37102-48-0Relevant academic research and scientific papers
Modular Access to Eight-Membered N-Heterocycles by Directed Carbonylative C?C Bond Activation of Aminocyclopropanes
Boyd, Olivia,Wang, Gang-Wei,Sokolova, Olga O.,Calow, Adam D. J.,Bertrand, Sophie M.,Bower, John F.
supporting information, p. 18844 - 18848 (2019/11/28)
Aminocyclopropanes equipped with pendant nucleophiles undergo carbonylative heterocyclization triggered by C?C bond activation to generate eight-membered N-heterocycles. In these processes, intramolecular “capture” of a rhodacyclopentanone intermediate by an aryl or N-based nucleophile is followed by C?C or C?N bond-forming “collapse” to the targets. These studies demonstrate how the combination of cyclopropane strain release and the templating effect of catalytically generated metallacycles can be harnessed to enable otherwise challenging medium ring closures.
Methylpyrrole inhibitors of BET bromodomains
Hasvold, Lisa A.,Sheppard, George S.,Wang, Le,Fidanze, Steven D.,Liu, Dachun,Pratt, John K.,Mantei, Robert A.,Wada, Carol K.,Hubbard, Robbert,Shen, Yu,Lin, Xiaoyu,Huang, Xiaoli,Warder, Scott E.,Wilcox, Denise,Li, Leiming,Buchanan, F. Greg,Smithee, Lauren,Albert, Daniel H.,Magoc, Terrance J.,Park, Chang H.,Petros, Andrew M.,Panchal, Sanjay C.,Sun, Chaohong,Kovar, Peter,Soni, Nirupama B.,Elmore, Steven W.,Kati, Warren M.,McDaniel, Keith F.
, p. 2225 - 2233 (2017/04/27)
An NMR fragment screen for binders to the bromodomains of BRD4 identified 2-methyl-3-ketopyrroles 1 and 2. Elaboration of these fragments guided by structure-based design provided lead molecules with significant activity in a mouse tumor model. Further mo
HETEROARYL DERIVATIVES AS SEPIAPTERIN REDUCTASE INHIBITORS
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Paragraph 00916-00918, (2017/05/31)
Inhibitors of sepiapterin reductase of formula (I) or (I'), wherein the substituents are defined as in the claims, and uses of sepiapterin reductase inhibitors in analgesia, treatment of acute and chronic pain, anti-inflammation, and immune cell regulation are disclosed.
Alkaloids from the traditional chinese medicine ChanSu: Synthesis-enabled structural reassignment of bufopyramide to bufoserotonin C
Davison, Emma K.,Sperry, Jonathan
supporting information, p. 7911 - 7914 (2015/07/27)
A synthesis of putative bufopyramide has shown the structure assigned to the natural product to be incorrect. The spectroscopic data for the natural product bufopyramide matches that obtained from a synthetic sample of bufoserotonin C, confirming that the
PYRROLE AMIDE INHIBITORS
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Paragraph 0604, (2014/09/30)
The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R10 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
