| 摘要 |
This invention relates to peptide derivatives which are useful anticoagulant agents. These peptides have the formula X-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-Y wherein X is an amino terminal residue selected from hydrogen, one or two alkyl groups of from 1 to 6 carbon atoms, one or two acyl groups of from 2 to 10 carbon atoms, carbobenzyloxy or t-butyloxy carbonyl; A1 is a bond or is a peptide containing from 1 to 5 residues of any amino acid; A2 is Phe, SubPhe, beta -(2- and 3-thienyl)alanine, beta -(2-and 3-furanyl)alanine, beta -(2-, 3-, and 4-pyridyl)alanine, beta -(benzothienyl-2- and 3-yl)alanine, beta -(1- and 2-naphthyl)alanine, Tyr or Trp;. A3 is Glu or Asp; A4 is any amino acid; A5 is Ile, Val, Leu, Nle, or Thr; A6 is Pro, Hyp, 3,4-dehydroPro, thiazolidine-4-carboxylate, Sar, NMePgl or any amino acids having a D-configuration; A7 is any amino acid; A8 is Glu or Asp; A9 is a lipophilic amino acid selected from Tyr, Tyr(SO3H), Trp, Phe, Leu, Nle, Ile, Val, His and Pro or is a dipeptide containing at least one of these lipophilic amino acids; A10 is a bond or is a peptide fragment containing from one to five residues of any amino acid; and Y is a carboxy terminal residue selected from OH, C1-C6 alkoxy, amino, mono- or di(C1-C4) alkyl substituted amino, or benzylamino; and are useful anticoagulant agents. |
