GNRH antagonist betides

Details GNRH antagonist betides GNRH antagonist betides

1996-02-08

1998-09-15

Tsang, Cecilia J.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Lutenizing hormone releasing factor ; related peptides

530328, 514 15, C07K 723

Patent

active

058079831

ABSTRACT:
Betides having at least one betidamino acid are provided which have GnRH antagonistic properties. These antagonists may be used to regulate fertility and to treat steroid-dependent tumors, such as prostatic and mammary tumors. One particularly effective betide, which is an analog of the decapeptide GnRH that is highly soluble in water at physiologic pH, has the formula: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-Aph(acetyl)-D-Aph(acetyl)-Leu-D/L-Agl(methyl,i sopropyl .beta.-alanyl)-Pro-D-Ala-NH.sub.2, and another has the formula Ac-D-2Nal-D-Cpa-D-3Pal-D/L-Agl(For)-Aph(Ac)-D-Aph(Ac)-Leu-ILys-Pro-D-Ala-N H.sub.2.

REFERENCES:
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patent: 5296468 (1994-03-01), Hoeger et al.
patent: 5506207 (1996-04-01), Rivier et al.
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Abstract, Rivier et al., "Betidamino Acids: Versatile and Constrined Scaffolds for Drug Discovery", L020, 14th American Peptide Symposium, Columbus, Ohio (Jun. 18-23, 1995).
Bock et al., "Differentially Protected Alpha-Aminoglycine", J. Org. Chem. 1986, vol. 51, pp. 3718-3720.
Abstract, Koerber et al., "Solvation Energy Effects on the Conformation of Normal and Methylated Peptides and Betides", P505, 14th American Peptide Symposium, Columbus, Ohio (Jun. 18-23, 1995).
Abstract, Rivier et al., "Betidamino Acids: Versatile and Constrained Scaffolds for Drug Discovery", L020, 14th American Peptide Symposium, Columbus, Ohio (Jun. 18-23, 1995).
Abstract, Rivier et al., "Betidamino Acids: Versatile and Constrained Novel Scaffolds for Drug Discovery", Western Biotech Conference (Oct. 18-21, 1995).

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