Patent ID: 6183722
Filing Date: 2001-02-06
Classification: A61K

Abstract:
A somatostatin receptor-binding peptide having a formula: ##STR30##wherein R.sup.1, R.sup.2, R.sup.5 and R.sup.6 are independently H, lower alkyl or substituted alkyl, aryl orsubstituted aryl;R.sup.3 and R.sup.4 are each independently H, lower alkyl or substituted alkyl, aryl or substituted aryl, or wherein either R.sup.3 or R.sup.4 is X.sup.1 ;A.sup.1 and C.sup.3 are independently a bond, a D-amino acid, or an L-amino acid;A.sup.2, A.sup.3 and C.sup.1 are each independently a bond, a lipophilic D-amino acid, or a lipophilic L-amino acid;B.sup.1 is D--Phe, L--Phe, D--Tyr, L--Tyr, D--Nal, L--Nal, or Ain;B.sup.2 is D--Trp or L--Trp;B.sup.3 is D--Lys, L--Lys, Hly, Achxa, Amf, Aec, Apc, Aes, or Aps;B.sup.4 is Thr, Ser, Val, Phe, Ile, Abu, Nle, Leu, Nva or Aib;C.sup.2 is a bond, D--Thr, L--Thr, Ser, Val, Phe, Ile, Abu, Nle, Leu, Nva, Nal or Aib;X.sup.1 is N(R.sup.10).sub.2, wherein each R.sup.10 is independently hydrogen, lower alkyl or substituted lower alkyl, aryl or substituted aryl or substituted with a hydrophilic moiety of less than about 1500 daltons;X.sup.2 is --COOR.sup.9, --CH.sub.2 OH, CH.sub.2 COOR.sup.9, or --CON(R.sup.9).sub.2, where each R.sup.9 is independently H, lower linear or cyclic alkyl or substituted with a hydrophilic moiety of less than about 1500 daltons;m is 0, 1, 2 or 3;p is 0, 1 or 2;R.sup.7 and R.sup.8 are independently H, lower alkyl or substituted lower alkyl, or either R.sup.7 or R.sup.8 are --COOH or CO.N(R.sup.10).sub.2 or --COOR.sup.12, or R.sup.7 and R.sup.8 together comprise O;R.sup.12 is hydrogen, lower alkyl or substituted lower alkyl, aryl or substituted aryl;Z is S, O, NR.sup.13, NR.sup.13 NR.sup.13, NR.sup.13.CO.NR.sup.13, SO.sub.2, NR.sup.13 SO.sub.2 or S.dbd.O;R.sup.13 is hydrogen, lower alkyl or substituted lower alkyl, aryl or substituted aryl;wherein when Z is NR.sup.13, R.sup.7 and R.sup.8 do not together comprise an oxygen atom.