Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1993-01-21
1994-03-22
Cashion, Jr., Merrell C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514 2, 514800, 530313, 530328, 930110, 930DIG803, 930DIG801, 930DIG800, A61K 3738, C07K 720, C07K 706
Patent
active
052964680
ABSTRACT:
Peptides which include unnatural amino acids and which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such peptides that are GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The antagonists may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions. Such unnatural amino acids are useful in the synthesis of peptides and have the formula U.sup.* : ##STR1## where W is (CH.sub.2).sub.n or ##STR2## n is an integer from 1 to 6; and j=1, 2 or 3. Preferably, either Y is N--CN, X is NH and R.sub.2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pridyl or ##STR3## where R.sub.11 is H or acyl.
REFERENCES:
patent: 4935491 (1990-06-01), Folkers et al.
patent: 5110904 (1992-05-01), Howiv et al.
Theobald et al., "General Method for incorporation of modified N.omega.-cyanoguanidino moieties on selected amino functions during solid-phase peptide synthesis," J. Am. Chem. Soc., 112(26):9624-9626 (1990).
Rivier et al., "Gonadotropin releasing hormone antagonists: Novel structures incorporating N.sup..omega. -cyano modified guanidine moieties," Biochem. and Biophys. Research Comm., 176(1):406-412 (1991).
Theobald et al., "Novel Gonadotropin-releasing hormone antagonists: Peptides incorporating modified N.omega.-cyanoguandino moieties", J. Med. Chem., 34(8):2395-2402 (1991).
Rivier et al., "Gonadotropin-releasing hormone antagonists with N.sup..omega. -triazolylornithine, -lysine, or -p-aminophenylalanine residues at positions 5 and 6", J. Med. Chem., 35(23):4270-4278 (1992).
Coy et al., Endocorianology, vol. 110, No. 4, pp. 1445-1447, (1982).
Hoeger Carl A.
Porter John S.
Rivier Catherine L.
Rivier Jean E. F.
Theobald Paula G.
Cashion Jr. Merrell C.
The Salk Institute for Biological Studies
Wessendorf T. D.
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