HEPTAPEPTIDE OXYTOCIN ANALOGUES

摘要

HEPTAPEPTIDE ANALOGUES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF CONSIST OF A HEXAPEPTIDE MOIETY S AND A C-TERMINAL BETA-AMINOALCOHOL RESIDUE Z BOUND TO THE MOIETY S BY AN AMIDE BOND, WHEREIN THE BETA-AMINOALCOHOL Z IS -NR-CH (Q) -CH₂OH, Q IS (CH2)N-NH-A, N IS 1-6 AND A IS H OR -C (=NH)NH₂, AND R IS CH₃ OR C₂H5, AND THE MOIETY S IS MPA-X-ILE-Y-ASN-ABU- WHEREIN X IS A D-AROMATIC ALPHA-AMINOACID AND Y IS AN ALIPHATIC ALPHA-AMINOACID, AND HAVE OXYTOCIN ANTAGONIST ACTIVITY. ALSO DISCLOSED IS: A METHOD OF THEIR SYNTHESIS; PHARMACEUTICAL COMPOSITIONS CONTAINING THESE ANALOGUES; THE SYNTHESIS OF SUCH COMPOSITIONS; A METHOD OF CONTROL OF UTERINE CONTRACTIONS.