Preparation and purification method and application of a kind of peptidomimetic compound

A compound and peptide technology, applied in the field of medicine, can solve problems such as inconvenient clinical administration of injections, joint swelling, anaphylactic shock, etc.

A compound and peptide technology, applied in the field of medicine, can solve problems such as inconvenient clinical administration of injections, joint swelling, anaphylactic shock, etc.

CN108610394BActive Publication Date: 2021-08-31SHENZHEN WINKEY MEDICAL RES DEV
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  • Preparation and purification method and application of a kind of peptidomimetic compound
  • Preparation and purification method and application of a kind of peptidomimetic compound
  • Preparation and purification method and application of a kind of peptidomimetic compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Anti-platelet peptidomimetic compound Scutellarin-HomoArg-Gly-Asp-Trp-NH 2 Synthesis

[0034] 1.1 Preparation of Fmoc-Linker-Amide Resin

[0035] Weigh 50 g (60 mmol) of Amide Resin resin into a 2L solid-phase synthesis reaction column. Wash the resin once with 400ml DMF, swell the resin with 500ml DCM for 20min, and remove the solvent. 400ml DMF washed the resin 3 times.

[0036] Weigh 80.9g (150mmol) of Fmoc-linker and 24.3g (180mmol) of HOBt into a dry 500ml wide-mouth Erlenmeyer flask. Add about 150ml of DMF solvent to dissolve and place in ice-water bath to cool for 2min, add DIC 30ml (195mmol) to activate for 3min, avoid water vapor. The activated amino acid was added to the swollen resin to react for 2 hours, and the reaction solution was sucked away. Wash the resin 3 times with 400ml DMF, 2min each time.

[0037] Join Ac 2 O 28ml (300mmol), DIPEA 10.7ml (60mmol), DMF 400ml mixed solution sealed for 3h, the resin was washed four times with DMF 50...

Embodiment 2

[0070] Example 2 Anti-platelet peptidomimetic compound Scutellarin-HomoArg-Gly-Asp-NH 2 Synthesis

[0071] 2.1 Preparation of Fmoc-Linker-Amide Resin

[0072] Weigh 50 g (60 mmol) of Amide Resin resin into a 2L solid-phase synthesis reaction column. Wash the resin once with 400ml DMF, swell the resin with 500ml DCM for 20min, and remove the solvent. The resin was washed three times with 400ml DMF.

[0073] Weigh 80.9g (150mmol) of Fmoc-linker and 24.3g (180mmol) of HOBt into a dry 500ml wide-mouth Erlenmeyer flask. Add about 150ml of DMF solvent to dissolve and place it in an ice-water bath to cool for 2 minutes, add 30ml of DIC (195mmol) to activate for 3 minutes, and avoid water vapor. The activated amino acid was added to the swollen resin to react for 2 hours, and the reaction solution was sucked away. Wash the resin 3 times with 400ml DMF, 2min each time.

[0074] Join Ac 2 O 28ml (300mmol), DIPEA 10.7ml (60mmol), DMF 400ml mixed solution sealed for 3h, the resin w...

Embodiment 3

[0102] Example 3 Anti-platelet peptidomimetic compound Scutellarin-HomoArg-Gly-Asp-Trp-Pro-NH 2 Synthesis

[0103] 3.1 Preparation of Fmoc-Linker-Amide Resin

[0104] Weigh 50 g (60 mmol) of Amide Resin resin into a 2L solid-phase synthesis reaction column. Wash the resin once with 400ml DMF, swell the resin with 500ml DCM for 20min, and remove the solvent. The resin was washed three times with 400ml DMF.

[0105] Weigh 80.9g (150mmol) of Fmoc-linker and 24.3g (180mmol) of HOBt into a dry 500ml wide-mouth Erlenmeyer flask. Add about 150ml of DMF solvent to dissolve and place it in an ice-water bath to cool for 2 minutes, add 30ml of DIC (195mmol) to activate for 3 minutes, and avoid water vapor. The activated amino acid was added to the swollen resin to react for 2 hours, and the reaction solution was sucked away. Wash the resin 3 times with 400ml DMF, 2min each time.

[0106] Join Ac 2 O 28ml (300mmol), DIPEA 10.7ml (60mmol), DMF 400ml mixed solution sealed for 3h, the...

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Abstract

The invention discloses a class of anti-platelet aggregation peptidomimetic drugs and a preparation method and application thereof. This compound is a platelet GPIIb / IIIa receptor antagonist. It uses scutellarin, an active substance of traditional Chinese medicine, to modify the RGD peptide structure of GPⅡb / Ⅲa receptors, which can not only improve the GPⅡb / Ⅲa receptors of RGD peptides Specificity, but also improve the solubility of scutellarin. The compound has the pharmacological effect of anti-platelet aggregation, and can be used clinically to prevent myocardial oxygen supply artery occlusion, heart attack, unstable angina, no Q wave myocardial infarction, sudden death caused by coronary intervention, or can be used for acute coronary Syndrome patients.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a peptidomimetic compound for anti-platelet aggregation, including its synthesis technology and screening method. The compound can be clinically used to prevent myocardial oxygen supply arterial occlusion, heart attack, unstable angina pectoris, non-Q wave myocardial infarction, sudden death caused by coronary intervention, or can be used for patients with acute coronary syndrome. Background technique [0002] Thrombotic disease is a common cardiovascular and cerebrovascular disease. It is a variety of diseases caused by the stenosis and occlusion of the blood vessel cavity caused by thrombus, which causes ischemia and infarction of major organs and causes dysfunction. It often manifests as myocardial infarction, ischemia, etc. Cerebral infarction and venous thromboembolism can affect various organs and systems of the body, and its morbidity, disability and mortality are high. [0003] In ...

Claims

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Application Information

Patent Timeline
31 Aug 2021
Publication
CN108610394B
IPC
C07K5/09; C07K5/11; C07K7/06; C07K1/04; A61K38/06; A61K38/07; A61K38/08; A61P7/02; A61P9/00
CPC
A61K38/00; A61P7/02; A61P9/00; C07K5/0817; C07K5/1019; C07K7/06
Inventors
丁文锋