- Heterocyclic compound used as MNK inhibitor
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The invention relates to a heterocyclic compound, a pharmaceutical composition containing the heterocyclic compound, a preparation method thereof, and application thereof used as a mitogen activated protein kinase interacting kinase 1 and 2-MNK1/MNK2 inhibitor. The inhibitor is the heterocyclic compound as shown in the formula (I), or its pharmaceutically acceptable salt, prodrug, solvent compound, polycrystal, isomer, stable isotope derivative or a pharmaceutical composition containing the heterocyclic compound. The compound of the invention can be used for treating or preventing MNK-mediatedrelated diseases, such as cancers.
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- Hydrogen bonding-mediated self-assembly of square and triangular metallocyclophanes
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Intramolecular three-centered hydrogen bonding has been used to induce dipyridyl anthranilamide 5 and diphenylacetylene anthranilamide 11 to adopt rigid straight conformation. Compound 5 reacted with Pd(dppp)(OTf)2 (12a) or Pt(dppp)(OTf)2 (12b) in dichloromethane to afford square metallocyclophanes 13a and 13b in 70% and 40% yield, respectively. In contrast, the reaction of 11 with 12b in dichloromethane gave triangular metallocyclophane 14 in 15% yield.
- Wu, Zong-Quan,Jiang, Xi-Kui,Li, Zhan-Ting
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p. 8067 - 8070
(2007/10/03)
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- Inotropic 'A' ring substituted sulmazole and isomazole analogues
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A series of 'A' ring substituted sulmazole and isomazole analogues have been prepared and evaluated as inotropic agents. pK(A)'s, protonation sites, and log P values were measured for selected compounds and their electronic properties were calculated. No simple correlation between inotropic activity and pK(A), protonation site, or log P value was observed. However, in vitro inotropism did correlate with the calculated charge density of the 'B' ring imidazo nitrogen atom. The 6-position of sulmazole appeared to be the most tolerant toward substituents, th 6-amino derivative 7 being a more potent inotrope than sulmazole itself. 4-Methoxyisomazole 13 had comparable in vivo inotropic properties to those of isomazole.
- Barraclough,Black,Cambridge,Collard,Firmin,Gerskowitch,Glen,Giles,Hill,Hull,Iyer,King,Kneen,Lindon,Nobbs,Randall,Shah,Smith,Vine,et al.
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p. 2231 - 2239
(2007/10/02)
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