Crisaborole prodrug and its preparation method and use

A pharmacy and CH2 technology, applied in chemical instruments and methods, antipyretics, drug combinations, etc., can solve problems such as side effects and depression, and achieve the effects of enhancing drug efficacy, good solubility, and high bioavailability
CN112824418BActive Publication Date: 2022-04-19苏州东南药业股份有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
苏州东南药业股份有限公司
Publication Date
2022-04-19

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Abstract

The present invention obtains a series of Crisaborole prodrugs represented by the general formula I by modifying the active site of Crisaborole: the compound designed by the present invention can be rapidly converted into the original drug Crisaborole in plasma, and compared with the original drug, it has better It has better solubility, higher bioavailability, enhanced efficacy, and is a new type of compound with PDE‑4 inhibitory activity.
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Description

technical field

[0001] The invention belongs to the technical field of organic compound synthesis and medical application, and in particular relates to a prodrug of Crisaborole and its preparation method and application. Background technique

[0002] Prodrugs, also known as prodrugs, drug precursors, prodrugs, etc., are mainly aimed at improving the bioavailability of drugs, increasing drug stability, reducing toxic and side effects, and promoting long-acting drugs. Prodrug is a very useful drug design method. After chemical structure modification, it is inactive or less active in vitro, and the active drug is released through enzymatic or non-enzymatic conversion in vivo to exert its medicinal effect. At present, clinical prodrugs have been widely used in the treatment of various diseases, and there is still a lot of room for development. In conclusion, prodrug strategies have become an integral part of drug design and delivery methods.

[0003] Phosphodiesterases (PDEs) ...

Claims

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