JAK kinase inhibitor containing 4-aminopyrazole structure, preparation method and application thereof

A kind of aminopyrazole, alkyl technology, applied in the field of organic compound synthesis and medical application

Active Publication Date: 2016-03-23
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Despite the success of ruxolitinib and tofacitinib, both drugs have serious immune and blood-related side effects

Method used

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  • JAK kinase inhibitor containing 4-aminopyrazole structure, preparation method and application thereof
  • JAK kinase inhibitor containing 4-aminopyrazole structure, preparation method and application thereof
  • JAK kinase inhibitor containing 4-aminopyrazole structure, preparation method and application thereof

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Experimental program
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Embodiment Construction

[0094] The terms and definitions used in this document have the following meanings:

[0095] "Alkanes" refer to C1-C6 aliphatic chains, cyclopropane, cyclobutane, cyclopentane, cyclohexane, cycloheptane, etc.

[0096] "Aryl" refers to a group containing an aromatic carbocyclic ring and a substituted aryl group with substituents on the ring. The preferred aromatic ring contains 6-10 carbon atoms.

[0097] "Heteroaromatic ring" mainly includes pyrimidine ring, pyrrolopyrimidine ring, purine ring, pyrazolopyrimidine ring, furopyrimidine ring, thienopyrimidine ring, quinazoline and the like.

[0098] Hela cells, a type of cell used in biological and medical research, are derived from the cervical cancer cell line of an American woman, Henrietta Lacks. In the medical field, HeLa cells are widely used in tumor research, biological experiments or cell culture, and have become a very important tool in medical research.

[0099] 3. Application of JAK kinase inhibitors containing 4-am...

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Abstract

The invention relates to a JAK kinase inhibitor containing a 4-aminopyrazole structure, a preparation method and an application thereof. Compounds of the series have structures shown in a general formula (I) or a general formula (II). The invention also provides the preparation method of the kinase inhibitor, and the application of the kinase inhibitor in preparation of medicines for preventing or treating inflammation, tumor and blood-related diseases.

Description

technical field [0001] The invention relates to a JAK kinase inhibitor containing a 4-aminopyrazole structure and a preparation method and application thereof, belonging to the technical field of organic compound synthesis and medical application. Background technique [0002] JAK kinases are a group of intracellular non-receptor tyrosine kinases that play important physiological roles in the regulation of inflammation, hematopoiesis, and tumorigenesis. In the JAK-Stat signaling pathway, JAK kinase acts as an important medium to transmit the feedback biological information of upstream signaling factors such as interferon, cytokines, growth factors, G protein-coupled receptors, etc. to the downstream signaling pathway. thereby regulating gene expression. JAK kinases contain four subtypes, namely JAK1, JAK2, JAK3, and TYK2. Among them, JAK1 and JAK3 can regulate interleukin factors (ILs) related to immune function, and JAK2 can regulate various cells related to bone marrow ce...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04C07D403/12C07D473/34C07D495/04A61K31/519A61K31/517A61K31/52A61K31/506A61P35/00A61P29/00A61P7/00A61P19/02A61P19/08A61P31/18
CPCC07D403/12C07D473/34C07D487/04C07D495/04
Inventor 张颖杰徐文方梁学武
Owner SHANDONG UNIV
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