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US 2013/0157928 A1Published application
Nociceptin mimetics
AssigneeThe University of Queensland
InventorsDavid Fairlie, Rosemary Sharon Harrison, Nicholas Evan Shepherd
Life of this patent
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Abstract
The present invention relates to nociceptin peptide mimetics that have α-helical structures and bind to and modulate the opioid receptor-like-1 (ORL-1) receptor. The peptide mimetics are constrained cyclic nociceptin analogues which have either agonist or antagonist activity. Pharmaceutical compositions comprising the nociceptin peptide mimetics and methods of treating or preventing a disease or condition ameliorated by modulating the ORL-1 receptor are also described.
Claims34
A peptide of formula (I):
- R1-Xaa1Xaa2Xaa3Xaa4Xaa5Xaa6Lys1Xaa7Xaa8Xaa9Asp1
- Arg1Lys2Lys3Xaa10Xaa11Xaa12Asp2-R2
- (I)
- wherein
- Xaa1 is Phe or N-BzlGly;
- Xaa2 is Gly;
- Xaa3 is Gly or Ala;
- Xaa4 is Phe or 4-R3-Phe;
- Xaa5 is Thr or Ser;
- Xaa6 is any amino acid residue;
- Xaa8 is a basic amino acid residue;
- Xaa7, Xaa9, Xaa10, Xaa11 and Xaa12 are independently selected from any amino acid residue;
- R1 is hydrogen or an N-terminal capping group, with the proviso that when Xaa1 is N-BzlGly, R1 is absent;
- R2 is —OH or a C-terminal capping group;
- and
- R3 is an electron withdrawing substituent;
- wherein the side chains of Lys1 and Asp1 are linked to form a lactam bridge and the side chains of Lys3 and Asp2 are linked to form a lactam bridge;
- or a pharmaceutically acceptable salt thereof
- or a pharmaceutically acceptable salt thereof.
16 more elements
34-35. (canceled)
Dependencies are inferred from the claim text.