- N-(SUBSTITUTED-PHENYL)-SULFONAMIDE DERIVATIVES AS KINASE INHIBITORS
-
The invention relates to N-(substituted-phenyl)-sulfonamide compounds, which are extremely useful as inhibitors of protein kinases (e.g. PERK kinase) and accordingly can be used for the treatment of cell proliferative disorders, such as cancer, or diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
- -
-
Page/Page column 28-29
(2018/04/11)
-
- Improved synthesis of 3-substituted-4-amino-[3,2-c]-thienopyridines
-
(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
-
experimental part
p. 3849 - 3855
(2009/09/26)
-
- Inhibitors of protein kinases
-
Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
- -
-
Page/Page column 20
(2010/11/27)
-
- 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
-
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
-
p. 250 - 254
(2007/10/03)
-
- Thienopyridine urea inhibitors of KDR kinase
-
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.
-
p. 1246 - 1249
(2007/10/03)
-
- Discovery of thienopyridines as Src-family selective Lck inhibitors
-
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
-
p. 1167 - 1171
(2007/10/03)
-
- Thienopyridine and furopyridine kinase inhibitors
-
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.
- -
-
-
- Thienopyridine kinase inhibitors
-
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.
- -
-
-
- Thienopyridine and furopyridine kinase inhibitors
-
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.
- -
-
Page/Page column 56
(2010/02/10)
-
- NOVEL CHEMICAL COMPOUNDS
-
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.
- -
-
-
