C-glucoside derivative

By developing C-glycoside derivatives as SGLT inhibitors, the problems of side effects and poor therapeutic effects of existing diabetes drugs have been solved, and effective hypoglycemic and weight management for various types of diabetes have been achieved, with safety and high productivity.

CN102875503AActive Publication Date: 2013-01-16JILIN HUISHENG BIOPHARMACEUTICAL CO LTD +1
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Patent Information

Application Number
CN201210212402.9
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2011-12-22
Filing Date
2012-06-25
Publication Date
2013-01-16
Estimated Expiration
2032-06-25

AI Technical Summary

Technical Problem

Existing diabetes drugs have potential side effects and are unsafe, especially for patients with type II diabetes, and there is a lack of effective oral treatment options that make it difficult to control blood sugar and promote weight loss at the same time.

Method used

A C-glycoside derivative was developed as a sodium-glucose cotransporter (SGLT) inhibitor to lower blood glucose by acting on SGLT2 and SGLT1, combined with its pharmaceutically acceptable salts, readily hydrolyzable esters or stereoisomers body to form pharmaceutical preparations to treat various diabetes-related diseases.

Benefits of technology

The compound significantly inhibits SGLT2, has good hypoglycemic effect and low toxicity, can be safely used to treat and prevent diabetes, has a simple preparation process, high product purity, and is suitable for large-scale production.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to C-glucoside derivative as shown in the general form (I), pharmaceutically acceptable salt, easily-hydrolyzed ester, stereoisomer and intermediate of the C-glucoside derivative, a method for preparing such compounds and intermediates, and medicinal preparation and medicine composition containing such compounds. The C-glucoside derivative provided by the invention can be served as the sodium-glucose cotransporter (SGLT) inhibitor to be applicable to insulin-dependent diabetes mellitus (I type diabetes mellitus) and non-insulin dependent diabetes mellitus (II type diabetes mellitus) and the like, and also can be used for treating insulin resistant disease and various relevant diseases of diabetes mellitus relevant to fat, and preventing there diseases, wherein R1, R2, R3, R4, R5a, R5b, R5c and X are shown as the definition in the specification.
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