, D-amino acids, non-natural amino acids, modified natural amino acids, and amino acid analogs.    
     
     
         22 . (canceled)  
     
     
         23 . (canceled)  
     
     
         24 . (canceled)  
     
     
         25 . The hexapeptide of  claim 21 , having the formula of SEQ ID NO: 12.  
     
     
         26 . The hexapeptide of  claim 21 , having the formula of SEQ ID NO: 13.  
     
     
         27 . The hexapeptide of  claim 21 , having the formula of SEQ ID NO: 20.  
     
     
         28 . The hexapeptide of  claim 21 , having the formula of SEQ ID NO: 21.  
     
     
         29 . The hexapeptide of  claim 21 , having the formula of SEQ ID NO: 16.  
     
     
         30 . The hexapeptide of  claim 21 , having the formula of SEQ ID NO: 22.  
     
     
         31 . The hexapeptide of  claim 21 , wherein Xaa is a modified Tyr amino acid molecule.  
     
     
         32 . The hexapeptide of  claim 31 , wherein Xaa is Tyr (2, 6 di-Me) (SEQ ID NO: 15).  
     
     
         33 . (canceled)  
     
     
         34 . (canceled)  
     
     
         35 . (canceled)  
     
     
         36 . (canceled)  
     
     
         37 . (canceled)  
     
     
         38 . (canceled)  
     
     
         39 . (canceled)  
     
     
         40 . (canceled)  
     
     
         41 . (canceled)  
     
     
         42 . (canceled)  
     
     
         43 . (canceled)  
     
     
         44 . (canceled)  
     
     
         45 . (canceled)  
     
     
         46 . (canceled)  
     
     
         47 . (canceled)  
     
     
         48 . (canceled)  
     
     
         49 . (canceled)  
     
     
         50 . (canceled)  
     
     
         51 . (canceled)  
     
     
         52 . A hexapeptide of the formula: 
 Arg-Tyr-Tyr-Arg-Xaa-Arg (SEQ ID NO: 27), wherein the hexapeptide binds with the ORL-1 receptor, wherein Xaa is selected from the group consisting of natural amino acids, D-amino acids, non-natural amino acids, modified natural amino acids, and amino acid analogs.    
     
     
         53 . (canceled)  
     
     
         54 . (canceled)  
     
     
         55 . (canceled)  
     
     
         56 . (canceled)  
     
     
         57 . (canceled)  
     
     
         58 . (canceled)  
     
     
         59 . (canceled)  
     
     
         60 . (canceled)  
     
     
         61 . (canceled)  
     
     
         62 . (canceled)  
     
     
         63 . (canceled)  
     
     
         64 . (canceled)  
     
     
         65 . (canceled)  
     
     
         66 . (canceled)  
     
     
         67 . (canceled)

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