Gonadoliberin antagonists

Details Gonadoliberin antagonists Gonadoliberin antagonists

1993-11-12

1995-07-18

Warden, Jill

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530313, 530328, A61K 3800, C07K 700, C07K 723

Patent

active

054341388

ABSTRACT:
Peptides of the formula ##STR1## in which X is alkanoyl, A is optionally substituted D-Nal(2), D-Phe or D-Trp, B is optionally substituted D-Phe, C is D-Pal(3) or optionally substituted D-Phe or D-Trp, and D is Tyr or His, E is D-Ser (R.sup.1), F is Leu, Trp or Phe, G is L-Ser(R.sup.1), H is Gly-NH.sub.2, D-Ala-NH.sub.2 or Azagly-NH.sub.2 and R.sup.1 is a glycosyl radical. These peptides have an inhibitory effect on the formation of the gonadotropins lutropin and follitropin and thus also on the synthesis of testo-sterone and estrogen. A process for the preparation of these peptides is described.

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Ljungqvist et al., "Design, Synthesis and Bioassays of Antagonists of LHRH Which Have High Antiovulatory Activity and Release Negligible Histamine", Biochemical and Biophysical Research Communications, 148, 849-856 (1987).
European Search Report.

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