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Long-acting adrenomedullin derivatives

A technology of adrenomedullin and compounds, which is applied in the field of long-acting adrenomedullin derivatives, can solve problems such as short half-life, and achieve the effect of pharmacological inhibition and long-term sustained action of adverse side effects

Active Publication Date: 2022-04-26
UNIVERSITY OF MIYAZAKI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Peptides are generally known to have a short half-life in vivo due to metabolic reactions in the body (e.g. blood)

Method used

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  • Long-acting adrenomedullin derivatives
  • Long-acting adrenomedullin derivatives
  • Long-acting adrenomedullin derivatives

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Embodiment

[0380] The present invention will be described in more detail below using examples. However, the technical scope of the present invention is not limited to these examples.

[0381]

[0382] [Experiment I-1: Synthesis of full-length adrenomedullin derivatives]

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Abstract

The present invention provides a novel adrenomedullin derivative with long-lasting action, which can maintain the pharmacological effect of adrenomedullin and substantially suppress adverse side effects. As an exemplary embodiment, the present invention relates to a compound represented by formula (I) or a salt thereof, or a hydrate thereof: A-CH 2 -B(I). In formula (I), A is a modification group containing more than one polyethylene glycol group, and B is a peptide part derived from adrenomedullin or its modification having adrenomedullin activity, wherein the peptide part B Linkage to the remainder is through the covalent bonding of the nitrogen atom of its N-terminal alpha amino group to the carbon atom of the methylene group.

Description

technical field [0001] The present invention relates to a long-acting adrenomedullin derivative. Background technique [0002] Adrenomedullin (hereinafter also referred to as "AM") is a biologically active peptide isolated and identified from pheochromocytoma tissue in 1993 (Non-Patent Document 1). At the beginning of discovery, it has been confirmed that AM can exert a strong antihypertensive effect of dilating blood vessels. For example, Patent Document 1 describes a peptide comprising a human AM amino acid sequence that has a hypotensive effect. [0003] Subsequent studies have shown that AM can exert various pharmacological effects such as cardiovascular protection, anti-inflammation, angiogenesis, and tissue repair promotion. In addition, in order to apply the pharmacological action of AM to the treatment of diseases, studies on the administration of AM to patients with various diseases have been conducted. Among them, AM is expected to be useful as a therapeutic dru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K19/00A61K38/00A61P29/00A61P9/00C07K14/46C12N15/09C12P21/02
CPCC07K14/575A61K47/60A61P29/00A61P37/00A61P9/00A61P9/08A61P9/12A61K38/00C07K14/46C07K19/00C12N15/09C12P21/02A61K38/22
Inventor 北村和雄山崎基生
Owner UNIVERSITY OF MIYAZAKI
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