Isoxazole derivatives as mutant isocitrate dehydrogenase 1 inhibitors

A compound and hydrogen atom technology, applied in the field of isoxazole derivatives as mutant isocitrate dehydrogenase 1 inhibitors, can solve problems such as the influence of tumor properties
CN106795146BActive Publication Date: 2020-06-26DAIICHI SANKYO CO LTD +1
5 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
DAIICHI SANKYO CO LTD
Publication Date
2020-06-26

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The present invention finds that the compound of general formula (I) with an isoxazole skeleton has excellent inhibitory activity on mutant IDH1 protein, can inhibit the production of 2-HG through the protein, and can effectively inhibit various tumors expressing the protein proliferation.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The present invention relates to a compound having excellent inhibitory activity against mutant isocitrate dehydrogenase 1 (hereinafter also referred to as "IDH1") and a pharmaceutically acceptable salt thereof. Background technique

[0002] Isocitrate dehydrogenases (IDHs: isocitrate dehydrogenases) are a group of enzymes that convert isocitrate into 2-oxoglutarate (α-ketoglutarate). This group of enzymes can be further subdivided into NAD+-dependent isocitrate dehydrogenases (EC 1.1.1.41) and NADP+-dependent isocitrate dehydrogenases (EC 1.1.1.42).

[0003] IDH1 (isocitrate dehydrogenase 1 (NADP+), soluble) protein and IDH2 (isocitrate dehydrogenase 2 (NADP+), mitochondrial) protein are classified as NADP+-dependent isocitrate dehydrogenase (EC 1.1.1.42) enzymes. Mutations in the IDH1 gene or IDH2 gene are found in various cancers. Specific examples include glioma and glioblastoma, acute myeloid leukemia, myelodysplastic syndrome, myeloproliferati...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More