Patent ID: 6235711
Filing Date: 2001-05-22
Classification: A61K,A61P,C07K,Y10S

Abstract:
A cyclic peptide of the formula ##STR19##whereXaa.sub.1 is selected from an L-amino acid or a D-amino acid, wherein the L-amino acid is selected from Phe, Lys and Arg, the D-amino acid is selected from Phe and Met, and the L- or D-amino acid optionally is substituted on its ax-carbon or ax-amino group with a C.sub.1-4 alkyl group,orXaa.sub.1 is MeIle;Xaa.sub.2 is Leu, optionally substituted on its .alpha.-carbon or .alpha.-amino group with a C.sub.1-4 alkyl group;Xaa.sub.3 is Asp, optionally substituted on its .alpha.-carbon or cc-amino group with a C.sub.1-4 alkyl group;Xaa.sub.4 is Val, optionally substituted on its .alpha.-carbon or .alpha.-amino group with a C.sub.1-4 alkyl group;X.sup.1 is a D-amino acid selected from Ala, Phe, Arg, Lys, Trp, hArg(Et).sub.2, Orn(CHMe.sub.2), Orn(Me.sub.2), Lys(CHMe.sub.2) and Arg(Pmc), optionally substituted on its .alpha.-carbon or its .alpha.-amino group with a C.sub.1-4 alkyl group;orX.sup.1 is ##STR20##NH(CH.sub.2).sub.5 CO, or NH(CH.sub.2).sub.2 S(CH.sub.2).sub.y CO where y is 1 or 2;X.sup.2 is a D-amino acid selected from Ala, Arg, Lys, His, hArg(Et).sub.2, Orn(CHMe.sub.2), and Orn(Me.sub.2), optionally substituted on its .alpha.-carbon or its .alpha.-amino group with a C.sub.1-4 alkyl group,orx.sup.2 is NH(CH.sub.2).sub.2 SCH.sub.2 CO, or NH(CH.sub.2).sub.x CO where x is 2 or 3;Xaa.sub.5 and Xaa.sub.6 are each, independently, a D-amino acid selected from Ala and Arg, optionally substituted on its .alpha.-carbon or .alpha.-amino group with a C.sub.1-4 alkyl group;p is 0 or 1; andq is 0 or when p is 1, q is 0 or 1;or a salt thereof;with the proviso that when Xaa.sub.1 is MeIle, Xaa.sub.2 is Leu, Xaa.sub.3 is Asp, Xaa.sub.4 is Val and p and q are both 0, theni) X.sup.2 is not D-Ala, D-Arg, or D-Lys when X.sup.1 is D-Ala;ii) X.sup.2 is not D-Arg when X.sup.1 is ##STR21##iii) X.sup.2 is not D-Ala, D-Arg or D-His when X.sup.1 is D-Arg;iv) X.sup.2 is not D-Ala when X.sup.1 is D-Orn(CHMe.sub.2) or D-Arg(Pmc);v) x.sup.2 is not D-Ala or D-Lys when X.sup.1 is D-Lys; andvi) X.sup.2 is not D-Lys or D-Arg when X.sup.1 is D-Phe or D-Trp.