A crocetin derivative gx-ring, its preparation method, and its application in preventing or treating cardiovascular and cerebrovascular diseases

A technology of crocus acid and crocus, applied in the field of new crocus acid derivatives, can solve the problems of poor fat solubility and water solubility of crocus acid, limited clinical application, low bioavailability, etc. Or treat cardiovascular and cerebrovascular diseases, improve bioavailability, and overcome the effects of extremely low fat solubility
CN106431950BActive Publication Date: 2018-06-29LIVZON PHARM GRP INC
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
LIVZON PHARM GRP INC
Publication Date
2018-06-29

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Abstract

The present invention relates to a crocetin derivative GX-Ring and a preparation method thereof. The preparation method comprises the following steps of A, adding crocetin and CH2Cl2 in a reaction bottle, adding oxalyl chloride and DMF under the condition of an ice bath, stirring at the room temperature, subjecting an obtained mixture to reaction for 4 to 6 hours, continuously adding amide for further reaction, placing an obtained product overnight at the room temperature, adding H2O and stirring for reaction; B, filtering an obtained reaction liquid to remove a solvent, adding EA to dissolve a solute, washing and removing the solvent to obtain a crude product; C, separating the crude product through a silicagel column, and eluting to obtain a product. The above crocetin derivative GX-Ring can be prepared into tablets, sustained release tablets, granules, suspensions and other oral preparations for preventing or treating cardiovascular and cerebrovascular diseases. The clinical application of the crocetin derivative GX-Ring is wider in range.
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Description

technical field

[0001] The invention relates to a new crocetin derivative, in particular to a pharmaceutically acceptable amide of crocetin, a preparation method thereof, and an application of the derivative in preventing and treating cardiovascular and cerebrovascular diseases. Background technique

[0002] Saffron (Crocus sativus L.), also known as saffron, is the dry stigma of Crocus sativus L., a plant of the Iridaceae genus Crocus. Saffron is a kind of precious Chinese herbal medicine. It is widely used clinically in the treatment or prevention of cardiovascular and cerebrovascular diseases, as well as tumor, inflammation, pain suppression and protection of liver, kidney and nervous system, and has significant curative effect.

[0003] The main medicinal substances of saffron include crocetin, crocin, dimethyl crocetin, crocin, etc., and also contain eucalyptol, pinene, and multivitamins. Modern studies at home and abroad have shown that crocetin is the main active com...

Claims

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