As tyrosine kinase inhibitors containing nitrogen and ring compound
The invention belongs to the technical field of medicine, particularly relates to a heterocyclic nitrogen compound which acts as a tyrosine kinase inhibitor and is represented by a general formula (I) as well as a deuterated material, pharmaceutically acc
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Paragraph 0272; 0276; 0277; 0278
(2017/04/26)
Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis
By applying conformational restrictions, we were able to discover highly potent 1,3-diaminopyrimidine based covalent inhibitors of BTK, such as 8a (IC50 = 3.76 nM), and providing useful information of its active conformation. We are developing these novel small molecule covalent inhibitors of BTK toward oral agents for Rheumatoid arthritis.