Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1994-03-18
1996-04-09
Warden, Jill
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
530328, A61K 3804, C07K 700
Patent
active
055062075
ABSTRACT:
Analogs of the decapeptide GnRH which include two significantly modified amino acids at positions 5 and 6 inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads and may be used to treat steroid-dependent tumors. Particularly effective peptides which are soluble in water at physiologic pH and which have a low tendency to gel when administered in vivo have the following formula:
REFERENCES:
patent: 4444759 (1984-04-01), Rivier et al.
patent: 4619914 (1986-10-01), Vale et al.
patent: 5169932 (1992-12-01), Hoeger et al.
patent: 5296468 (1994-03-01), Hoeger et al.
Dayhoff, Atlas of Protein Sequence and Structure, 1972, vol. 5, (see last page).
Moimas et al., "A New Approach to 1-Nitro-2,2-bis[alkyl-or arylamino]ethylenes: A New Synthesis of Ranitidine", Communications, pp. 509-510, May 1985.
Rivier et al., "Novel Linear and Cyclic Gonadotropin Releasing Hormone Antagonists:", 26.sup.es Recontres Internationales de Chimie Therapeutique, Univ. of Montpellier, Montpellier, France, Jul. 3-5, 1990.
Rao et al., "Synthesis of cis and trans-4-Aminocyclohexyl-D-Alanine Derivatives and Determination of their Stereochemistry", Organic Preparations and Procedures Inc., 23(1), pp. 103-110, 1991.
Rivier et al., "Gonadotropin Releasing Hormone Antagonists: Novel Structures Incorporating N.sup..omega. -Cyano Modified Guanidine Moieties", Biochemical and Biophysical Research Communications, vol. 176, No. 1, pp. 406-412, Apr. 15, 1991.
Rivier et al., "Gonadotropin-Releasing Hormone Antagonists with N.sup..omega. -Triazolylornithine, -lysine, or -p-aminophenylalanine Residues at Positions 5 and 6", Journal of Medicinal Chemistry, pp. 4270-4278, 1992, 35.
Theobald et al., "General Method for Incorporation of Modified N.sup..omega. -Cyanoguanidino Moeities on Selected Amino Functions during Solid-Phase Peptide Synthesis", J. Am. Chem. Soc., 112, pp. 9624-9626, 1990.
Theobald et al., "Novel Gonadotropin-Releasing Horomone Antagonists: Peptides Incorporating Modified N.sup..omega. -Cyanoguanidino Moieties", Journal of Medicinal Chemistry, pp. 2395-2402, 1991, 34.
Hoeger Carl A.
Jiang Guangcheng
Porter John S.
Rivier Catherine L.
Rivier Jean E. F.
Prickril Benet
The Salk Institute for Biological Studies
Warden Jill
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