nonapeptid - and decapeptide lhrh analogue of the lhrh antagonists serve.

摘要

Peptides of formula (I) and pharmaceutically acceptable salts are new: A-B-C-Ser-D-E-F-G-Pro-J (I) where A= aminoacyl from D- or L- isomers of: N-Ac-D,L- delta (3,4)-Pro, N-Ac-D,L-Pro, N-Ac-D,L-Phe, N-Ac-D,L- Pcl-Phe, N-Ac-D,L-PF-Phe, N-Ac-3-(1-naphthyl)-D,L-Ala, N-Ac-3-(2-naphthyl)-D,L-Ala and N-Ac-3-(2,4,6-trimethylphenyl)-D,L-Ala; B = D-Phe, D-Pcl-Phe, D-PF-Phe, D-PNO2-Phe, 2,2-diphenylglycyl, D-alpha-methyl-P-cl-Phe or 3-(2-naphthyl)-D-Ala; C= D-Trp, D-Phe, 3-(3-pyridyl)-D-Ala or 3-(2-naphthyl)-D-Ala; D= L-Phe, L-Tyr, 3-(3-pyridyl)-Ala, Arg or G; E= 3-(2-naphthyl)-D-Ala, 3-(3-pyridyl)-D-Ala, D-Tyr, D-Trp, D-nicotinyl-Lys, pyridylacetyl-Lys, D-Glu(AA) or G; F= L-Leu, L-Nle, L-Phe, L-Trp or 3-(2-naphthyl)-L-Ala; G = gp. of formula (IIa), (IIb) or (IIc); n = 1-5; R1 = 1-6C alkyl or fluoroalkyl; R2 = H or R1; or R1-NH-C=NR2 = ring of formula (IIIa), (IIIb) or (IIIc): m = 1-4; A = H or 1-6C alkyl; X = A or halogen; R3 = H, 1-6C alkyl, phenyl or phenyl-lower alkyl; J = D-Ala-NH2, D-Leu-NH2, Gly-NH2 or -NHR4; R4 = lower alkyl or -NHCONH2; D-On(AA) = anisole adduct to D-Glu to form a P-methoxy-phenylketone (at the carboxyl termius of the glutamic acid side chain), i.e. Glu (pMeO-Ph).