913173-72-5Relevant academic research and scientific papers
Bioisosteric discovery of npa101.3, a second-generation ret/vegfr2 inhibitor optimized for single-agent polypharmacology
Moccia, Marialuisa,Frett, Brendan,Zhang, Lingtian,Lakkaniga, Naga Rajiv,Briggs, David C.,Chauhan, Rakhee,Brescia, Annalisa,Federico, Giorgia,Yan, Wei,Santoro, Massimo,Mcdonald, Neil Q.,Li, Hong-Yu,Carlomagno, Francesca
, p. 4506 - 4516 (2020)
RET receptor tyrosine kinase is a driver oncogene in human cancer. We recently identified the clinical drug candidate Pz-1, which targets RET and VEGFR2. A key in vivo metabolite of Pz-1 is its less active demethylated pyrazole analogue. Using bioisosteri
5-aminoisoxazole derivative and application thereof in preparation of multi-kinase inhibitor
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Paragraph 0073-0074, (2021/05/12)
The invention relates to a 5-aminoisoxazole derivative and an application thereof in preparation of a multi-kinase inhibitor, in particular to a 5-aminoisoxazole derivative shown in a formula I, and an isotope form, a stereoisomeric form, a tautomeric for
Fragment-Based Discovery of a Dual pan-RET/VEGFR2 Kinase Inhibitor Optimized for Single-Agent Polypharmacology
Frett, Brendan,Carlomagno, Francesca,Moccia, Maria Luisa,Brescia, Annalisa,Federico, Giorgia,Defalco, Valentina,Admire, Brittany,Chen, Zhongzhu,Qi, Wenqing,Santoro, Massimo,Li, Hong-Yu
supporting information, p. 8717 - 8721 (2015/11/27)
Oncogenic conversion of the RET (rearranged during transfection) tyrosine kinase is associated with several cancers. A fragment-based chemical screen led to the identification of a novel RET inhibitor, Pz-1. Modeling and kinetic analysis identified Pz-1 a
BENZIMIDAZOLE ANALOGUES AND RELATED METHODS
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Paragraph 0096; 0097, (2015/12/24)
The invention relates to compounds of the formula (VIII) wherein the moieties R1, R2, R3, R4, and R5 are as defined in the specification, and salts thereof, as well as their use, methods of use for th
PHENYLACETAMIDES SUITABLE AS PROTEIN KINASE INHIBITORS
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Page/Page column 69, (2008/06/13)
The invention relates to compounds of the formula (I) wherein the moieties R1 , R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof; as well as their use, methods of use for them and method of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.
