864960-96-3Relevant academic research and scientific papers
Design, synthesis, and characterization of oxadiazolopyrazine analogs with application as anticancer agents
Chen, Wei-Chia,Chen, Chia-Ling,Chang, Tzu-Ting,Hsieh, Feng-Chun,Chen, Wei-Sheng,Li, Wen-Shan
, p. 375 - 387 (2021/12/23)
Here, we describe the synthesis and evaluation of a class of cell-permeable indeno-oxadiazolopyrazine analogs as the anticancer agents. A new and facile approach to the synthesis of substituted analogs of indeno-oxadiazolopyrazine is illustrated. We find that the designed indeno-oxadiazolopyrazines, 3, 4, 10, 11, 15, and 16, act as potent anticancer agents compared to camptothecin, topoisomerase I inhibitor. These observations suggest that the electron-donating group (methoxy) at the C-5, C-6, and C-8 positions or electron-withdrawing group (fluoro) at the C-6 and C-7 positions on the A ring of indeno-oxadiazolopyrazines is required for antiproliferative activities against MDA-MB-231, BT549, and MCF7 cell lines.
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate
Zhou, Yu,Fu, Yan,Yin, Wanchao,Li, Jian,Wang, Wei,Bai, Fang,Xu, Shengtao,Gong, Qi,Peng, Tao,Hong, Yu,Zhang, Dong,Zhang, Dan,Liu, Qiufeng,Xu, Yechun,Xu, H. Eric,Zhang, Haiyan,Jiang, Hualiang,Liu, Hong
, p. 1844 - 1855 (2021/03/01)
The acetylcholinesterase (AChE) inhibitors remain key therapeutic drugs for the treatment of Alzheimer's disease (AD). However, the low-safety window limits their maximum therapeutic benefits. Here, a novel kinetics-driven drug design strategy was employed to discover new-generation AChE inhibitors that possess a longer drug-target residence time and exhibit a larger safety window. After detailed investigations, compound 12 was identified as a highly potent, highly selective, orally bioavailable, and brain preferentially distributed AChE inhibitor. Moreover, it significantly ameliorated cognitive impairments in different mouse models with a lower effective dose than donepezil. The X-ray structure of the cocrystal complex provided a precise binding mode between 12 and AChE. Besides, the data from the phase I trials demonstrated that 12 had good safety, tolerance, and pharmacokinetic profiles at all preset doses in healthy volunteers, providing a solid basis for its further investigation in phase II trials for the treatment of AD.
SUBSTITUTED 2,2'-BIPYRIMIDINYL COMPOUNDS, ANALOGUES THEREOF, AND METHODS USING SAME
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, (2019/12/04)
The present invention includes substituted 2,2'-bipyrimidinyl compounds, analogues thereof, and compositions comprising the same, which can be used to treat and/or prevent hepatitis B virus (HBV) and/or hepatitis B virus (HBV)-hepatitis D virus (HDV) infection in a patient.
GPR120 RECEPTOR AGONISTS AND USES THEREOF
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, (2012/01/06)
GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
GPR120 RECEPTOR AGONISTS AND USES THEREOF
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, (2010/08/04)
GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
ARYL GPR120 RECEPTOR AGONISTS AND USES THEREOF
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Page/Page column 86, (2010/05/13)
Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
CYCLIC AMINE DERIVATIVE OR SALT THEREOF
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Page/Page column 22; 43, (2010/11/27)
Provided are compounds which are an NMDA antagonist having a broad safety margin and are useful as a treating agent or a preventing agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, pain, etc. Concretely prov
ISOQUINOLINE AMINOPYRAZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS FOR THE TREATMENT OF CANCER
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Page/Page column 78, (2008/06/13)
Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
Heterocyclic compound having oxime group
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, (2010/02/14)
The present invention provides a compound that has an excellent inhibitory activity on STAT6 activation and is effective against allergic diseases, and a medicinal composition thereof. According to the present invention, disclosed is the compound represented by the General Formula (I) [where R1 and R2 independently represent a C1-6 alkyl group and the like that may have a hydrogen atom or a substituent; R3 represents a C1-6 alkyl group and the like that may have a substituent; R4 and R5 independent represents a hydrogen atom or a C1-6 alkyl group and the like that may have a substituent; R6 represents a hydrogen atom and the like; W represents —SO2— and the like; and X represents a sulphur atom and the like.]or a salt thereof, or a hydrate thereof.
