128883-86-3Relevant articles and documents
Design and Synthesis of a Series of Novel Macrocycle Janus Kinase 2 Inhibitors
Wang, Yanling,Ge, Huan,Wang, Disha,He, Huan,Li, Lu,Diao, Yanyan,Shen, Zihao,Zhu, Lili,Li, Shiliang,Zhao, Zhenjiang,Li, Honglin
supporting information, p. 1259 - 1263 (2019/11/21)
Macrocycle has attracted the attention of many researchers in the field of medicinal chemistry due to its unique advantages and good prospects, but the difficulties in drug design and synthesis of macrocycle limit its applications. In this study, a series of macrocyclic derivatives designed from anaplastic lymphoma kinase (ALK) inhibitor lorlatinib were synthesized as Janus kinase 2 (JAK2) selective inhibitors. Among them, 17f had the best inhibitory activity (IC50 = 0.177 μmol·L–1) and selectivity for JAK2 over JAK1 and JAK3, which indicated that design of the macrocyclic derivatives might be a feasible strategy for the discovery of novel selective JAK2 inhibitors.
NOVEL COMPOUNDS
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Page/Page column 97; 100, (2019/04/27)
The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
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Paragraph 0389, (2017/02/24)
Compounds of Formula (I) or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein A, J, R1, R2, R3, R4, R5, R6, R7, R9, X, m and n are as described herein, compositions thereof, and methods and uses thereof.
