Patent ID: 6136781
Filing Date: 2000-10-24
Classification: A61K,C07K,Y10S

Abstract:
A cyclic pentapeptide of the formula:cyclo(-A.sub.1 '-A.sub.2 '-A.sub.3 '-A.sub.4 '-A.sub.5 '-)wherein A.sub.1 ' is Arg, Arg(Tos) or Arg(Mtr); and A.sub.2 ', A.sub.3 ', A.sub.4 ', and A.sub.5 ' are defined as follows:when A.sub.2 ' is Lys, Lys(Isopropyl), Lys(SO.sub.2 Nap(1)), Lys(SO.sub.2 Nap(2)), Lys(COPh), Lys(COCH.sub.2 Ph), Lys(CO--(CH.sub.2).sub.3 -Ph), Lys(CO--(CH.sub.2).sub.5 -Ph), Lys(Ac), Lys(CO-Nap(1)), Lys(Nic), or Trp then A.sub.3 ' is Tyr or Trp, A.sub.4 ' is Tyr or Trp, and A.sub.5 ' is Leu;when A.sub.2 ' is Glu, Glu(NH--CH.sub.2 --CH.sub.2 -Ph), Glu(NH--CH.sub.2 -Ph), Glu(NH--CH-Ph.sub.2), Glu(NH--CH.sub.2 -Nap(1)), Glu(Php), Glu(Bzlp), Glu((2)-Pyp), Glu(2-MeOPhp), or Glu(4-MeOPhp), then A.sub.3 ', is Lys, Lys(Isopropyl), Lys(SO.sub.2 Nap(1)), Lys(SO.sub.2 Nap(2)), Lys(COPh), Lys(COCH.sub.2 Ph), Lys(CO--(CH.sub.2).sub.3 -Ph), Lys(CO--(CH.sub.2).sub.5 -Ph), Lys(Ac), Lys(CO-Nap(1)), Lys(Nic), or Tyr, A.sub.4 ' is Trp, and A.sub.5 ' is Leu; orwhen A.sub.2 ' is Phe, (p-Cl)Phe or (p-F)Phe, then A.sub.3 ' is Ala, A.sub.4 ' is Trp and A.sub.5 ' is Phe, (p-Cl)Phe, (p-F)Phe, or Phg;wherein A.sub.1 ', A.sub.3 ' and A.sub.5 ' have an L-configuration, and A.sub.2 ' and A.sub.4 ' have a D-configuration; or A.sub.2 ', A.sub.4 ' and A.sub.5 ' have an L-configuration, and A.sub.1 ' and A.sub.3 ' has a D-configuration; or a salt thereof.