74290-66-7Relevant articles and documents
Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors
Barlaam, Bernard,Cosulich, Sabina,Fitzek, Martina,Germain, Hervé,Green, Stephen,Hanson, Lyndsey L.,Harris, Craig S.,Hancox, Urs,Hudson, Kevin,Lambert-van der Brempt, Christine,Lamorlette, Maryannick,Magnien, Fran?oise,Ouvry, Gilles,Page, Ken,Ruston, Linette,Ward, Lara,Delouvrié, Bénédicte
, p. 3030 - 3035 (2017)
We report the discovery of a novel aminopyrazine series of PI3Kα inhibitors, designed by hybridizing two known scaffolds of PI3K inhibitors. We describe the progress achieved from the first compounds plagued with poor general kinase selectivity to compounds showing high selectivity for PI3Kα over PI3Kβ and excellent general kinase selectivity. This effort culminated with the identification of compound 5 displaying high potency and selectivity, and suitable physiochemical and pharmacokinetic properties for oral administration. In vivo, compound 5 showed good inhibition of tumour growth (86% tumour growth inhibition at 50?mg/kg twice daily orally) in the MCF7 xenograft model in mice.
Compounds used as JAK inhibitor, and use of compounds
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Paragraph 0357; 0358; 0359; 0340, (2017/08/27)
The invention provides compounds used as a JAK inhibitor, and a use of the compounds, and concretely provides compounds (represented by formula (I)) with JAK inhibition activity or a stereoisomer, a geometric isomer, a tautomer, a racemate, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a medicinal composition including the compounds. The invention also discloses a use of the compounds or the medicinal composition thereof in the preparation of medicines used for treating autoimmune diseases or proliferative diseases.
TREATMENT OF CHRONIC GRAFT VERSUS HOST DISEASE WITH SYK INHIBITORS
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Page/Page column 33, (2016/11/17)
The present disclosure provides methods of utilizing Syk inhibiting compounds in the treatment for graft versus host disease (GVHD) in a human, including acute graft versus host disease (aGVHD) and chronic graft versus host disease (cGVHD), including the use of compounds selected from the group consisting of the formulas below: (I) and (II).