TH2215A - GRF analogues - Google Patents

Abstract

Synthetic peptides are very potent for stimulating pituitary GH secretion in mammals. This is because it is a model of The release factor (hormone) in the nature of the hypothalamus. The peptides of specific species are pigs, cows, goats and sheep. These peptides are in the following order: Try-Ala-Asp-Ala-Ile-Phe-The-Asn-Ser-Try-Arg-Lys-R13-Leu-Gly-Gln. -Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-R28-Arg-Gln-Gly-Glu-Arg-Asn-Gln-Glu-Glu-Gly-Ala-R41-Val -Arg-Leu where R13 is Val or Ile; R28 is Ser or Asn; And R41 is Arg or Lys-peptide or its bioactive parts or its analogues with known substitutions or additions or their non-toxic salts can be given to pets. Baby milk Or used in the diagnosis This peptide is very useful. This is especially true in stimulating GH secretion, which accelerates the growth of non-human or certain warm-blooded animals. And / or to improve aquaculture

Claims (9)

1. Process of compound preparation with formula (I), H-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-R13-Leu-Gly-Gln-Leu-Ser. -Ala-Arg-Lys-Leu-Leu-Gin-Asp-Ile-Met-R28-Arg-Gln-Gln-Gly-Glu-Arg-Asn-Gln-Glu-Gln-Gly-Ala-R41-Val-Arg -Leu-Y where R13 is Val or Ile, R28 is Ser or Asn; R41 is Arg or Lys; And y is OH or NH2. The preparation procedure consists of (a) preparing a compound with at least one protection group and the formula (II) X1-Tyr (X2) -Ala-Asp (X3) -Ala-Ile-Phe-. Thr (X4) -Asn-Ser (X5) - Try (X2) -Arg (X6) -Lys (X7) R-13-Leu-Gly-Gln-Leu-Ser (X5) -Ala- Arg (X6) - Lys (X7) -Leu-Leu-Gln-Asp (X3) -Ile-Met-R28 (X5) Arg (X6) -Gln-Gln-Gly-Glu (X3) -Arg (X6) -Asn-Glu (X3 - Gln-Gly-Ala-R41 (X6 or X7) -Val-Arg (X6) -Leu-X8 It is capable of eliminating any or all radicals from R28 to the carbon end where (X1), (X2), (X3), (X4), (X5), (X6) and (X7). Each group may be hydrogen or A protective group, and where (X8) can be an ammeter or hydroxy group Or protection group and (b) eliminate the protection group from the formula (II) to obtain the bioactive formulation peptide (I) or its fragment. And if desired (c) to convert the peptides into non-toxic salts. 2. The process mentioned in claim 1 where R28 is Asn and R41 is Lys. 3.The process is mentioned in claim 2, where R13 is Lle. 4.The process is mentioned in claim 2 where R13 is Val. 5. The process mentioned in claim 1 where R13 is Val, R28 is Ser and R41 is Arg. 6. The process mentioned in any of the claims 1 to 5, where Y is NH2. 7. That process in any of the claims 1 to 5, where Y is OH. 8.Such procedure in any of claims 1 to 7 where Y is hydrogen or alpha amino group protection group, X2 is hydrogen or phenolic hydroxy protective group. Tyr; X3 is hydrogen or Asp or Glu's carboxy defensive group; X4 is Hydrogen or Thr's hydroxy alcohol defense group; X5 is hydrogen or alcohol defense group. Ser hydroxy; X6 is the hydrogen or Lys lateral chain amino defense group; And X8 is selected from a group consisting of OH, OCH3, amethyst ester, hydrazide, -O-CH2-resin supports, and? NH-supported resin. 9. The process mentioned in claim 8 where X1 is BOC, X2 is 2,6 dichlorobenzyl, X3 is Bzl, X4 is Bzl, X5 is Bzl, X6 is Tos, X7 2- Chlorobane. The silicon carbonyl and X8 are -O-CH2- resin backed 1. 0. As mentioned in claim 8, X1 is BOC, X2 is 2,6-dichlorobenzyl, X3 is Bzl, X4 is Bzl, X5 is Bzl, X6 is Tos, X7 is 2-chloro. Robenzyl oxycarbonyl and X8 are -NH-resins.