Patent number: 5550212
Abstract: Synthetic analogues of hGH-RH(1-29)NH.sub.2 having substitutions of various amino acids and acylated at the N-terminus, and exhibiting prolonged antagonistic duration. Embodiments include analogues of the formula: ##STR1## wherein X is nil, H, Ac, IAc, BrProp, Ibu, Nac, 2-Nac, 1- or 2-Npt, 1- or 2-Npr or Aqc; R.sup.1 is Tyr, His, Glu or Glt; R.sup.2 is D-Arg, D-Cit, D-Har, D-Lys or D-Orn; R.sup.3 is Asp, Ala or Gly; R.sup.4 is Ala or Gly; R.sup.5 is Ile, Ala or Gly; R.sup.6 is Phe, Ala, Pro, Tpi, Nal or Phe(Y), in which Y is F, Cl, Br, NO.sub.2, CH.sub.3 or OCH.sub.3 ; R.sup.8 is Asn, Ser, Val, Ile, Ala, Abu, Nle, or Aib; R.sup.11 is Arg, D-Arg or Cit; R.sup.12 is Lys, D-Lys, Cit or Ala; R.sup.15 is Gly, Ala, Abu or Gln; R.sup.19 is Ala or Abu; R.sup.20 is Arg, D-Arg or Cit; R.sup.21 is Lys, D-Lys or Cit; R.sup.27 is Met, Nle or Abu; R.sup.28 is Ser, Asn, Asp or Abu; R.sup.29 is Agm, Arg-NH.sub.2, Arg-OH, Cit-NH.sub.2, Cit-OH, Har-NH.sub.2 or Har-OH; provided that when R.sup.
Type:
Grant
Filed:
December 17, 1993
Date of Patent:
August 27, 1996
Assignee:
The Administrators of the Tulane Educational Fund
Inventors:
Marta Zarandi, Andrew V. Schally