Long-acting PSD-95 inhibitor

A-AA2, lys-leu-ser-ser-ile-glu-ser-asp-val-aa1 technology, applied in the field of long-acting PSD-95 inhibitors, can solve the problem of short half-life of Nerinetide, poor patient compliance, clinical The problem of high cost, to achieve a significant protective effect, the effect of stable nature

Active Publication Date: 2020-10-16
CHENGDU AODA BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Due to the short half-life of Nerinetide in the body, patients need a large dose of medication every day, which leads to poor patient compliance and high clinical costs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The preparation of embodiment 1 compound 1

[0032] Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Lys-Leu-Ser-Ser-Ile-Glu-Ser-Asp-Val-Lys (AEEA-AEEA-γGlu-18 alkane Diacid)-NH 2

[0033] The preparation method includes: preparing the peptide resin by solid-phase polypeptide synthesis method, acid hydrolyzing the peptide resin to obtain a crude product, and finally purifying the crude product to obtain a pure product; wherein the step of preparing the peptide resin by the solid-phase polypeptide synthesis method is to pass solid-phase The phase-coupled synthesis method sequentially inserts the corresponding protected amino acids or fragments in the following sequences to prepare peptide resins:

[0034] In the above preparation method, the amount of the Fmoc-protected amino acid or protected amino acid fragment is 1.2-6 times of the total moles of the resin fed; preferably 2.5-3.5 times.

[0035] In the above preparation method, the substitution value of the carrier resi...

Embodiment 2

[0070] The preparation of embodiment 2 compound 2

[0071] Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Lys-Leu-Ser-Ser-Ile-Glu-Ser-Asp-Val-Lys (cholesteryl succinate)- NH 2

[0072] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0073]

[0074]

[0075] 7.7 g of pure product was obtained, the purity was 97.1%, and the total yield was 24.7%. The molecular weight is 3114.6 (100% M+H).

Embodiment 3

[0076] The preparation of embodiment 3 compound 3

[0077] Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Lys-Leu-Ser-Ser-Ile-Glu-Ser-Asp-Val-Lys(PEG 5 CH 2 CO-γGlu-18 alkanedioic acid)-NH 2

[0078] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0079]

[0080]

[0081] 9.3 g of pure product was obtained, the purity was 98.7%, and the total yield was 27.8%. Molecular weight 3349.2 (100% M+H).

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PUM

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Abstract

The invention relates to the field of medicine synthesis, and discloses a long-acting PSD-95 inhibitor. The long-acting PSD-95 inhibitor is used to prepare a pharmaceutical composition for treating diseases, and the pharmaceutical composition is used in the preparation of neuroprotective drugs after ischemic brain injury.

Description

technical field [0001] The invention relates to a long-acting PSD-95 inhibitor and its use. Background technique [0002] Acute ischemic stroke is one of the diseases with the highest mortality rate and disability rate in the world, and there is currently no effective treatment in clinical practice. Cerebral ischemia can cause a cascade reaction from energy deprivation to cell death. Early events mainly include excitotoxicity and oxidative stress, while late events mainly include inflammation and apoptosis. At present, a large number of basic and clinical researches are devoted to the intervention of signaling molecules related to stroke pathology to develop effective neuroprotective therapy. As the initial link of stroke pathology, excitotoxicity is the primary target of stroke treatment. [0003] After cerebral ischemia, excitatory glutamate is excessively released and continues to act on N-methyl-D-aspartate receptors, thereby initiating a series of downstream harmful s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/00A61K38/16A61P9/10
CPCC07K14/001A61P9/10A61K38/00
Inventor 黄晓兵周述靓代景莹
Owner CHENGDU AODA BIOTECHNOLOGY CO LTD
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