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Gip receptor activating peptide

A representative, optional technique, applied in the field of novel peptide compounds

Pending Publication Date: 2020-01-17
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the peptide compounds of the present invention and compounds having a selective activation effect on GIP receptors have not been disclosed

Method used

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  • Gip receptor activating peptide
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Examples

Experimental program
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preparation example Construction

[1062] Compound (I) can be produced according to a peptide synthesis method known per se. The peptide synthesis method may be, for example, any of a solid-phase synthesis process and a liquid-phase synthesis process. That is, the target peptide can be produced by repeatedly condensing a partial peptide or amino acid capable of constituting the compound (I) and the remainder (which may be composed of two or more amino acids) according to a desired sequence. When the product with the desired sequence has a protecting group, the target peptide can be produced by eliminating the protecting group. Examples of known condensation methods and elimination methods of protecting groups include the methods described in (1) to (5) below.

[1063] (1) M. Bodanszky and M.A. Ondetti: Peptide Synthesis, Interscience Publishers, New York (1966)

[1064] (2) Schroeder and Luebke: The Peptide, Academic Press, New York (1965)

[1065] (3) Nobuo Izumiya et al.: Peptide Gosei-no-Kiso to Jikken (B...

Embodiment 1

[1269] Synthesis of H-Tyr-Aib-Glu-Gly-Thr-Val-Val-Ser-Leu-Tyr-Ser-Ile-Aib-Leu-Asp-Lys-Gln-Ala-Gln-Aib-Glu-Phe-Val-Lys -Trp-Leu-Leu-Lys-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-Lys-NH2 (SEQ ID NO: 12) (Compound 6)

[1270] Weigh the H-Glu(OtBu)-Phe-Val-Lys(Boc)-Trp(Boc)-Leu-Leu-Lys(Boc)-Gly-Gly-Pro-Ser(tBu)- prepared in Reference Example 1 Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Lys(Boc)-Sieber amide resin (0.220meq / g, 46mg) was put into a reaction tube and swelled with DMF. After removing DMF by filtration, Fmoc-Aib-OH (32.5 mg), 0.5M Oxyma in DMF (200 μL) and diisopropylcarbodiimide (15.9 μL) were successively added to the resin, and the mixture was shaken for 2 hours. The reaction solution was filtered off, and then the resin was washed 6 times with DMF. After negative confirmation in the ninhydrin test, a 20% piperidine solution in DMF was added thereto, and the mixture was shaken for 1 minute. The solution was filtered off, then 20% piperidine in DMF was added thereto ...

Embodiment 2

[1279] Synthesis of H-Tyr-Aib-Glu-Gly-Thr-Val-Val-Ser-Leu-Tyr-Ser-Ile-Aib-Leu-Asp-Lys-Gln-Ala-Gln-Aib-Glu-Phe-Val-Lys -Trp-Leu-Leu-Lys-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-Lys-NH 2 (acetate ester of compound 6)

[1280] The powder (1084.2 mg) prepared in the same manner as in Example 1 was dissolved in a small amount of acetonitrile-water, an ion exchange resin (AG1 X8 resin (acetate form), 1.2 meq / mL, 2.1 mL) was added thereto, and then The resulting mixture was allowed to stand for 1 hour with occasional shaking. After removing the resin by filtration, the filtrate was freeze-dried to obtain 929.6 mg of a white powder.

[1281] Mass spectrometry result: (M+H) + 4231.3 (calculated value 4231.3)

[1282] HPLC elution time: 7.5 minutes

[1283] Elution conditions:

[1284] Column Chromolith Performance RP-18e (100x 4.6mm ID)

[1285] Eluent: Use solution A: 0.1% TFA-water, and solution B: acetonitrile with 0.1% TFA, A / B: 95 / 5 to 35 / 65. Linear concentration gradie...

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PUM

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Abstract

The present invention provides a novel peptide compound having an activating action on GIP receptors and use of the peptide compound as a medicament. Specifically, a peptide containing a sequence represented by the formula (I) or a salt thereof and a medicament comprising the same are provided. P1-Tyr-A2-Glu-Gly-Thr-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25-A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-A37-A38-A39-A40-P2 (I) wherein each symbol is as defined herein.

Description

technical field [0001] related application [0002] The present invention relates to novel peptide compounds having an activating effect on GIP receptors and the use of the peptide compounds as medicines. Background technique [0003] Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are both peptides called incretins. GLP-1 and GIP are secreted from L and K cells of the small intestine, respectively. [0004] GLP-1 acts via the GLP-1 receptor, and is known to have a glucose-dependent insulinotropic action and a feeding inhibitory action. On the other hand, GIP is known to have a glucose-dependent insulinotropic action via the GIP receptor, but the effect of GIP alone on food intake is unclear. [0005] Attempts have been made to find peptides and modified products thereof having GLP-1 receptor / GIP receptor co-agonist or glucagon receptor / GLP-1 receptor / GIP receptor triple receptor agonist activity, and these peptides Developed as an ...

Claims

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Application Information

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IPC IPC(8): C07K14/605A61K38/00
CPCA61K47/60A61P1/08C07K14/4705C07K14/605A61K38/00
Inventor 浅见泰司西泽直树新居田步兼松阳子安达万里竹河志郎浅川智子
Owner TAKEDA PHARMA CO LTD
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