137469-90-0Relevant articles and documents
High-Potency Phenylquinoxalinone Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Activators
Son, Jung-Ho,Zhu, Jie S.,Phuan, Puay-Wah,Cil, Onur,Teuthorn, Andrew P.,Ku, Colton K.,Lee, Sujin,Verkman, Alan S.,Kurth, Mark J.
, p. 2401 - 2410 (2017/04/03)
We previously identified phenylquinoxalinone CFTRact-J027 (4) as a cystic fibrosis transmembrane conductance regulator (CFTR) activator with an EC50 of ~200 nM and demonstrated its therapeutic efficacy in mouse models of constipation. Here, structure-activity studies were done on 36 synthesized phenylquinoxalinone analogs to identify compounds with improved potency and altered metabolic stability. Synthesis of the phenylquinoxalinone core was generally accomplished by condensation of 1,2-phenylenediamines with substituted phenyloxoacetates. Structure-activity studies established, among other features, the privileged nature of a properly positioned nitro moiety on the 3-aryl group. Synthesized analogs showed improved CFTR activation potency compared to 4 with EC50 down to 21 nM and with greater metabolic stability. CFTR activators have potential therapeutic indications in constipation, dry eye, cholestatic liver diseases, and inflammatory lung disorders.
HETEROCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING THE SAME
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Paragraph 0281 - 0284, (2016/11/28)
The present specification provides a heterocyclic compound and an organic light emitting device using the same. The organic light emitting device comprises: a first electrode; a second electrode facing the first electrode; and one or more organic material layers including a light emitting layer formed between the first electrode and the second electrode, wherein the organic material layers comprise the heterocyclic compound.COPYRIGHT KIPO 2015
Synthesis of Bi- and Tri-cyclic Tetrazepinones
Bertrand, J. Jean-Claude,Just, George
, p. 2525 - 2529 (2007/10/02)
Diazotization of N,N'-dialkyl-N-(o-aminophenyl) ureas 7, 13 and 17 gave 3,5-dimethyl-3H-1,2,3,5-benzotetrazepin-4(5H)-one 8, 3-methyl-6,7-dihydro-1,2,3,5-tetrazepinoquinolin-4(3H)-one 14 and 3-methyl-6,7-dihydrooxazino-1,2,3,5-benzotetrazepin-4-one 19.The structures of these bi- and tri-cyclic systems were confirmed by 1H, 13C and 15N NMR data.X-Ray diffraction of compound 14 shows that the tetrazepinone ring is nonplanar.