- Gas-liquid flow hydrogenation of nitroarenes: Efficient access to a pharmaceutically relevant pyrrolobenzo[1,4]diazepine scaffold
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Using a Tube-in-Tube device based on the amorphous Teflon AF-2400 fluoropolymer, a series of nitroarenes was hydrogenated to afford the corresponding aniline compounds. The system was then applied to the construction of a pyrrolobenzo[1,4]diazapene scaffold through a tandem hydrogenation-condensation-hydrogenation sequence.
- Dimitriou, Eleni,Jones, Richard H.,Pritchard, Robin G.,Miller, Gavin J.,O'Brien, Matthew
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p. 6795 - 6803
(2018/10/15)
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- COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
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The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.
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Paragraph 0448; 0449; 0450; 0451
(2013/03/26)
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- COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
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The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.
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Page/Page column 90
(2013/03/28)
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- COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
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The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.
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Paragraph 0464; 0465
(2013/03/26)
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- COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
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The invention provides compounds of formulae (I) and (II) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRcalpha PDGFRbeta) kinases
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Page/Page column 104; 105
(2013/03/28)
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- Synthesis and pharmacological evaluation of 2-aryloxy/arylamino-5- cyanobenzenesulfonylureas as novel thromboxane A2 receptor antagonists
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New series of original 2-aryloxy/arylamino-5-cyanobenzenesulfonylureas were synthesized and evaluated as thromboxane A2 receptor (TP receptor) antagonists. A functional pharmacological test was used, which consisted of measuring the inhibition
- Bambi-Nyanguile, Sylvie-Mireille,Hanson, Julien,Ooms, Annie,Alpan, Lutfiye,Kolh, Philippe,Dogné, Jean-Michel,Pirotte, Bernard
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- THERAPEUTIC AGENT FOR CEREBRAL INFARCTION
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The invention provides a therapeutic drug for ischemic stroke. The therapeutic drug has the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof, as an active ingredient.
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- TETRAZOLE DERIVATIVES
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The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases.
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Page/Page column 27
(2011/02/24)
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- Thiazolyl-Dihydro-Indazole
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The present invention encompasses compounds of general formula (1) wherein R1 to R6 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use th
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Page/Page column 11; 12
(2008/06/13)
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