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Peptide compounds

A sequence and amino acid technology, applied in the field of peptide compounds, can solve the problem that the influence of food intake is not very clear

Active Publication Date: 2019-12-10
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, GIP is known to have a glucose-dependent insulinotropic effect via the GIP receptor, however, its effect on food intake is not well understood

Method used

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  • Peptide compounds
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0459] synthesis

[0460] H-Tyr-Aib-Glu-Gly-Thr-αMePhe-Thr-Ser-Asp-Tyr-Ala-Ile-Aib-Leu-Asp-Lys-Gln-Ala-Gln-Ala-Glu-Phe-Val-Lys- Trp-Leu-Leu-Lys-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-Lys-NH 2 (SEQ ID NO: 13)

[0461] Prepared with reference to Example 1

[0462] H-Glu(OtBu)-Phe-Val-Lys(Boc)-Trp(Boc)-Leu-Leu-Lys(Boc)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala- Pro-Pro-Pro-Ser(tBu)-Lys(Boc)-Sieber amide resin (0.244 meq / g, 41.0 mg) was weighed into a reaction tube and swelled with DMF. After removing DMF by filtration, Fmoc-Ala-OH (31.1 mg), 0.5M OxymaPure / DMF (200 μL) and diisopropylcarbodiimide (15.9 μL) were sequentially added to the resin, and the mixture was shaken for 1.5 hours . The reaction solution was filtered, and then the resin was washed 6 times with DMF. After being negative in the Kaiser test, 20% piperidine in DMF was added thereto, and the mixture was shaken for 1 minute. The solution was filtered, then 20% piperidine in DMF was added again, and the mixtu...

Embodiment 2

[0472] synthesis

[0473] H-Tyr-Aib-Glu-Gly-Thr-αMePhe-Thr-Ser-Asp-Tyr-Aib-Ile-Aib-Leu-Asp-Lys-Gln-Ala-Gln-Ala-Glu-Phe-Val-Lys- Trp-Leu-Leu-Lys-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-Lys-NH 2 (SEQ ID NO: 14)

[0474] Prepared with reference to Example 1

[0475] H-Glu(OtBu)-Phe-Val-Lys(Boc)-Trp(Boc)-Leu-Leu-Lys(Boc)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala- Pro-Pro-Pro-Ser(tBu)-Lys(Boc)-Sieber amide resin (0.244 meq / g, 41.0 mg) was weighed into a reaction tube and swelled with DMF. After removing DMF by filtration, Fmoc-Ala-OH (31.1 mg), 0.5M OxymaPure / DMF (200 μL) and diisopropylcarbodiimide (15.9 μL) were sequentially added to the resin, and the mixture was shaken for 1.5 hours . The reaction solution was filtered, and then the resin was washed 6 times with DMF. After being negative in the Kaiser test, 20% piperidine in DMF was added thereto, and the mixture was shaken for 1 minute. The solution was filtered, then 20% piperidine in DMF was added again, and the mixtu...

Embodiment 3

[0485] synthesis

[0486] H-Tyr-Aib-Glu-Gly-Thr-αMePhe-Thr-Ser-Asp-Tyr-Ala-Ile-Aib-Leu-Asp-Lys-Gln-Ala-Gln-Ser-Glu-Phe-Val-Lys- Trp-Leu-Leu-Lys-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-Lys-NH 2 (SEQ ID NO: 15)

[0487] Prepared with reference to Example 1

[0488] H-Glu(OtBu)-Phe-Val-Lys(Boc)-Trp(Boc)-Leu-Leu-Lys(Boc)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala- Pro-Pro-Pro-Ser(tBu)-Lys(Boc)-Sieber amide resin (0.244 meq / g, 41.0 mg) was weighed into a reaction tube and swelled with DMF. After removing DMF by filtration, Fmoc-Ser(tBu)-OH (38.3 mg), 0.5M OxymaPure / DMF (200 μL) and diisopropylcarbodiimide (15.9 μL) were sequentially added to the resin, and the mixture Shake for 1.5 hours. The reaction solution was filtered, and then the resin was washed 6 times with DMF. After being negative in the Kaiser test, 20% piperidine in DMF was added thereto, and the mixture was shaken for 1 minute. The solution was filtered, then 20% piperidine in DMF was added again, and the mixtur...

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Abstract

The present invention provides a novel peptide compound having an activating effect on GLP-1 receptor and GIP receptor, and the use of the peptide compound as a medicine. Specifically, a peptide containing a partial sequence represented by formula (I) or a salt thereof, and a medicament containing the peptide or a salt thereof are provided. P 1 ‑Tyr‑Aib‑Glu‑Gly‑Thr‑αMePhe‑Thr‑Ser‑Asp‑Tyr‑A11‑A12‑A13‑Leu‑Asp‑A16‑A17‑Ala‑Gln‑A20‑Glu‑Phe‑Val‑Lys‑Trp ‑Leu‑Leu‑Lys‑A29(I). wherein, each symbol is as defined herein.

Description

[technical field] [0001] The present invention relates to novel peptide compounds having an activating effect on GLP-1 receptor and GIP receptor, and the use of said peptide compound as a medicine. [0002] [Background of the invention] [0003] Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are both peptides known as incretins. GLP-1 and GIP are secreted from intestinal L cells and K cells, respectively. [0004] GLP-1 acts through the GLP-1 receptor, and it is known that it has a glucose-dependent insulinotropic action and a feeding-inhibiting action. On the other hand, GIP is known to have a glucose-dependent insulinotropic action via the GIP receptor, but its influence on food intake is not well understood. [0005] Coadministration of the GLP-1 receptor agonist liraglutide and the GIP receptor agonist N-Ac-GIP has been reported to improve glucose tolerance more than liraglutide alone Improvement effect and body weight reduction ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/605
CPCC07K14/605A61K38/00A61P3/04A61P3/10A61P43/00
Inventor 浅见泰司新居田步
Owner TAKEDA PHARMA CO LTD