HEPTAPEPTIDE ANALOGS HAVING OXYTOCIN ANTAGONIST ACTIVITY, METHODS OF SYNTHESIS OF THE SAME, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND THE USE OF THE SAME IN THE MANUFACTURE OF MEDICAMENTS

摘要

A heptapeptide analogue, or a pharmaceutically acceptable salt thereof, having oxytocin antagonist activity and consisting of a b-aminoalcohol residue Z bound to the C-terminus of a hexapeptide moiety S by an amide bond, wherein Z is: wherein Q is (CH2)n-NH-A, n is 1-6 and A is H or C(=NH)NH2, and wherein R is CH3 or C2H5; and the moeity S is: Mpa-X-Ile-Y-Asn-Abu- wherein Mpa, Ile, Asn and Abu have the following meanings: Mpa3-mercaptopropionic acid residue Ileisoleucine residue Asnasparagine residue Abua-aminobutyric acid residue; and wherein X is a D-aromatic a-amino acid; and Y is an aliphatic a-amino acid.