SYNTHETIC PEPTIDES THAT ANTAGONIZE NEUROKININ A, THEIR SALTS AND THEIR MANUFACTURING PROCESSES

摘要

Linear and cyclic synthetic peptides with the formula: X-Asp-Tyr-DTrp-Val-DTrp-DTrp-Y (I) where Y=A-R; A is one of the following amino acids: Lys, Orn, Glu, Gln, Asp, Asn, His, Ala, beta Ala, Val, Leu, Nle, Ile, Gly, Pro, Trp, Ser, Thr; R=NH2 (C-terminal carboxamide); X=H (free N-terminal amino group) or A is one of the following amino acids: Arg, Lys, Orn, Glu, Gln, Asp, Asn, His, Ala, beta Ala, Val, Leu, Nle, Ile, Gly, Pro, Phe, Trp, DTrp, Tyr, Met, Ser, Thr; when R and X together constitute an amide bond that joins together the two ends of the peptide chain to give a cyclic peptide; and their pharmaceutically acceptable salts with organic and inorganic acids or bases. These compounds are competitive antagonists of neurokinin A and are highly selective for the NK-2 receptor.