Highly potent full and partial agonists and antagonists of the nociceptin receptor

Highly potent full and partial agonists and antagonists of the nociceptin receptor

  • CN 101,128,482 A
  • Filed: 02/15/2006
  • Published: 02/20/2008
  • Est. Priority Date: 02/15/2005
  • Status: Active Application
First Claim
Patent Images

1. the polypeptide that has general formula (I)Xaa 1-?

  • -Gly 2-Gly 3-Xbb 4-Thr 5-Gly 6-Xcc 7-Arg 8-Lys 9-Ser 10- Xdd 11-Arg 12-Lys 13-Xee 14-Xff 15-R (I)Wherein;

    Xaa 1Be selected from Phe or N-benzyl-glycine;

    The binding substances of expression between two amino-acid residues, and be selected from CO-NH and CH 2-NH and CH 2-O;

    Xbb 4Be Phe or pXPhe, wherein " X " is selected from H, Cl, Br, I, F, NO 2And CN, and " p " is illustrated in the contraposition of the phenyl ring of phenylalanine;

    Xcc 7And Xdd 11Be selected from Ala, 2-amino-2-methyl-propionic acid (Aib), 2-amino-2-methyl-butyric acid (Iva), 2-amino-2-ethyl-butyric acid (Deg), 2-amino-2-propyl group-valeric acid (Dpg), (CaCH 3) Leu, (CaCH 3) Val, 1-amino-cyclopropyl-carboxylic acid (Ac 3C), 1-amino-cyclopentyl-carboxylic acid (Ac 5C) and 1-amino-cyclohexyl-carboxylic acid (Ac 6C);

    Xee 14And Xff 15Be selected from Arg, Lys, Orn, omoArg, DAB, diaminopropionic acid and Trp;

    R represents dipeptides Asn-Gln-NH 2, Asn-Gln-OH, the Asn that has amino or hydroxy terminal group or amino (NH 2) or hydroxyl (OH) terminal group;

    With and the acceptable salt of pharmacology.

View all claims
    ×
    ×

    Thank you for your feedback

    ×
    ×