- Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine-a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays
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We describe the identification of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine (3), a potent, orally active Src inhibitor with desirable PK properties, demonstrated activity in human tumor cell lines
- Noronha, Glenn,Barrett, Kathy,Boccia, Antonio,Brodhag, Tessa,Cao, Jianguo,Chow, Chun P.,Dneprovskaia, Elena,Doukas, John,Fine, Richard,Gong, Xianchang,Gritzen, Colleen,Gu, Hong,Hanna, Ehab,Hood, John D.,Hu, Steven,Kang, Xinshan,Key, Jann,Klebansky, Boris,Kousba, Ahmed,Li, Ge,Lohse, Dan,Mak, Chi Ching,McPherson, Andrew,Palanki, Moorthy S.S.,Pathak, Ved P.,Renick, Joel,Shi, Feng,Soll, Richard,Splittgerber, Ute,Stoughton, Silva,Tang, Suhan,Yee, Shiyin,Zeng, Binqi,Zhao, Ningning,Zhu, Hong
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p. 602 - 608
(2007/10/03)
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- Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors
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We report the discovery and preliminary SAR studies of a series of structurally novel benzotriazine core based small molecules as inhibitors of Src kinase. To the best of our knowledge, benzotriazine template based compounds have not been reported as kina
- Noronha, Glenn,Barrett, Kathy,Cao, Jianguo,Dneprovskaia, Elena,Fine, Richard,Gong, Xianchang,Gritzen, Colleen,Hood, John,Kang, Xinshan,Klebansky, Boris,Li,Liao,Lohse, Dan,Mak, Chi Ching,McPherson, Andrew,Palanki, Moorthy S.S.,Pathak, Ved P.,Renick, Joel,Soll, Richard,Splittgerber, Ute,Wrasidlo, Wolfgang,Zeng, Binqi,Zhao, Ningning,Zhou
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p. 5546 - 5550
(2007/10/03)
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- Benzotriazine inhibitors of kinases
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The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.
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Page/Page column 28
(2008/06/13)
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- Vasculostatic agents and methods of use thereof
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Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as retinopathies or macular degeneration or other vitreoretinal diseases, inflammatory diseases, vascular leakage syndrome, edema, transplant rejection, adult/acute respiratory distress syndrome (ARDS), and the like.
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