Cyclic anticoagulant peptides

Claim 1

A peptide derivative of the formula 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 - butyloxycarbonyl; A 1 is a bond or is a peptide containing from 1 to 5 residues of any amino acid; A 2 is Phe, SubPhe, β-(2- and 3-thienyl)alanine, β-(2- and 3-furanyl)alanine, β-(2-, 3-, and 4-pyridyl)-alanine, β-(benzothienyl-2- and 3-yl)alanine, β-(1- and 2-naphthyl)alanine, Tyr, or Trp; A3 is Glu or Asp; As is lie, Val, Leu, Nle, or Thr; As is Pro, Hyp, 3,4-dehydroPro, thiazolidine-4-carboxylate, Sar, NMePgl, or any amino acids having a D-configuration; As is Glu or Asp; As is a lipophilic amino acid selected from Tyr, Tyr(SO 3 H), Trp, Phe, Leu, Nle, Ile, Val, His, and Pro or is a dipeptide containing at least one of these lipophilic amino acids; A 1 o is a bond or is a peptide fragment containing from one to five residues of any amino acid; Y is a carboxy terminal residue selected from OH, (C 1 -C 6 )alkoxy, amino, mono- or di-(C 1 -C 4 )alkyl substituted amino, or benzylamino; R, R , Ri, and R 1 ' are each selected from a hydrogen or (C 1 -C 4 )alkyl group; B is selected from -S-, -S-S-, or -S-Alk 3 -S-; Alki, Alk 2 , and Alk 3 are each selected from a (C 1 -C 8 )methylene or ethylene group; and wherein "D" and "L" indicate that the stereochemistry of the indicated carbon is that corresponding to D-cysteine and L-cysteine, respectively, as well as a dimer or a mixture of a peptide derivative and the dimer thereof and their pharmaceutically acceptable salts.