LARSEN, BJARNE DUE,PETERSEN, JORGEN SOBERG,KAPUSTA, DANIEL R.,HARLOW, KENNETH WILLIAM
申请号：
CA2410224
公开号：
CA2410224C
申请日:
2001.06.15
申请国别(地区):
CA
年份:
2013
代理人:
摘要：
Disclosed are a variety of peptide conjugates represented by the followinggeneral formula (I): R1-Z-X-Z'-R2, wherein X represents a hexapeptide of theformula (II): A1-A2-A3-A4-A5-A6 wherein A1 represents Arg, Lys, or His, A2represents Tyr, Trp, or Phe, A3 represents Tyr, Asn, Trp or Phe, A4 representsLys, Arg or His, A5 represents Phe, Tyr, Trp, Leu, Val or Ile, and A6represents Arg, Lys, or His and wherein each amino acid residue in saidhexapeptide may be in the L or D form； Z represents a charged peptide chain offrom 4 to 20 amino acid residues having the D or L configuration or ismissing； and Z' represents a charged peptide chain of from 4 to 20 amino acidresidues having the D or L configuration or is missing, providing that notboth of Z and Z' are missing； R1 represents H or an acyl group； R2 representsNR3R4 where each of R3 and R4 independently represents hydrogen, C(1-6)alkoxy,aryloxy, or a lower alkyl as defined herein； or R2 represents OH； the peptideconjugates of formula (I) being optionally further linked to a transportmoiety； and salts, hydrates and solvates thereof, and C-terminally amidated oresterified derivatives thereof with suitable organic or inorganic acids,including methods or making and using such conjugates. Also provided areantibodies that specifically bind the peptide conjugates. The presentinvention has a wide spectrum of important applications including use in thetreatment of disorders impacted by nociceptin and related opioid-like peptides.
