384337-90-0Relevant articles and documents
EFFICIENT METHOD FOR THE PREPARATION OF TOFACITINIB CITRATE
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Paragraph 0096-0097, (2016/10/31)
Disclosed is a novel process for the synthesis of tofacitinib citrate on an industrial scale with high yields and purity starting with cis-(1-benzyl-4-methyl-piperidin-3-yl)methylamine bis-hydrochloride racemate (intermediate VIII), which comprises: 1. Condensation between intermediates VII and VIII to give intermediate VI 2. Hydrogenation of intermediate VI to give intermediate V 3. Resolution of intermediate V to give intermediate IV with enantiomeric purity >99% 4. Release of intermediate IV in a basic medium to give intermediate III 5. N-acylation reaction of intermediate III to give II (tofacitinib) 6. Salification of intermediate II to give tofacitinib monocitrate (I)
PIPERIDINE INHIBITORS OF JANUS KINASE 3
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Page/Page column 52, (2010/11/05)
The present invention relates to a new piperidine inhibitors of Janus Kinase 3 activity, pharmaceutical compositions thereof, and methods of use there-of.
Method of treatment of atherosclerosis
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Page/Page column 11, (2008/06/13)
A method of treating or preventing atherosclerosis comprising administering a compound of the formula wherein R1, R2 and R3 are as defined above.