3783-61-7Relevant articles and documents
AN IMPROVED PROCESS FOR THE PREPARATION OF UPADACITINIB INTERMEDIATE
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Page/Page column 5-6, (2022/03/09)
The present invention provides an improved process for the preparation of upadacitinib of intermediate of formula II by reacting formula B with Grignard reagent in presence of an Iron catalyst.
An aza-nucleoside, fragment-like inhibitor of the DNA repair enzyme alkyladenine glycosylase (AAG)
Al Yahyaei, Balqees,Chu, Shuyu,Elliott, Ruan M.,Howlin, Brendan J.,Imperato, Manuel,Lopez, Arnaud,Mas Claret, Eduard,Meira, Lisiane B.,Whelligan, Daniel K.
, (2020/04/23)
The DNA repair enzyme AAG has been shown in mice to promote tissue necrosis in response to ischaemic reperfusion or treatment with alkylating agents. A chemical probe inhibitor is required for investigations of the biological mechanism causing this phenomenon and as a lead for drugs that are potentially protective against tissue damage from organ failure and transplantation, and alkylative chemotherapy. Herein, we describe the rationale behind the choice of arylmethylpyrrolidines as appropriate aza-nucleoside mimics for an inhibitor followed by their synthesis and the first use of a microplate-based assay for quantification of their inhibition of AAG. We finally report the discovery of an imidazol-4-ylmethylpyrrolidine as a fragment-sized, weak inhibitor of AAG.
GNAQ targeted dsRNA compositions and methods for inhibiting expression
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Page/Page column 41, (2017/03/08)
The invention relates to a double-stranded ribonucleic acid (dsRNA) targeting a G-alpha q subunit (GNAQ) of a heterotrimeric G gene, and methods of using the dsRNA to inhibit expression of GNAQ.
