Pyrrolopyrimidine compounds, their preparation method and use

A technology for pyrrolopyrimidine and compound, which is applied in the field of organic compound synthesis and medical application, can solve the problem of no pyrrole ring amino modification and the like, and achieves the effects of good solubility, high bioavailability and enhanced drug efficacy
CN106496233BActive Publication Date: 2018-05-15SOUTHEAST UNIV

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SOUTHEAST UNIV
Publication Date
2018-05-15

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Abstract

The invention discloses a pyrrolomiazine compound shown as the general formula I (please see the formula in the description) and pharmaceutically-acceptable salt or solvate of the pyrrolomiazine compound, and further discloses preparation methods and application of the pyrrolomiazine compound shown as the general formula I and the pharmaceutically-acceptable salt or solvate of the pyrrolomiazine compound. The prepared pyrrolomiazine compound can be quickly converted into a stock drug baricitinib in plasma and has the better solubility, the higher bioavailability and the enhanced drug efficacy compared with the stock drug.
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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 pyrrolopyrimidine compounds, a preparation method and uses thereof. Background technique

[0002] Prodrug refers to a class of compounds that are inactive or less active in vitro and undergo one or more steps of biotransformation of enzymes and chemical species in vivo to release active substances and produce pharmacological effects. Reversible drugs. It is usually formed by linking a biologically active drug molecule (original drug) with a non-toxic carrier (transient transport group). According to the chemical structure, prodrugs can be divided into four categories: carrier-linked prodrugs, biological prodrugs, macromolecular prodrugs and drug-antibody conjugates.

[0003] Prodrugs are a useful method for drug design and are widely used in the design of a variety of drug molecules. Many drugs are administered in the form...

Claims

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