- KINASE INHIBITORS
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Disclosed herein are protein kinase inhibitors, in particular Bruton's tyrosine kinase (BTK) inhibitors, pharmaceutical compositions comprising them, processes for preparing them and uses of such protein kinase inhibitors to treat or prevent diseases, disorders and conditions associated with kinase function. In particular, the present invention relates to selective BTK inhibitors.
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Page/Page column 102
(2021/10/15)
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- Intramolecular Reductive Cyclization of o-Nitroarenes via Biradical Recombination
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A visible-light-induced/thiourea-mediated intramolecular cyclization of o-nitroarenes under mild conditions is realized for the first time, which provides an efficient and environmentally friendly way to access pharmaceutical relevant quinazolinone derivatives. The reaction can be easily extended to gram level by using a continuous-flow setup with high efficiency. Mechanistic investigation including control experiments, transient fluorescence, UV-vis spectra, and DFT calculations suggests that the formation of active biradical intermediates via intramolecular single electron transfer (SET) is key stage in the catalytic cycle.
- Lu, Cong,Su, Zhishan,Jing, Dong,Jin, Songyang,Xie, Lijuan,Li, Liangrui,Zheng, Ke
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p. 1438 - 1443
(2019/03/07)
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- Metal-Free Synthesis of Polycyclic Quinazolinones Enabled by a (NH4)2S2O8-Promoted Intramolecular Oxidative Cyclization
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An efficient metal-free, (NH4)2S2O8 mediated intramolecular oxidative cyclization for the construction of polycyclic heterocycles was disclosed. A series of polycyclic quinazolinone derivatives with good functional group tolerance were obtained in high yields. The natural products tryptanthrin and rutaecarpine, as well as their derivatives, were easily synthesized by this strategy. A preliminary mechanism study suggested the carbon-centered radical was involved in the catalytic cycle.
- Xie, Lijuan,Lu, Cong,Jing, Dong,Ou, Xinrui,Zheng, Ke
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p. 3649 - 3653
(2019/06/04)
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- Tetrahydroisoquinoline compound and its preparation method, pharmaceutical composition and use
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The invention relates to a tetrahydroisoquinoline compound and its preparation method, pharmaceutical composition and use. The tetrahydroisoquinoline compound is shown by the general formula (1). In the general formula (1), the symbols have the same definitions as in the specification.
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Paragraph 0225-0226
(2018/03/24)
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- Heterocyclic compound with Wnt signal path inhibitory activity and application thereof
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The invention provides a heterocyclic compound with Wnt signal path inhibitory activity. The heterocyclic compound and chemically acceptable salt, isotope, isomer and a crystal structure thereof are provided with a structure shown as the general formula I (see the formula in the description). The invention further provides application of the heterocyclic compound with the Wnt signal path inhibitory activity. The heterocyclic compound with the Wnt signal path inhibitory activity serves as effective antagonist of a Wnt signal path, and can be used for treating or preventing diseases caused by abnormity of the Wnt signal path.
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Paragraph 0191; 0196; 0197
(2016/10/08)
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- An unusual chemoselective hydrogenation of quinoline compounds using supported gold catalysts
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The pursuit of modern sustainable chemistry has stimulated the development of innovative catalytic processes that enable chemical transformations to be performed under mild and clean conditions with high efficiency. Herein, we report that gold nanoparticles supported on TiO2 catalyze the chemoselective hydrogenation of functionalized quinolines with H2 under mild reaction conditions. Our results point toward an unexpected role for quinolines in gold-mediated hydrogenation reactions, namely that of promoter; this is in stark contrast to what prevails in the traditional noble metal Pd-, Pt-, and Ru-based catalyst systems, in which quinolines and their derivatives typically act as poisons. As a result of the remarkable promotional effect of quinoline molecules to H2 activation over supported gold, the transformation can proceed smoothly under very mild conditions (even at temperatures as low as 25 °C). Of practical significance is that various synthetically useful functional groups including halogens, ketone, and olefin remain intact during the hydrogenation of quinolines. Moreover, the protocol also shows promise for the regiospecific hydrogenation of the heterocyclic ring of a variety of other biologically important heteroaromatic nitrogen compounds, such as isoquinoline, acridine, and 7,8-benzoquinoline, in a facile manner. Apart from its importance in catalytic hydrogenation, we believe that this intriguing self-promoted effect by reactant molecules may have fundamental implications for the broad field of gold catalysis and form the basis for development of new catalytic procedures for other key transformations.
- Ren, Dong,He, Lin,Yu, Lei,Ding, Ran-Sheng,Liu, Yong-Mei,Cao, Yong,He, He-Yong,Fan, Kang-Nian
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p. 17592 - 17598,7
(2012/12/12)
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- NOVEL COMPOUNDS
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The invention provides novel hydantoin derivatives; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
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Page/Page column 45
(2009/03/07)
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