- The role of methoxy substituents in regulating the activity of selenides that serve as spirodioxyselenurane precursors and glutathione peroxidase mimetics
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A series of o-(hydroxymethyl)phenyl selenides containing single or multiple methoxy substituents was synthesized, and the rate at which each compound catalyzed the oxidation of benzyl thiol to its disulfide with excess hydrogen peroxide was measured. This
- Press, David J.,Back, Thomas G.
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Read Online
- PhI(OAc)2-mediated dearomative C-N coupling: Facile construction of the spiro[indoline-3,2′-pyrrolidine] skeleton
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A facile construction of the spiro[indole-3,2′-pyrrolidine] skeleton, through diacetoxyiodobenzene (PIDA) mediated C-N bond-forming dearomatization of C3 sulfonamide linked indole derivatives, has been developed. A variety of spiro-indolepyrrolidines were
- Zhou, Yali,Li, Dengke,Tang, Shi,Sun, Hongwei,Huang, Jinbo,Zhu, Qiang
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supporting information
p. 2039 - 2042
(2018/03/27)
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- Easy Access to Quinolin-2(1 H)-ones via a One-Pot Tandem Oxa-Michael-Aldol Sequence
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An efficient strategy for the synthesis of a variety of quinolin-2(1 H)-one derivatives has been developed. The reaction proceeded from cinnamide derivatives via a tandem reaction in the presence of NaOH to afford the corresponding 2- quinolin-2(1 H)-one derivatives in good to excellent yields.
- Jarrige, Lucie,Merad, Jeremy,Zaied, Siwar,Blanchard, Florent,Masson, Géraldine
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p. 1724 - 1728
(2017/10/06)
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- Decarboxylative [4+2] Cycloaddition by Synergistic Palladium and Organocatalysis
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A novel reaction based on synergistic catalysis, combining palladium- and organocatalysis has been developed. The palladium catalyst activates vinyl benzoxazinanones via a decarboxylation to undergo a [4+2] cycloaddition with iminium-ion activated α,β-uns
- Leth, Lars A.,Glaus, Florian,Meazza, Marta,Fu, Liang,Th?gersen, Mathias K.,Bitsch, Emma A.,J?rgensen, Karl Anker
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supporting information
p. 15272 - 15276
(2016/12/03)
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- INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
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Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
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Paragraph 0476; 0477; 0478
(2015/05/05)
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- INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
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Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
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Page/Page column 72
(2014/02/15)
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- N-heterocyclic-carbene-catalyzed synthesis of 2-aryl indoles
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A convergent and efficient transition-metal-free catalytic synthesis of 2-aryl-indoles has been developed. The interception of a highly reactive and transient aza-ortho-quinone methide by an acyl anion equivalent generated through N-hetereocyclic carbene catalysis is central to this successful strategy. High yields and a wide scope as well as the streamlined synthesis of a kinase inhibitor are reported. Umpolung: N-heterocyclic carbene catalysis is used for the convergent and efficient transition-metal-free synthesis of 2-aryl-indoles. The interception of a highly reactive and transient aza-ortho-quinone methide by an acyl anion equivalent is central to this successful strategy. The reaction exhibits high yields and a wide scope, and it has been applied to a streamlined synthesis of a kinase inhibitor.
- Hovey, M. Todd,Check, Christopher T.,Sipher, Alexandra F.,Scheidt, Karl A.
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supporting information
p. 9603 - 9607
(2014/10/15)
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- Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands
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We have reported previously the novel δ opioid agonist KNT-127 which showed high affinity and selectivity for the δ receptor. Moreover, the analgesic effect of subcutaneously administered KNT-127 was more potent than that of a prototypical δ agonist (-)-TAN-67 in the acetic acid writhing test. This study of the structure-activity relationship of KNT-127 derivatives focused on the introduction of substituents onto the 5′-, 6′-, 7′- or 8′-position of the quinoline ring and revealed that many derivatives with 5′- or 8′-substituents showed high affinities and selectivities for the δ receptor. Especially, SYK-153 with an 8′-OH group showed the highest affinity and the most balanced and highest selectivity for the δ receptor among the synthesized compounds.
- Ida, Yoshihiro,Matsubara, Ayaka,Nemoto, Toru,Saito, Manabu,Hirayama, Shigeto,Fujii, Hideaki,Nagase, Hiroshi
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p. 5810 - 5831
(2012/11/06)
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- Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II: Broad-spectrum antibacterial agents with reduced hERG activity
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Novel non-fluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) are of interest for the development of new antibacterial agents that are not impacted by target-mediated cross-resistance with fluoroquinolones. Aminopiperidines that have a bicyclic aromatic moiety linked through a carbon to an ethyl bridge, such as 1, generally show potent broad-spectrum antibacterial activity, including quinolone-resistant isolates, but suffer from potent hERG inhibition (IC50= 3 M for 1). We now disclose the finding that new analogues of 1 with an N-linked cyclic amide moiety attached to the ethyl bridge, such as 24m, retain the broad-spectrum antibacterial activity of 1 but show significantly less hERG inhibition (IC 50= 31 M for 24m) and higher free fraction than 1. One optimized analogue, compound 24l, showed moderate clearance in the dog and promising efficacy against Staphylococcus aureus in a mouse thigh infection model.
- Reck, Folkert,Alm, Richard,Brassil, Patrick,Newman, Joseph,Dejonge, Boudewijn,Eyermann, Charles J.,Breault, Gloria,Breen, John,Comita-Prevoir, Janelle,Cronin, Mark,Davis, Hajnalka,Ehmann, David,Galullo, Vincent,Geng, Bolin,Grebe, Tyler,Morningstar, Marshall,Walker, Phil,Hayter, Barry,Fisher, Stewart
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p. 7834 - 7847
(2012/01/06)
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- COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS
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The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.
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