873852-15-4Relevant articles and documents
The discovery of potent small molecule activators of human STING
Pryde, David C.,Middya, Sandip,Banerjee, Monali,Shrivastava, Ritesh,Basu, Sourav,Ghosh, Rajib,Yadav, Dharmendra B.,Surya, Arjun
supporting information, (2020/10/09)
The adaptor protein STING plays a major role in innate immune sensing of cytosolic nucleic acids, by triggering a robust interferon response. Despite the importance of this protein as a potential therapeutic target for serious unmet medical conditions inc
Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors
Qin, Xuemei,Lv, Yongjuan,Liu, Peng,Li, Zhipeng,Hu, Liming,Zeng, Chengchu,Yang, Leifu
, p. 1571 - 1575 (2016/07/27)
A series of novel morpholin-3-one-fused quinazoline derivatives were designed, synthesized and evaluated as EGFR tyrosine kinase inhibitors. Nineteen compounds showed significant inhibitory activities against EGFRwtkinase (IC50?wt(IC50?=?53.1?nM). Compound a7 and a8 showed excellent inhibitory activities against mutant EGFRT790M/L858Rand strong antiproliferative activity against H358 and A549 cell lines. Finally, molecular docking studies were performed to predict the possible binding mode of the target compounds. It is believed that this work would be very useful for designing a new series of tyrosine kinase inhibitors targeting EGFR.
3-Aminobenzamide compounds and inhibitors of vanilloid receptor subtype 1 (VR1) activity
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Page/Page column 25, (2010/10/19)
The present invention relates to a novel 3-aminobenzamide compound represented by the following formula which effectively inhibits vanilloid receptor subtype 1 (VR1) activity (wherein, for example, R1 is a C1-6 alkyl group which may be substituted, R2 is a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group which may be substituted, R3 is a hydrogen atom or a C1-6 alkyl group, R4 is a C1-6 alkyl group, a C1-6 alkoxy group, or a halo C1-6 alkyl group, m is an integer of 1 to 5 and P is a carbon or hetero ring) or a pharmaceutically acceptable salt thereof. The pharmaceutical composition comprising as active ingredients the 3-aminobenzamide compound or a pharmaceutically acceptable salt thereof is useful for treating diseases involved in VR1 activity such as pain, acute pain, chronic pain, neuropathic pain, rheumatoid arthritis pain, and neuralgia.