- PYRROLO[2,1-F][1,2,4]TRIAZINE DERIVATIVES SERVING AS SELECTIVE HER2 INHIBITORS AND APPLICATION THEREOF
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The present invention relates to a group of pyrrolo[2, 1-f][1,2,4]triazine derivatives serving as selective HER2 inhibitors and an application thereof in the preparation of a drug that serves as an HER2 inhibitor. Specifically, the present invention relates to a compound represented by formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof.
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- New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
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Novel C-5 substituted pyrrolotriazines were optimized for dual EGFR and HER2 protein tyrosine kinase inhibition. The lead compound exhibited promising oral efficacy in both EGFR and HER2 driven human tumor xenograft models. It is hypothesized that its C-5
- Mastalerz, Harold,Chang, Ming,Chen, Ping,Dextraze, Pierre,Fink, Brian E.,Gavai, Ashvinikumar,Goyal, Bindu,Han, Wen-Ching,Johnson, Walter,Langley, David,Lee, Francis Y.,Marathe, Punit,Mathur, Arvind,Oppenheimer, Simone,Ruediger, Edward,Tarrant, James,Tokarski, John S.,Vite, Gregory D.,Vyas, Dolatrai M.,Wong, Henry,Wong, Tai W.,Zhang, Hongjian,Zhang, Guifen
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p. 2036 - 2042
(2007/10/03)
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- PYRROLOTRIAZINE COMPOUNDS AS KINASE INHIBITORS
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The present invention provides compounds of formula (I); and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative 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 33-34
(2008/06/13)
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- Di-substituted pyrrolotrizine compounds
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The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
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Page/Page column 11
(2010/02/13)
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