1072448-08-8Relevant articles and documents
Pyrazole derivative for FGFR inhibitor and preparation method of pyrazole derivative
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Paragraph 0411-0415, (2021/03/06)
The invention provides a pyrazole derivative for an FGFR inhibitor and a preparation method of the pyrazole derivative. The invention specifically relates to an amide pyrazole compound serving as an FGFR irreversible inhibitor, and a preparation method and application thereof. The present invention provides a compound as shown in Formula I, or a pharmaceutically acceptable salt, or solvate, isotope substitute, prodrug, or metabolite thereof. The compound as shown in general formula I have FGFR inhibitory activity, and is capable of preventing or treating disorders associated with FGFR activityor expression, preferably such as cancer.
Identification and preliminary structure-activity relationship studies of 1,5-dihydrobenzo[e][1,4]oxazepin-2(3h)-ones that induce differentiation of acute myeloid leukemia cells in vitro
Bataille, Carole J. R.,Cogswell, Thomas J.,Davies, Stephen G.,Georgiou, Irene,Jackson, Thomas R.,Jay-Smith, Morgan,Josa-Culleré, Laia,Milne, Thomas A.,Russell, Angela J.,Vyas, Paresh,Wynne, Graham M.
, (2021/11/11)
Acute myeloid leukemia (AML) is the most aggressive type of blood cancer, and there is a continued need for new treatments that are well tolerated and improve long-term survival rates in patients. Induction of differentiation has emerged as a promising alternative to conventional cy-totoxic chemotherapy, but known agents lack efficacy in genetically distinct patient populations. Previously, we established a phenotypic screen to identify small molecules that could stimulate differentiation in a range of AML cell lines. Utilising this strategy, a 1,5-dihydrobenzo[e][1,4]oxazepin-2(3H)-one hit compound was identified. Herein, we report the hit validation in vitro, structure-ac-tivity relationship (SAR) studies and the pharmacokinetic profiles for selected compounds.
SUBSTITUTED PYRIDINES AND METHOD OF USE
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, (2016/12/22)
The invention discloses compounds of Formula (I) wherein X, R1, R2, and R3 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.