Therapeutic LHRH analogs

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Lutenizing hormone releasing factor ; related peptides

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514800, C07K 720

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active

046329790

ABSTRACT:
A compound having the formula K-His-Trp-Ser-Tyr-M-Q-Arg-Pro-T, wherein K is N-Acetyl-Sarconsine or pGlu; is D-Phe, D-Trp, D-.beta.-Naphthylalanine, or D-4-X-Phe, wherein X is OH, F, Cl, Br, or Me; Q is Leu, Phe, 4-X-Phe, Trp, or .beta.-Naphthylamine (wherein X is OH, F, Cl, Br, or Me), or an N-Me-derivative thereof; and T is Gly-NH.sub.2, NHCH.sub.3, NHCH.sub.2 CH.sub.3, or NHCH.sub.2 CH.sub.2 CH.sub.3 ; provided that, when Q is Leu or N-Me-Leu, K cannot be pGlu; or a pharmaceutically acceptable salt thereof.

REFERENCES:
patent: 4010125 (1977-03-01), Schally
patent: 4010149 (1977-03-01), Baba et al.
patent: 4018726 (1977-04-01), Schally et al.
patent: 4034082 (1977-07-01), Johnson et al.
patent: 4071622 (1978-01-01), Johnson
patent: 4218439 (1980-08-01), Rivier
patent: 4234571 (1980-11-01), Nestor et al.
patent: 4321260 (1982-03-01), Auclair
Schally (1971) Biochem. Biophys. Res. Comm. 43: 393, 1334.
Tolis (1982) PNAS 79: 1658-1662.
Borgmann, The Lancet, May 15, 1982, pp. 1097-1099.
Redding (1982) PNAS 79: 1273-1276.

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