1116228-85-3Relevant articles and documents
PYRIMIDINE DERIVATIVE AND USE THEREOF
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, (2018/09/27)
The present invention provides a pyrimidine derivative and a use thereof. The pyrimidine derivative is the compound shown in formula I or a pharmaceutically acceptable salt, hydrate, solvate, metabolite or prodrug thereof, wherein, R1, R2, R3, R4 and R5 are, for example, as defined in the specification. The compound can act as an ALK inhibitor, and is for preparing an anti-tumor medicament for suppressing an anaplastic lymphoma kinase.
Tyrosine Kinase Inhibitor And Uses Thereof
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, (2017/05/15)
Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.
Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f ][1,2,4]triazines: Identification of orally bioavailable, efficacious ALK inhibitors
Mesaros, Eugen F.,Thieu, Tho V.,Wells, Gregory J.,Zificsak, Craig A.,Wagner, Jason C.,Breslin, Henry J.,Tripathy, Rabindranath,Diebold, James L.,McHugh, Robert J.,Wohler, Ashley T.,Quail, Matthew R.,Wan, Weihua,Lu, Lihui,Huang, Zeqi,Albom, Mark S.,Angeles, Thelma S.,Wells-Knecht, Kevin J.,Aimone, Lisa D.,Cheng, Mangeng,Ator, Mark A.,Ott, Gregory R.,Dorsey, Bruce D.
, p. 115 - 125 (2012/03/11)
Chemical strategies to mitigate cytochrome P450-mediated bioactivation of novel 2,7-disubstituted pyrrolo[2,1-f][1,2,4]triazine ALK inhibitors are described along with synthesis and biological activity. Piperidine-derived analogues showing minimal microsomal reactive metabolite formation were discovered. Potent, selective, and metabolically stable ALK inhibitors from this class were identified, and an orally bioavailable compound (32) with antitumor efficacy in ALK-driven xenografts in mouse models was extensively characterized.