10491-77-7Relevant academic research and scientific papers
HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY
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Paragraph 0905; 0906, (2015/11/16)
Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I foranddiagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
11B-HSD1 inhibitors for the treatment of diabetes
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Page/Page column 11, (2008/06/13)
Compounds of the formula (I): as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
On the Chichibabin Amination of Pyrimidine and N-Alkylpyrimidinium Salts Using Liquid Ammonia/Potassium Permanganate
Buurman, Dick J.,Plas, Henk C. van der
, p. 1377 - 1380 (2007/10/02)
Treatment of the 2-R-pyrimidines (1, R = methyl, ethyl, i-propyl and t-butyl) with potassium amide/liquid ammonia/potassium permanganate leads to amination at C-4(6).The yields of the 4(6)-amino compounds 3 increase in the order 2-methyl (10percent), 2-ethyl (30percent), 2-i-propyl (45percent) and 2-t-butyl (60percent).Treatment of the 2-R-N-methylpyrimidinium salts (4, R = hydrogen, methyl) with liquid ammonia/potassium permanganate leads to a regiospecific imination at C-6, the corresponding 2-R-1,6-dihydro-6-imino-1-methylpyrimidines 6 being obtained in 80-85percent yield.It is proved by 15N-labelling that no ring opening is involved in these imination reactions.Treatment of the imino compounds with base leads to the corresponding 2-R-6-methylaminopyrimidines 8, involving, as proved by 15N-labelling, an ANRORC-mechanism. 2-t-Butyl-1-ethylpyrimidinium tetrafluoroborate (9b) when treated with liquid ammonia/potassium permanganate undergoes N-deethylation, 2-t-butylpyrimidine being exclusively formed.
