90892-59-4Relevant articles and documents
PRMT5 INHIBITORS
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Page/Page column 38, (2021/06/26)
The present invention provides a compound selected from: compounds A, B, C, D and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds disclosed herein, pharmaceutic
CEREBLON BINDERS FOR THE DEGRADATION OF IKAROS
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Page/Page column 377; 378, (2019/10/23)
The present invention provides cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway along with their use in therapeutic applications as described herein.
Development of two diastereoselective routes towards trans-4-aminomethyl-piperidin-3-ol building blocks
Gijsen, Harrie J.M.,De Cleyn, Michel J.A.,Love, Christopher J.,Surkyn, Michel,Van Brandt, Sven F.A.,Verdonck, Marc G.C.,Moens, Luc,Cuypers, Jef,Bosmans, Jean-Paul R.M.A.
, p. 2456 - 2464 (2008/09/18)
Two diastereoselective, scaleable routes towards trans-3,4-disubstituted piperidines with a 4-hydroxymethyl-3-hydroxy or 4-aminomethyl-3-hydroxy substitution pattern are being described. In the first route, the 3,4-trans configuration was introduced regio- and diastereoselectively via a hydroboration/oxidation sequence starting from 4-hydroxymethylpyridine. In the second route, regioselective epoxide ring opening of N-benzyl-3,4-epoxy-piperidine was achieved with LiCN, in situ generated from acetocyanohydrin and LiNH2. The regioselectivity of both the hydroboration and the epoxide ring opening was positively influenced by the presence of the basic piperidine nitrogen. Both routes have been optimized to be performed at large scale.