Analogs of gonadoliberin with improved solubility, methods for t

Details Analogs of gonadoliberin with improved solubility, methods for t Analogs of gonadoliberin with improved solubility, methods for t

1991-06-28

1992-02-25

Lee, Lester L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530313, 530328, 514800, A61K 3702, A61K 3743, C07K 706, C07K 720

Patent

active

050913670

ABSTRACT:
The invention relates to peptides of the formula ##STR1## in which X is absent or is hydrogen or acyl; A is Pgl, de-hydro-Pro, Pro, D-Thi or D-Pgl or represents optionally substituted D-Nal(2), D-Phe or D-Trp; B is His or optionally substituted D-Phe; C is Trp, D-Thi, D-Pal(3) or optionally substituted D-Trp; D is Tyr, Arg of His; E is D-Ser(R.sup.1), .beta.-Asn, .beta.-Asp-OMe, D-Thi or --NH--CH(CH.sub.2 R.sup.2)--CO--; F is Ser(R.sup.1), Leu, Trp or Phe; G is Gly-NH.sub.2, Aza-Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-alkyl; R.sup.1 is glycosyl and R.sup.2 is hydrogen, acyl, aryl or heteroaryl.
The invention also relates to methods for the preparation of these peptides, agents containing them and their use.

REFERENCES:
patent: 4472382 (1984-09-01), Labrie et al.
patent: 4728640 (1988-03-01), Labrie et al.
Chem. Abstr., vol. 110, 58099v (1989).
Synthesis of a Glycotripeptide and a Glycosomatostatin Containing the 3-O-(2-Acetamido-2-Deoxy-.beta.-D-Glucopyranosyl)-L-Serine Residue.

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