- IMIDAZOPYRIDINYL COMPOUNDS AND USE THEREOF FOR TREATMENT OF PROLIFERATIVE DISORDERS
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The present disclosure provides a compound of Formula (I) or pharmaceutically acceptable salt, stereoisomers thereof, a pharmaceutical composition comprising the compound, and a method to treat or prevent cancer diseases and/or proliferative disorders usi
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Paragraph 0113-0115
(2020/09/08)
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- Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors
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A series of imidazo[1,2-a]pyridin-6-yl-benzamide analogs was designed as inhibitors of B-RAFV600E. Medicinal chemistry techniques were employed to explore the SAR for this series and improve selectivity versus P38 and VEGFR2.
- Smith, Aaron,Ni, Zhi-Jie,Poon, Daniel,Huang, Zilin,Chen, Zheng,Zhang, Qiong,Tandeske, Laura,Merritt, Hanne,Shoemaker, Kevin,Chan, John,Kaufman, Susan,Huh, Kay,Murray, Jeremy,Appleton, Brent A.,Cowan-Jacob, Sandra W.,Scheufler, Clemens,Kanazawa, Takanori,Jansen, Johanna M.,Stuart, Darrin,Shafer, Cynthia M.
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supporting information
p. 5221 - 5224
(2017/11/01)
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- Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K
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PI3 kinases are a family of lipid kinases mediating numerous cell processes such as proliferation, migration and differentiation. The PI3 Kinase pathway is often de-regulated in cancer through PI3Kα overexpression, gene amplification, mutations and PTEN p
- Pecchi, Sabina,Ni, Zhi-Jie,Han, Wooseok,Smith, Aaron,Lan, Jiong,Burger, Matthew,Merritt, Hanne,Wiesmann, Marion,Chan, John,Kaufman, Susan,Knapp, Mark S.,Janssen, Johanna,Huh, Kay,Voliva, Charles F.
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supporting information
p. 4652 - 4656
(2013/08/23)
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- Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors
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Imidazo[1,2-a]pyridine derivatives were designed, synthesized, and evaluated as inhibitors of the apoptosis signal-regulating kinase 1 (ASK1). These were based on a benzothiazole derivative that was discovered from high-throughput screening of our compound library. As a result, we identified potent, selective, and orally bioavailable ASK1 inhibitors for wide range of therapeutic targets.
- Terao, Yoshito,Suzuki, Hideo,Yoshikawa, Masato,Yashiro, Hiroaki,Takekawa, Shiro,Fujitani, Yasushi,Okada, Kengo,Inoue, Yoshihisa,Yamamoto, Yoshio,Nakagawa, Hideyuki,Yao, Shuhei,Kawamoto, Tomohiro,Uchikawa, Osamu
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supporting information
p. 7326 - 7329
(2013/02/21)
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- Fragment based discovery of a novel and selective PI3 kinase inhibitor
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We report the use of fragment screening and fragment based drug design to develop a PI3c kinase fragment hit into a lead. Initial fragment hits were discovered by high concentration biochemical screening, followed by a round of virtual screening to identify additional ligand efficient fragments. These were developed into potent and ligand efficient lead compounds using structure guided fragment growing and merging strategies. This led to a potent, selective, and cell permeable PI3c kinase inhibitor with good metabolic stability that was useful as a preclinical tool compound.
- Hughes, Samantha J.,Millan, David S.,Kilty, Iain C.,Lewthwaite, Russell A.,Mathias, John P.,Reilly, Mark A.O.,Pannifer, Andrew,Phelan, Anne,Stühmeier, Frank,Baldock, Darren A.,Brown, David G.
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scheme or table
p. 6586 - 6590
(2011/12/04)
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- PI-3 KINASE INHIBITORS AND METHODS OF THEIR USE
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Phosphatidylinositol (PI) 3 kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceuticall
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Page/Page column 62-63
(2010/11/28)
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