- Thermal synthesis of 3-bromothieno[3,2-c]pyridin-4-(5h)-one: A telescoped procedure with tributylamine
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3-Bromothieno[3,2-c]pyridine-4-(5H)-one (1) was prepared from (2E)-3-(4-bromo-2-thienyl)-2- propenoic acid (3) by the Eloy-Deryckere thermal benzo/heteropyridinone synthesis. A telescoped procedure was developed, which reduces some of the risk associated with the classic procedure. Use of tributylamine as an additive in this process was shown to facilitate E/Z-isomerization of the intermediate vinyl isocyanate and lower the temperature necessary for the overall thermal process.
- Boros, Eric E.,Kaldor, Istvan
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Read Online
- NEW BICYCLIC DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Compounds of formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, W, A and n are as defined in the description. Medicaments.
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Page/Page column 111
(2017/05/12)
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- NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
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The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders
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- Improved synthesis of 3-substituted-4-amino-[3,2-c]-thienopyridines
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(Chemical Equation Presented) Two syntheses of 3-substituted-4-amino-[3,2- c]thienopyridines have been developed to replace the standard literature route to these compounds, which uses unattractive conditions involving azide and high temperatures. The fir
- Engstrom, Kenneth M.,Baize, Amanda L.,Franczyk, Thaddeus S.,Kallemeyn, Jeffrey M.,Mulhern, Mathew M.,Rickert, Robert C.,Wagaw, Seble
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experimental part
p. 3849 - 3855
(2009/09/26)
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- Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases
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A novel class of 3,7-diphenyl-4-amino-thieno and furo[3,2-c]pyridine has been designed based on pharmacophore models of ATP competitive kinase inhibitors. Versatile synthetic methods via double Suzuki coupling to explore SAR have been established and potent inhibitors against angiogenetic targets, VEGFR2, Tie-2, and EphB4, have been successfully discovered.
- Miyazaki, Yasushi,Nakano, Masato,Sato, Hideyuki,Truesdale, Anne T.,Stuart, J. Darren,Nartey, Eldridge N.,Hightower, Kendra E.,Kane-Carson, Laurie
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p. 250 - 254
(2007/10/03)
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- Thienopyridine urea inhibitors of KDR kinase
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A series of substituted thienopyridine ureas was prepared and evaluated for enzymatic and cellular inhibition of KDR kinase activity. Several of these analogs, such as 2, are potent inhibitors of KDR (10 nM) in both enzymatic and cellular assays. Further
- Heyman, H. Robin,Frey, Robin R.,Bousquet, Peter F.,Cunha, George A.,Moskey, Maria D.,Ahmed, Asma A.,Soni, Niru B.,Marcotte, Patrick A.,Pease, Lori J.,Glaser, Keith B.,Yates, Melinda,Bouska, Jennifer J.,Albert, Daniel H.,Black-Schaefer, Candace L.,Dandliker, Peter J.,Stewart, Kent D.,Rafferty, Paul,Davidsen, Steven K.,Michaelides, Michael R.,Curtin, Michael L.
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p. 1246 - 1249
(2007/10/03)
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- Discovery of thienopyridines as Src-family selective Lck inhibitors
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We describe the identification, SAR, and in vivo pharmacology of a new series of Src-family selective Lck inhibitors. These thienopyridines were designed based on a desire to access the unique residues in the extended hinge region of Lck.
- Abbott, Lily,Betschmann, Patrick,Burchat, Andrew,Calderwood, David J.,Davis, Heather,Hrnciar, Peter,Hirst, Gavin C.,Li, Biqin,Morytko, Michael,Mullen, Kelly,Yang, Bryant
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p. 1167 - 1171
(2007/10/03)
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- Compounds
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Thienopyridine compounds which are potassium channel inhibitors are described. Pharmaceutical compositions comprising the compounds and their use in the treatment or prevention of cancer, arrhythmias, autoimmune diseases and inflammatory diseases, including gastric cancer, atrial fibrillation, type-2 diabetes mellitus, rheumatoid arthritis, type-1 diabetes, inflammatory bowel disorder and demyelinating disorders such as multiple sclerosis are also disclosed.
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Page/Page column 8
(2010/11/27)
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- Thienopyridine and furopyridine kinase inhibitors
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Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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- Thienopyridine kinase inhibitors
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Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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- Thienopyridine and furopyridine kinase inhibitors
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Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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Page/Page column 26
(2010/02/10)
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- NOVEL CHEMICAL COMPOUNDS
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This invention relates to newly identified compounds for treating and preventing tumors ans cancers, and methods for treating proliferative diseases associated with the imbalance or inappropriate activity of tyrosine kinases implicated in proliferative diseases.
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Page 26-27; 17
(2008/06/13)
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