1004-96-2Relevant academic research and scientific papers
Substituent effects in isoxazoles: Identification of 4-substituted isoxazoles as Michael acceptors
Lee, Connie K.Y.,Easton, Christopher J.,Gebara-Coghlan, Mariana,Radom, Leo,Scott, Anthony P.,Simpson, Gregory W.,Willis, Anthony C.
, p. 2031 - 2038 (2002)
Crystallographic and theoretical studies have been used to investigate substituent effects, which are manifest in electrochemical and yeast-catalysed reactions of 4- and 5-acyl-, alkoxycarbonyl-, cyano- and phenyl-substituted isoxazoles. The results show that isoxazoles substituted at the 4-position with π-electron-withdrawing substituents have enhanced C4-C5 bond polarity and are structurally similar to Michael acceptors. As a consequence there is elongation and weakening of their N-O bonds. By contrast, their 5-substituted regioisomers and isoxazoles substituted at C4 with conjugating, but not π-electron-withdrawing, substituents have diminished C4-C5 bond polarity. This results in the selective electrochemical and yeast-catalysed reduction of 4-substituted isoxazoles, as well as their hydrogenolytic ring cleavage and conjugate reduction with sodium borohydride.
N-SUBSTITUTED-3,4-(FUSED 5-RING)-5-PHENYL-PYRROLIDINE-2-ONE COMPOUNDS AS INHIBITORS OF ISOQC AND/OR QC ENZYME
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Page/Page column 427, (2021/02/12)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain N-substituted-3,4-(fused 5-ring)-5-phenyl-pyrrolidin-2-one compounds (also referred to herein as "FRPPO compounds"), that, inter alia, inhibit glutaminyl-peptide cyclotransferase-like (isoQC) enzyme and/or glutaminyl-peptide cyclotransferase (QC) enzyme (e.g., inhibit or reduce or block the activity or function of isoQC and/or QC enzyme). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit isoQC and/or QC enzyme; to treat disorders that are ameliorated by the inhibition of isoQC and/or QC enzyme; to treat cancer, atherosclerosis, fibrotic diseases, infectious diseases, Alzheimer's disease, etc.
HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS
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Paragraph 0671-0672; 0673, (2018/06/12)
Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
SUBSTITUTED BICYCLIC COMPOUNDS AS BROMODOMAIN INHIBITORS
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Paragraph 0165, (2016/07/05)
The present disclosure relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
HETEROCYCLIC NUCLEAR HORMONE RECEPTOR MODULATORS
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Paragraph 0700, (2014/07/08)
The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
Compounds Which Selectively Modulate The CB2 Receptor
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Page/Page column 24, (2011/04/18)
Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Generation of Nitrile Oxides via O-Tributylstannyl Aldoximes; Application to the Synthesis of Isoxazolines and Isoxazoles
Moriya, Osamu,Takenaka, Hideo,Iyoda, Masaichi,Urata, Yoshikiyo,Endo, Takeshi
, p. 413 - 418 (2007/10/02)
Nitrile oxides were generated readily by the reaction of aldoximes 1, with tert-butyl hypochlorite and bis(tributyltin) oxide.The reaction proceeded efficiently under mild conditions, in which O-stannylated aldoximes 2 are thought to be key intermediates.This reaction system was applicable to the one-pot syntheses of isoxazole derivatives 4 and 5 in the presence of dipolarophiles via a cycloaddition.
Stereoselectivity in the Peterson reaction - Application to the synthesis of BRL 49467
Bell, David,Crowe, Eleanor A.,Dixon, Nicholas J.,Geen, Graham R.,Mann, Inderjit S.,Shipton, Mark R.
, p. 6643 - 6652 (2007/10/02)
The E:Z selectivity in the introduction of the tri-substituted double bond in BRL 49467 could be controlled by the choice of base and silyl group used in a Peterson olefination reaction. The method allowing optimum E-selectivity was developed such that it
Synthesis of Isoxazolines and Isoxazoles via Generation of Nitrile Oxides from O-Stannyl Aldoximes
Moriya, Osamu,Takenaka, Hideo,Urata, Yoshikiyo,Endo, Takeshi
, p. 1671 - 1672 (2007/10/02)
The reactions of O-tributylstannyl aldoximes and active halogen compounds such as tert-butyl hypochlorite or N-bromosuccinimide, whereby nitrile oxides are generated effectively, are applied to the preparations of isoxazolines and isoxazoles via d
