1020174-04-2Relevant articles and documents
TYK-2 INHIBITOR
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Paragraph 0635-0637, (2022/01/05)
Disclosed herein is a compound of Formula (I) for inhibiting TYK2 and treating a disease associated with the undesirable tyk-2 activity (tyk-2 related diseases), a method of using the compounds disclosed herein for treating inflammatory or autoimmune disease, and a pharmaceutical composition comprising the same.
Synthetic method of 1-methyl-1H-pyrazole-3-boronic acid pinacol ester
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Paragraph 0037; 0038; 0039; 0040, (2016/10/27)
The invention discloses a synthetic method of 1-methyl-1H-pyrazole-3-boronic acid pinacol ester. The method comprises the following steps: step 1, 3-iodine-1-methyl-1H-pyrazole is synthesized from N-methyl-3-aminopyrazole through a diazotization reaction; step 2, 3-iodine-1-methyl-1H-pyrazole prepared in the step 1 is taken as a raw material of reaction, n-butyllithium is taken as a base, isopropoxyboronic acid pinacol ester is taken as a boronizing reagent, and 1-methyl-1H-pyrazole-3-boronic acid pinacol ester is obtained through synthesis. 1-methyl-1H-pyrazole-3-boronic acid pinacol ester with high purity is prepared with a simpler process, lower cost and higher yield. After deep analysis of a target product, N-methyl-3-aminopyrazole is taken as the raw material, iodine with higher activity is prepared through direct diazotization, and production of isomers during methyl introduction in the prior art is avoided, so that the yield is increased greatly and the purification difficulty is reduced greatly.
HETEROCYCLIC COMPOUND
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Paragraph 0578, (2015/01/18)
The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.