TH1762A - Synthetic peptides showing growth hormone-releasing activity of pituitary - Google Patents

Abstract

Process for producing peptides Which consists of the amino acids being components together to form peptides in sequence Of the amino acids selected from the group consisting of (chemical formula). In addition, this invention also includes a process for producing mixtures. Of various compounds Containing (a) peptides, which have at least one type of formula III (chemical formula). In addition, this invention also includes a process for producing mixtures. Which contains at least the types of peptides mentioned above One with at least one type of growth aid, peptides, and these mixtures show direct action on the pituitary gland. Oval made the release of growth hormone from the gland.

Claims (3)

1. Peptides with formulas (chemical formulas) where X1, X2 and X3 are selected from groups containing N-terminal and des amino substitutions. Alpha-Carbon a and b are 0 or 1, whose terms a and b are 0 when A1 is the fraction of des amino; A1 and A4.Choose from groups containing His, Arg, Lys, (Formula) -Naphth, (Formula) -Naphth, Iql, Tyr, Trp, Phe, Homologs and analogues of these groups, and, Specific. A1, the de-amino form of these groups; A2 and A5 are selected from the group consisting of D-Mis, D-Arg, D-Lys, D- (Formula) -nAPHTH, D- (Formula) -Naphth, D-Iql, D-Tyr, D-Trp, D-. Phe, the homolog and its analogues of these groups, and, only A5, the decarlox form of these groups; A3 Choose from groups that include Gly, Ala, Val, Leu, Ile, Pro, Ser, Thr, Met, Asp, Glu, Asn, Gln, His, D-Ala, D-Val, D-Lue, D-Ile, D-Pro, D-Ser, D-Thr, D-Met, D-Asp, D-Glu, D-Asn, D-Gln, D-His, and the homolog and analogues of these groups; And Y is selected from a group that contains a group instead of a C-terminal and a descarboxy. Alpha - carbon; And salts of these substances, which are acceptable in pharmacy There is a requirement when (1) a is 1 and b is 0, and X1 and X2 are selected from a group containing -H and -CH3; (2) A1 and A4 are selected from the group consisting of Tyr, Trp and Phe; (3) A3. Choose from groups including Gly, Ala, Val, Leu, Ile, Pro, Ser, Thr, Met, Asp, Glu, Asn, Gln, and His; And (4) selects from groups containing -NR1R2, and -OR, where R, R1 and R2 are selected from hydrogen and alkyl groups. Where there are 1-6 carbon atoms with branches and without branches; Then A2 and A5 at least one option, not from the group. Containing D-Tyr, D-Trp, D-Phe, and, only A5, a decarboxy image of these groups; And when (1) a is 1 and b is 0, and X1 and X2 select from group containing -H and -CH3; (2) A2 and A5 select from group containing -H and -CH3; (2) A2 and A5. Choose from a group consisting of D-Tyr, D-Trp, D-Phe, and, only A5, the starbox image of these groups; (3) A3 selects from groups including Gly, Ala, Val, Leu, Ile, Pro, Ser, Thr, Met, Asp, Glu, Asn, Gln, and His; And (4) Y selects from groups containing -NR1R2, -CH2OR, and -OR, which R, R1 and R2 are selected from those composed of hydrogen and alkyl groups with 1-6 carbon branched atoms. And without branching; Then at least one A1 and A4 were chosen without Derived from a group consisting of Tyr, Trp, and Phe; 2. Peptide of claim 1, where a is 0 or 1 and b is 0; X1 and X2 are selected from the group that includes -R, -OR, And RC (0) -, where R chooses from the hydrogen group and the group Branched and non-branched alkyls with 1-6 carbon atoms A1 and A4 were selected from groups containing His, Tyr, Trp, Phe, homolog and their analogues, only A1 form. Des amino of those groups A2 and A5 select from a group consisting of D-His, D-Tyr, D-Trp, D-phe, homolog and their analogues, and only A5, de These squad carboxes A3 is selected from a group consisting of Gly, Ala, Ser, Asn, Pro, D-Ala, D-Ser, D-Asn, D-Pro, and the homolog and its analogues. Those Y were selected from the groups containing -CH2OH, -OR and -NR1R2, where R, R1 and R2 were selected from those containing hydrogen and Branched or unbranched alkyl groups with 1-6 carbon atoms and their salts, which are acceptable in pharmacology. 3. The peptide of Clause 1 has the formula. (Chemical formula) where a is 0 or 1. X2 Select from the RCO and R- group, where R is selected from the Hydrogen group and 1-2 Carbon Alkyl groups; A1 Selects from the Tyr group. , O-Me-Tyr, His, 3-N-Me-His, P-Cl-Phe, and their amino case figure A3. Select from group that includes Ala, Ser, and D-Ala A4. Select from the group. Which consists of Trp, Tyr, A5 Select from a group that consists of D-Phe, D-His, D-Tyr and Dp-Cl-Phe Y Select from group that includes -OR, and -NHR, which R is selected from the group that includes Hydrogen and alkyl groups with 1-2 carons and salts of those substances, which are Clause 1 Claim Peptide contains Formula H2-His-D-Trp-Ala-Trp-D-Phe-NH2 5. Clause 1 Claim Peptide Contains formula H2-Tyr-D-Trp-Ala-Trp-D-His-NH2 6. Clause 1 Peptide contains formula H2-His-D-Trp-Ala-Trp-D-His. Clause 1 Clause 1 Peptide contains formula H2-His-D-Trp-Ala-Trp-D-Tvr-NH2 8. Clause 1 Clause Peptide contains Formula H2-His-D-Trp-Ala-Trp-Dp-Cl-Phe-NH2 9. Peptide of Clause 1 has formula H2-Tyr-D-Ala-Trp-Trp-D- Phe-NH2 1 0. Cl-Phe-D-Phe-D-Trp-Ala-Trp-D-PheNH2 1 Peptide 1 1. Clause 1 Peptide contains the formula H-desamino Tyr-D-Trp-Ala-Trp-D-PheNH2 1. 2. Clause 1 Peptide, which has the formula CH3CO -Tyr-D-Trp-Ala-Trp-D-PheNH2 1. 3. Clause 1 claim peptide contains formula H2 O-Me-Tyr-D-Trp-Ala-Trp-D-PheNH2 (13 claims, 5 pages, 0 photos).