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US 5,491,217 AGranted
LHRH antagonists having modified aminoacyl residues at positions 5 and 6
AssigneeTAP Holding Inc.
InventorsFortuna Haviv, Jonathan Greer, Rolf E. Swenson, Daryl R. Sauer
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Abstract
A class of potent LHRH decapeptide antagonists possess N-alkylated aminoacyl residues where the side-chain portion of the residue is a 4-(substimtedamino)phenylalanyl, 4-(substituted-amino)cyclohexylalanyl, or .OMEGA.-(substitutedamino)alkyl group, and additionally the aminoacyl residues at position 5 are N-alkylated on the nitrogen atom of the peptide backbone.
Claims3
A compound or pharmaceutically acceptable salt thereof selected from the group consisting of
- NAc--D-2Nal --D-4ClPhe--D-3Pal--Ser--NMe--(4-Atza)Phe--D--(4-Atza)Phe--Leu--Lys(Isp)-- Pro--D--AlaNH.sub.2 ;
- NAc--D2Nal--D4ClPhe--D3Pal--Ser--NMe(4-Atza)Phe--DLys(Nic)--Leu--Lys(Isp)-- Pro--D--AlaNH.sub.2 ;
- NAc--D-2Nal--D--4ClPhe--D-3-Pal--Ser--NMeTyr--D--(4-Atza)Phe--Leu--Lys(Isp) --Pro--D--AlaNH.sub.2.
Dependencies are inferred from the claim text.