- ISOQUINOLINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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The present invention relates to a compound suitable for use as a kinase inhibitor
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Page/Page column 174-176
(2021/02/12)
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- ERK INHIBITORS
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The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.
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Page/Page column 91
(2016/07/05)
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- Titania-promoted carboxylic acid alkylations of alkenes and cascade addition-cyclizations
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Photochemical reactions employing TiO2 and carboxylic acids under dry anaerobic conditions led to several types of C-C bond-forming processes with electron-deficient alkenes. The efficiency of alkylation varied appreciably with substituents in the carboxylic acids. The reactions of aryloxyacetic acids with maleimides resulted in a cascade process in which a pyrrolochromene derivative accompanied the alkylated succinimide. The selectivity for one or other of these products could be tuned to some extent by employing the photoredox catalyst under different conditions. Aryloxyacetic acids adapted for intramolecular ring closures by inclusion of 2-alkenyl, 2-aryl, or 2-oximinyl functionality reacted rather poorly. Profiles of reactant consumption and product formation for these systems were obtained by an in situ NMR monitoring technique. An array of different catalyst forms were tested for efficiency and ease of use. The proposed mechanism, involving hole capture at the TiO2 surface by the carboxylates followed by CO2 loss, was supported by EPR spectroscopic evidence of the intermediates. Deuterium labeling indicated that the titania likely donates protons from surface hydroxyl groups as well as supplying electrons and holes, thus acting as both a catalyst and a reaction partner.
- Manley, David W.,McBurney, Roy T.,Miller, Phillip,Walton, John C.,Mills, Andrew,O'Rourke, Christopher
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p. 1386 - 1398
(2014/03/21)
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- Lewis-acid-mediated ring-exchange reaction of dihydrobenzofurans and its application to the formal total synthesis of (-)-quinocarcinamide
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An unusual Lewis-acid-mediated ring-exchange reaction of dihydrobenzofurans is described. The fused tricyclic ring system is the key structural element for this reaction as it restricts C-N bond rotation and/or destabilizes the benzofuran ring. We achieved the formal total synthesis of (-)-quinocarcinamide using a combination of this reaction and the Au(I)-catalyzed 6-endo-dig hydroamination of an alkyne.
- Chiba, Hiroaki,Sakai, Yuki,Oishi, Shinya,Fujii, Nobutaka,Ohno, Hiroaki
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supporting information
p. 6273 - 6276,4
(2012/12/12)
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- Lewis-acid-mediated ring-exchange reaction of dihydrobenzofurans and its application to the formal total synthesis of (-)-quinocarcinamide
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An unusual Lewis-acid-mediated ring-exchange reaction of dihydrobenzofurans is described. The fused tricyclic ring system is the key structural element for this reaction as it restricts C-N bond rotation and/or destabilizes the benzofuran ring. We achieved the formal total synthesis of (-)-quinocarcinamide using a combination of this reaction and the Au(I)-catalyzed 6-endo-dig hydroamination of an alkyne.
- Chiba, Hiroaki,Sakai, Yuki,Oishi, Shinya,Fujii, Nobutaka,Ohno, Hiroaki
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supporting information
p. 6273 - 6276
(2013/01/14)
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- PURINE AND IMIDAZOPYRIDINE DERIVATIVES FOR IMMUNOSUPPRESSION
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The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulas ( I ) and ( II ).
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Page/Page column 103; 106-107
(2010/11/24)
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- Q.S.A.R. DE DERIVES DE DIHYDRO-2,3 BENZOFURANNAMINE-3 INHIBITEURS DE CROISSANCE VEGETALE
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A series of N-(aminoacetyl)-2,3-dihydro-3-benzofurannamine were synthetized and tested by means of the growth inhibition technical using Lepidium Sativum L. root meristem.Simultaneous applications of Fujita-Ban, Hansch methods and molecular connectivity have shown the preponderant role of lipophilicity and of pKa determined experimentally.
- Turan-Zitouni, G.,Berge, G.,Noel-Artis, A. M.,Chevallet, P.,Fulcrand, P.,Castel, J.
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p. 643 - 656
(2007/10/02)
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