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Process for the synthesis of (aib8,35)hglp-1(7-36)-nh2

One-NH2, hglp-1 technology, applied in the direction of peptide preparation methods, chemical instruments and methods, pharmaceutical formulations, etc., can solve problems such as large investment

Active Publication Date: 2011-10-19
IPSEN MFG IRELAND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Generally, schemes based on hydrofluoric acid cracking require substantial investment to ensure that they are safe and scalable for industrial scale.

Method used

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  • Process for the synthesis of (aib8,35)hglp-1(7-36)-nh2
  • Process for the synthesis of (aib8,35)hglp-1(7-36)-nh2
  • Process for the synthesis of (aib8,35)hglp-1(7-36)-nh2

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Embodiment approach

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Abstract

The present invention relates to a process for the large-scale synthesis of (Aib8,35)hGLP-l(7-36)-NH2 (SEQ ED NO:2), i.e., His-Aib-Glu-Gly-Thr-Phe-Thr-Ser- Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gb-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val- Lys-Aib-Arg-NH2 (SEQ ID NO:2), which comprises solid-phase Fmoc-chemistry.

Description

field of invention [0001] The present invention relates to large-scale synthesis (Aib 8，35 )hGLP-1(7-36)-NH 2 (SEQ ID NO: 2) (i.e. His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu -Phe-Ile-Ala-Trp-Leu-Val-Lys-Aib-Arg-NH 2 (SEQ ID NO: 2)) comprising solid-phase Fmoc-chemical synthesis (Fmoc-chemistry). technical background [0002] Glucagon-like peptide 1 (7-36) amide (GLP-1) (SEQ ID NO: 1) through tissue-specific posttranslational processing of the glucagon precursor, preproglucagon, in small intestinal L cells synthesized and released into the circulation in response to a meal. The therapeutic potential of GLP-1 has been observed that a single subcutaneous dose of GLP-1 can completely normalize postprandial glucose levels in patients with non-insulin-dependent diabetes mellitus (NIDDM) (Gutniak, M.K. et al., 1994, Diabetes Care, 14 : 1039-44). This effect is thought to be mediated by increased insulin release and decreased glucagon s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/00
CPCC07K14/605C07K1/04C07K1/107A61K38/26
Inventor 董正欣T·C·拉夫曼F·赫利S·R·约翰逊
Owner IPSEN MFG IRELAND