Lh-rh antagonists

Details Lh-rh antagonists Lh-rh antagonists

C - Chemistry, Metallurgy

07

C

530/7.06

C07C 103/52 (1980.01)

Patent

CA 1181395

ABSTRACT OF THE DISCLOSURE Disclosed herein are peptide analogs of the luteinizing hormone releasing hormone (LH-RH) which are potent antagonist of LHRH. The analogs differ in structure from LH-RH by having different amino acid residues at positions 1, 2 and 6, and optionally at positions 3 and 10. Methods for preparing and using these analogs are described. The specification dis- closes compounds of this type, namely the LH-RH analogs represented by the formula I X-R1-R2-R3-Ser-Tyr-R4-Leu-Arg-Pro-R5-NH2 (I) in which X is hydrogen, lower alkanoyl, HOOC-(CH2)n-CO wherein n is an integer from 2 to 6, benzoyl or the acyl portion of glycine or a D- or L-amino acid; R1 is D-Trp, D-Phe or D-Phe having a substituent in the para position of the phenyl group selected from the group consisting of halo, nitro, amino, methyl, cyano, trifluoromethyl, hydroxy and methoxy; R2 is D-Phe having a substituent in the para position of the phenyl group selected Prom the group consisting of halo, nitro, amino, methyl, cyano, trifluoromethyl, hydroxy and methoxy; R3 is D-Trp, L-Trp or L-Phe; R4 is D-Trp, D-Phe or D-Phe having a substituent in the para position of the phenyl group selected from the group consisting of halo, nitro, amino, methyl, cyano, trifluoromethyl, hydroxy and methoxy; and R5 is Gly or D-Ala.

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