PSD-95 inhibitor

A technology of -AA2 and -AA3 is applied in the direction of peptide-nucleic acid, medical preparations containing active ingredients, peptide/protein components, etc., which can solve the problems of lack of treatment methods and achieve stable properties and significant protective effects

Active Publication Date: 2020-06-16
CHENGDU AODA BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002]Acute ischemic stroke is one of the diseases with the highest mortality and disability

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-

[0033] Glu-Ser-Asp-Val-Lys(Pal-γGlu)-NH 2

[0034] 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:

[0035] 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.

[0036] In the above preparation method, the substitution value of the carrier resin is 0.2-1.0 m...

Embodiment 2

[0072] The preparation of embodiment 2 compound 2

[0073] Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Lys-Leu-Ser-Ser-Ile-

[0074] Glu-Ser-Asp-Val-Lys(2-cholesterol butyrate)-NH 2

[0075] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0076]

[0077]

[0078] 7.2 g of pure product was obtained, the purity was 95.8%, and the total yield was 23.2%. The molecular weight is 3100.8 (100% M+H).

Embodiment 3

[0079] The preparation of embodiment 3 compound 3

[0080] Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Lys-Leu-Ser-Ser-Ile-

[0081] Glu-Ser-Asp-Val-Cys(cholesteryl acetate)-NH 2

[0082] 1. Preparation of peptide resin

[0083] Method is the same as embodiment 1, and the protected amino acid that uses is as following table:

[0084]

[0085]

[0086] 2. Preparation of crude product

[0087] Take the above peptide resin, add a cleavage reagent with a volume ratio of TFA: water: EDT = 95: 5: 5 (cleavage reagent 10mL / g resin), stir well, stir and react at room temperature for 3 hours, use a sand core funnel to filter the reaction mixture, collect The filtrate and the resin were washed 3 times with a small amount of TFA, the combined filtrates were concentrated under reduced pressure, anhydrous ether was added to precipitate, and then the precipitate was washed with anhydrous ether 3 times, dried to obtain off-white powder, dissolved in pure DMSO, added Equal molar tri...

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Abstract

The invention relates to the field of medicine synthesis, and discloses a PSD-95 inhibitor. The PSD-95 inhibitor disclosed by the invention is used for preparing a pharmaceutical composition for treating diseases and an application of the pharmaceutical composition in preparing a neuroprotective drug after ischemic brain injury.

Description

technical field [0001] The present invention relates to a 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. After cerebral ischemia, excitatory glutamate is excessively released and continues to act on N-methyl-D-aspartate (NMDA) receptors, thereby initiating a series of downstream harmful signali...

Claims

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Application Information

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IPC IPC(8): C07K14/00A61K38/16A61P9/10A61P25/00
CPCC07K14/001A61P9/10A61P25/00A61K38/00
Inventor 周述靓王鹏邓岚
Owner CHENGDU AODA BIOTECHNOLOGY CO LTD
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