- Synthesis of carbon-11-labeled 4-(phenylamino)-pyrrolo[2,1-f][1,2,4] triazine derivatives as new potential PET tracers for imaging of p38α mitogen-activated protein kinase
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The reference standards methyl 4-(2-methyl-5-(methoxycarbamoyl)phenylamino) -5-methylpyrrolo[2,1-f][1,2,4]triazine-6-carboxylate (10a), methyl 4-(2-methyl-5-(ethoxycarbamoyl)phenylamino)-5-methylpyrrolo[2,1-f][1,2,4] triazine-6-carboxylate (10b) and corre
- Wang, Min,Gao, Mingzhang,Zheng, Qi-Huang
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p. 3700 - 3705
(2014/09/17)
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- Pyrrolotriazine inhibitors of kinases
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The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
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Page/Page column 33
(2008/06/13)
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- Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors
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A versatile synthesis of the suitably functionalized pyrrolo[2,1-f][1,2,4] triazine nucleus is described. SAR at the C-5 and C-6 positions of the 4-(3-hydroxy-4-methylphenylamino)pyrrolo[2,1-f][1,2,4]triazine template led to compounds with good in vitro potency against VEGFR-2 kinase. Glucuronidation of the phenol group is mitigated by incorporation of a basic amino group on the C-6 side chain of the pyrrolotriazine nucleus.
- Borzilleri, Robert M.,Cai, Zhen-Wei,Ellis, Christopher,Fargnoli, Joseph,Fura, Aberra,Gerhardt, Tracy,Goyal, Bindu,Hunt, John T.,Mortillo, Steven,Qian, Ligang,Tokarski, John,Vyas, Viral,Wautlet, Barri,Zheng, Xioping,Bhide, Rajeev S.
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p. 1429 - 1433
(2007/10/03)
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- Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors
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Methods of treating one or more conditions associated with p38 kinase activity are disclosed comprising administering to a patient in need thereof at least one compound having the formula (I): 1or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, or NH2, preferably methyl, and X, R1 through R6, and Z are as described in the specification. Advantageously the groups —ZR4R5 taken together comprise an —NH-substituted aryl.
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