180080-56-2Relevant articles and documents
NEW SUBSTITUTED AZAINDOLINE DERIVATIVES AS NIK INHIBITORS
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Page/Page column 155, (2019/01/21)
The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK - also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
Acetic acid as a catalyst for the N-acylation of amines using esters as the acyl source
Sanz Sharley, Daniel D.,Williams, Jonathan M. J.
supporting information, p. 2020 - 2023 (2017/02/15)
We report a cheap and simple method for the acetylation of a variety of amines using catalytic acetic acid and either ethyl acetate or butyl acetate as the acyl source. Catalyst loadings as low as 10 mol% afforded acetamide products in excellent yields at temperatures ranging from 80-120 °C. The methodology can also be successfully applied for the synthesis of a broad range of other amides, including the formation of formamides at 20 °C.
1H-Pyrazole-1-carboxamidines: New inhibitors of nitric oxide synthase
Lee, Younghee,Martasek, Pavel,Roman, Linda J,Silverman, Richard B
, p. 2771 - 2774 (2007/10/03)
1H-Pyrazole-1-carboxamidines were prepared as potential inhibitors of the three isozymes of nitric oxide synthase. All of the compounds were found to be competitive inhibitors of all three isoforms. The most selective compound prepared was 1H-pyrazole-N-(3-aminomethylanilino)-1-carboxamidine (14), which is 100-fold selective for nNOS over eNOS with a K(i) value of 2μM. (C) 2000 Elsevier Science Ltd.
