Application examples of 2,6-dimethoxy-3-nitropyridine_Industrial additives

Background and overview of application examples of 2,6-dimethoxy-3-nitropyridine

2,6-Dimethoxy-3-nitropyridine is a pharmaceutical intermediate. There are reports in the literature that it can be used to prepare MALT1 inhibitors with a thiazolobromophenylboronic acid pyridine structure.

Application examples of 2,6-dimethoxy-3-nitropyridine

2,6-Dimethoxy-3-nitropyridine can be used to prepare 1-(5-chloro-2,4-dimethoxyphenyl)-3-( having the following thiazolopyridine structure 7-(1-methoxyethyl)-2-methylthiazolo[5,4-b]pyridin-6-yl)urea is a MALT1 inhibitor.

MALT1 is a crucial immune regulatory protein. Studies in Bcl-10 and MALT1-deficient mice showed the importance of MALT1 for transducing antigen receptor signals to the transcription factor NF-κB (WO 2009/065897). Additionally, the identification of several chromosomal translocations leading to the generation of constitutively active MALT1 or the identification of the MALT1 fusion protein API-MALT1/IgH-MALT1 leading to NF-κB activation independent of upstream stimulation (as in the case of Malt-type lymphoma ) further emphasizes the importance of this protein in cancer.

Inhibitors of MALT1 proteolytic activity have been reported to have antiproliferative activity against ABC-type DLBCL lymphoma. In addition, MALT1 has been reported to be involved in the pathology of various diseases, such as different types of tumor diseases, such as lung adenocarcinoma, breast cancer, mantle cell lymphoma, marginal zone lymphoma, cutaneous T-cell lymphoma of Sézary syndrome, pancreatic cancer, certain types of chronic lymphocytic leukemia with CARD11 mutations, and certain subtypes of GCB-DLBCL lymphoma involving MALT1. Furthermore, targeting immunomodulatory proteins may have direct and indirect benefits in various inflammatory disorders in multiple organs, such as psoriasis, multiple sclerosis, rheumatoid arthritis, Sjögren’s syndrome, ulcerative colitis and in the treatment of different types of allergic disorders caused by chronic inflammation.

References

[1] [Invented in China] CN201780058978.5 Substituted di-tert-butyl thiodicarbonate azolopyridine compound as a MALT1 inhibitor