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Nona-deca-peptides and peptide analogs of a manufacturing method Lhrh

机译:制造方法Lhrh的九碳十肽和肽类似物

摘要

Nonapeptide and decapeptide analogs of LHRH which have the formula IMAGE and the pharmaceutically acceptable salts thereof, wherein: A is an amino acyl residue selected from the group consisting of L-pyroglutamyl, D-pyroglutamyl, N-acyl-D,L-tryptophanyl, N-acyl-glycyl, N-Ac-D,L- DELTA 3,4-prolyl, N-Ac-D,L-prolyl, N-Ac-L-alkylprolyl, N-Ac-D,L-phenylalanyl, N-Ac-D,L-p-chlorophenylalanyl, N-Ac-D,L-seryl, N-Ac-D,L-threonyl, N-Ac-D,L-alanyl, 3-(1-naphthyl)-D,L-alanyl, 3-(2-naphthyl)-D,L-alanyl, 3-(2,4,6-trimethylphenyl)-D,L-alanyl, 3-(4-trifluoromethylphenyl)-D,L-alanyl, 3-(9-anthryl)-D,L-alanyl, 3-(2-fluorenyl)-D,L-alanyl, and 3-(Het)-D,L-alanyl wherein Het is a heterocyclic aryl containing radical selected from CHEM wherein A sec and A min are independently selected from the group consisting of hydrogen, lower alkyl, chlorine and bromine, and G is selected from the group consisting of oxygen, nitrogen and sulfur; B is an amino acyl residue selected from the group consisting of D-phenylalanyl, D-p-Cl-phenylalanyl, D-p-F-phenylalanyl, D-p-nitrophenylalanyl, 3-(3,4,5-trimethoxyphenyl)-D-alanyl, 2,2-diphenylglycine, D- alpha -methyl-p-Cl-phenylalanine and 3-(2,4,6-trimethylphenyl)-D-alanyl; C is an amino acyl residue selected from the group consisting of L-tryptophanyl, D-tryptophanyl, D-phenylalanyl, D-Me5phenylalanyl, 3-(2-pyridyl)-D-alanyl, 3-(-3-pyridyl)D-alanyl, 3-(1-naphthyl)-D-alanyl, 3-(2-naphthyl)-D-alanyl and 3-(4-pyridyl)-D-alanyl. D is an amino acyl residue selected from the group consisting of L-seryl, and D-alanyl; E is an amino acyl residue selected from the group consisting of L-phenylalanyl and L-tyrosyl; F is an amino acyl selected from the group consisting of the radicals represented by the following structural formulas:
机译:具有式的LHRH的九肽和十肽类似物及其药学上可接受的盐,其中:A是选自L-焦谷氨酰基,D-焦谷氨酰基,N-酰基-D,L-的氨基酰基残基色氨酸,N-酰基-糖基,N-Ac-D,L-DELTA 3、4-脯氨酰基,N-Ac-D,L-脯氨酰基,N-Ac-L-烷基脯氨酰基,N-Ac -D,L-苯丙氨酰基,N-Ac-D,Lp-氯苯丙氨酰基,N-Ac-D,L-seryl,N-Ac-D,L-苏氨酰基,N-Ac-D,L-丙氨酰基,3-( 1-萘基)-D,L-丙氨酰基,3-(2-萘基)-D,L-丙氨酰基,3-(2,4,6-三甲基苯基)-D,L-丙氨酰基,3-(4-三氟甲基苯基) -D,L-丙氨酰基,3-(9-蒽基)-D,L-丙氨酰基,3-(2-芴基)-D,L-丙氨酰基和3-(Het)-D,L-丙氨酰基,其中Het为选自的含杂环芳基的基团,其中A sec和A min独立地选自氢,低级烷基,氯和溴,且G选自氧,氮和硫。 B是选自以下的氨基酰基残基:D-苯丙酰基,Dp-C1-苯丙酰基,DpF-苯丙酰基,Dp-硝基苯丙酰基,3-(3,4,5-三甲氧基苯基)-D-丙酰基,2,2-二苯基甘氨酸,D-α-甲基-p-Cl-苯丙氨酸和3-(2,4,6-三甲基苯基)-D-丙氨酰基; C是选自以下的氨基酰基残基:L-色氨酸,D-色氨酸,D-苯丙酰基,D-Me 5苯丙酰基,3-(2-吡啶基)-D-丙酰基,3-(-3-吡啶基)D-丙氨酰基,3-(1-萘基)-D-丙氨酰基,3-(2-萘基)-D-丙氨酰基和3-(4-吡啶基)-D-丙氨酰基。 D是选自L-丝氨酸和D-丙氨酰基的氨基酰基残基; E是选自L-苯丙氨酰基和L-酪氨酰基的氨基酰基残基; F是选自以下结构式表示的基团的氨基酰基:

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