TH11535A - Polypeptide components that secrete growth hormones. - Google Patents

Abstract

A novel polypeptide that increases GH secretion when administered to animals has been revealed. This polypeptide has the formula Al-D raised to the power of B-Nal-A3-Trp-A5-A6-Z or AWlQ-DPhe-A3-Trp-A5-A6-Z.

Claims (31)

1. A peptide with the formula A1-A2-A3-Trp-A5-A6-Z. A1 is His, 3(NMe) His, His-Tyr, Ao-His or Ao-3. (NMe) His, where Ao is a naturally occurring L-amino acid. Met (O), DOPA, Abu or peptides of the formula L-Ao, where L is H, DOPA, Lys, Phe, Tyr, Cys, Tyr-DAla-Phe-Cly, Tyr- Cly-Phe, Tyr-Ala-Cly-Thr Tyr-DAla-Phe-Sar; A2 is D raised to the power of B. Nal or DPhe, A3 is Ala, Cly, or Ser. A5 is Drhe, D/L raised to the power of B (Me) phe or (NMe)DPhe, A6 is B-G or G, where B is any L-amino acid. A naturally occurring dipeptide of any amino acid. climb Naturally occurring or H2N(CH2)nCO2H (where N=2-12) And G is Arg, iLys, or Orn. Z represents the C-terminated group of a polypeptide. As mentioned, or one or more amino acids with a C-terminal. plus The term "terminus" is used where Z is -CONR². -COOR to the power of 1, CH2OR to the power of 1, -Cly-Z, -Met-Z, -Lys-Z'', -Cys-Z'',-Gly-Tyr-Z'' or -Ala-Tyr-Z''m Where R to the power of 1 is H, an alkyl group containing carbon atoms 1-6. Atom, cycloalkyl group containing 3-8 carbon atoms, Al group. Kilyl groups containing 2-8 atoms, or aryyl groups containing 6-12 carbon atoms. An atom R squared is the same as R one and may... Are they the same or different? And organic or inorganic salts that are accepted in pharmaceuticals. Of any of the aforementioned polypeptides. 2. The peptide as stated in claim 1, where Al is His, Ala, His-Ala or Ao-His. 3. The peptide as stated in claim 1, where A3 is Ala. 4. The peptide as stated in claim 2, where Ao is Ala, Lys, or Giu; A3 is Ala; A6 is Lys, iLys, Ala-Lys, Ala-Ala-Lys or H2N (CH2)n, CO-Lys, where n'' is 4-8. 5. The peptide as stated in claim 1, where A2 is DBNal. 6. The peptide as described in claim 1, with the formula... His-DBNal-Ala-Trp-Dphe-A6-Z. 7. The peptide is as stated in claim 1, where A2 is DPhe. 8. The peptide as described in claim 6, with the formula... His-DBNal-Ala-Trp-Dphe-Lys-NH2. 9. The peptide as described in claim 1, with the formula... AO-His- DBNal-Ala-Trp-Dphe-A6-Z. AO-His-DPhe- Ala-Trp-Dphe-A6-Z. 10. The peptide is as stated in claim 9, where Ao is Ala. 11. Any one of the peptides listed in claims 6, 9, 18, or 20. where Z in -CONH2 12. The peptide as stated in claim 12, with the formula... Ala-His-DPhe- Ala-Trp-Dphe-Lys-NH2. Ala-His- DBNal-Ala-Trp-Dphe- Lys-NH2 Ala-His-DPhe- Ala-Trp-Dphe-Ala-Lys-NH2, Ala-His-DPhe- Ala-Trp-Dphe-Ala- Ala-Lys-NH2, Lys- His-DPhe- Ala-Trp-Dphe-A6- NH2, or Glu- His-DPhe- Ala-Trp-Dphe-A6- NH2, 13. Which of the peptides listed in claims 2, 6, 9, 18, or 20 is valid? One, where A6 is G. 14. The peptide as stated in claim 8, with the formula... Ala-His-DPhe- Ala-Trp-Dphe-Lys-NH2. Ala-His-DPhe- Ala-Trp-Dphe-Ala- Ala-Lys-NH2 Lys- His-DPhe- Ala-Trp-Dphe-A6- NH2, or Glu- His-DPhe- Ala-Trp-Dphe-A6- NH2 15. The peptide as described in Claim 1, with the formula... His- Ala-DPhe- Ala-Trp-Dphe-A6-Z- 16. The peptide as stated in claim 15, where Z is -CONH2Z. -CONH2 17. The peptide as stated in claim 16, with the formula... His- His-DPhe- Ala-Trp-Dphe- Lys-NH2 18. The peptide as stated in claim 1, with the formula... His- -DPhe- Ala-Trp-Dphe-A6-Z- 19. The peptide as stated in claim 18, with the formula... His- -DPhe- Ala-Trp-Dphe-Lys-NH2 20. The peptide as stated in claim 1, with the formula... Ala-DPhe- Ala-Trp-Dphe-A6-Z- or Ala-DPhe- Ala-Trp-Dphe-A6-Z- 21. The peptide as stated in claim 20 has the formula... Ala-DBNal-Ala-Trp-DPhe-Lys-NH2 or Ala-DPhe-Ala-Trp-DPhe-Lys-NH2 22. Methods to increase the secretion of growth hormone. In animals, this involves administering the animal the specified amount. The effects of at least one peptide are included in the claim. 1, 4, 5, 7, 9, 12, 14, or 15 23. Method of claim 21 in which the animal is. mammals 24. Method of claim 21 in which the animal is. human 25. Pharmaceutical components for increasing hormone secretion levels. Controlling growth in animals that consist of at least... At one of the superpeptides of claims 1, 4, 5, 7, 9, 12, 14, or 15. And pharmaceutically acceptable carriers or diluents. 26. The peptide is stated in claim 2, where Ao is an amino acid. those that occur naturally 27. Methods to increase hormone levels that regulate hormonal imbalances. Growth is selectively achieved by providing a percentage of claim 1. The dosage has a synergistic effect with the second compound, where the second compound... These two compounds act as agonists on hormone receptors. The secretion of growth hormones or the inhibition of the effects of soma. Tostatin 28. The pharmaceutical components of claim 22, which also include: With a second compound acting as an agonist on the receptor. Hormone secretion controls growth or inhibits its effects. of somatostatin 29. Using compounds in formulas. In the place where Al-A2-A3-Trp-A5-A6-Z Al is HIS, 3(NMe) His,His-Ala,Ala-Tyr, Ao-His Or Ao-3(NMe)His, where Ao is the L-amino acid produced. Naturally Met(O), DOPA, Abu, or peptides of the formula L-Ao, where L is H, DOPA,Lys,Phe,Tyr,Cys,Tyr-DAla-Phe-Gly, Tyr-DAla-Gly-Phe,Tyr-Ala-Gly-Thr or Tyr-DAla-Phe-Sar; A2 stands for DBNal or DPhe. A3 is Ala, Gly, or Ser. A5 is DPhe, D/LB(Me)Phe or (NMe) DPhe, A6 is B-G or G. In the production of pharmaceuticals for increasing secretion and raising levels. Growth hormone in the blood. 30. Processes for preparing compound formulas. AL-A2-A3-Trp-A5-A6-Z Al is His, 3(NMe)His, His-Ala,Ala-Tyr, Ao-His, Or Ao3(NMe)His, where Ao is the L-amino acid that follows. nature Met (0), DOPA, Abu or peptides of the formula L-Ao where L is H DOPA,Lys,Phe,Tyr,Cys,Tyr-DAla-Phe-Gly,Tyr-DAla-Gly-Phe ,Tyr-Ala-Cly-Thr or Tyr-DAla-Phe-Sar; A2 stands for DBNal or DPhe. A3 is Ala, Gly, or Ser. A5 is DPhe, D/LB(Me)Phe or (NMe) DPhe, A6 is B-G or G. This consists of amino acid pairs or amino acid derivatives. In order to form the said compound. 31. The process for preparing the peptide of claim 1, which... It consists of the condensation reaction of the peptide portion to form peptides. The said Tide (31 claims, 5 pages, - image)