JAK kinase inhibitor with 4-amino-(1H)-pyrazole structure and preparation method and application thereof

A kinase inhibitor, pyrazole technology, applied in the field of organic compound synthesis and pharmaceutical applications, can solve the problem of undisclosed powerful inhibitors

Inactive Publication Date: 2017-01-25
SHANDONG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Previously, we synthesized a potent JAK kinase inhibitor, and the prior art of this potent inhibitor was not published

Method used

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  • JAK kinase inhibitor with 4-amino-(1H)-pyrazole structure and preparation method and application thereof
  • JAK kinase inhibitor with 4-amino-(1H)-pyrazole structure and preparation method and application thereof
  • JAK kinase inhibitor with 4-amino-(1H)-pyrazole structure and preparation method and application thereof

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Embodiment Construction

[0087] The terms and definitions used in this document have the following meanings:

[0088] "Alkanes" refer to C1-C6 aliphatic chains, such as cyclopropane, cyclobutane, cyclopentane, cyclohexane, cycloheptane and the like.

[0089] "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.

[0090] HEL cells are human leukemia cells, MCF-7 cells are human breast cancer cells, PC-3 cells are prostate cancer cells, K562 are human myeloid leukemia cells, and MOLT4 cells are human lymphoma leukemia cells. These cells are widely used in tumors Research, biological experiments or cell culture, has become a very important tool in medical research.

[0091] 3. Application of JAK kinase inhibitors containing 4-amino-(1H)-pyrazole ring structure

[0092]Activity screening experiments show that the compound of the present invention has good inhibitory activity of ...

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Abstract

The invention discloses a JAK kinase inhibitor with 4-amino-(1H)-pyrazole structure and a preparation method and application thereof. The compound has a structure shown in general formula (I) or (II), and the invention provides a specific preparation method of the compound and application of the compound in preventing or treating inflammation, tumor and blood related diseases; the inflammation, tumor and blood related diseases include psoriasis, rheumatic arthritis, polycythemia vera, cicatricial alopecia, primary thrombocythemia, ulcerative colitis, myelofibrosis with myeloid metaplasia, severe combined immune deficiency, various leukemia, various solid tumors and the like.

Description

technical field [0001] The invention relates to a JAK kinase inhibitor containing a 4-amino-(1H)-pyrazole structure, a preparation method and application thereof, and belongs to the technical field of organic compound synthesis and medical application. Background technique [0002] The JAK / STAT signaling pathway plays an important physiological role in autoimmunity, hematopoiesis, and tumorigenesis. The abnormality of JAK / STAT signaling pathway will induce diseases such as immunodeficiency, inflammation and tumor. Some tumors are accompanied by the continuous activation of JAKs kinases. Dysregulation of JAK2 isoforms is frequently found in patients with osteoproliferative neoplasms and childhood T-cell acute lymphoblastic leukemia. Hematologic malignancies such as malignant lymphoma and myeloproliferative disorders are associated with mutations in JAK2 subtypes. Binding of certain growth factors and cytokines to their receptors can stimulate JAKs to phosphorylate STAT3. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12C07D487/04A61P35/00A61P35/02
CPCC07D403/12C07D487/04
Inventor 张颖杰徐文方梁学武
Owner SHANDONG UNIV
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