68621-47-6Relevant academic research and scientific papers
Discovery of HN37 as a Potent and Chemically Stable Antiepileptic Drug Candidate
Zhang, Yang-Ming,Xu, Hai-Yan,Hu, Hai-Ning,Tian, Fu-Yun,Chen, Fei,Liu, Hua-Nan,Zhan, Li,Pi, Xiao-Ping,Liu, Jie,Gao, Zhao-Bing,Nan, Fa-Jun
, p. 5816 - 5837 (2021/06/01)
We previously reported that P-retigabine (P-RTG), a retigabine (RTG) analogue bearing a propargyl group at the nitrogen atom in the linker of RTG, displayed moderate anticonvulsant efficacy. Recently, our further efforts led to the discovery of HN37 (pynegabine), which demonstrated satisfactory chemical stability upon deleting the ortho liable -NH2 group and installing two adjacent methyl groups to the carbamate motif. HN37 exhibited enhanced activation potency toward neuronal Kv7 channels and high in vivo efficacy in a range of pre-clinical seizure models, including the maximal electroshock test and a 6 Hz model of pharmacoresistant limbic seizures. With its improved chemical stability, strong efficacy, and better safety margin, HN37 has progressed to clinical trial in China for epilepsy treatment.
NOVEL COMPOUND AS KCNQ POTASSIUM CHANNEL AGONIST, PREPARATION METHOD THEREFOR AND USE THEREOF
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Paragraph 0044-0045, (2014/09/17)
The present invention provides compounds having the structure represented by general formula I, pharmaceutically acceptable salts thereofagonist, preparation methods therefor and a use thereof in the preparation of a medcine for the treatment of nervous system diseases. The compounds or pharmaceutical compositions thereof can be used as the KCNQ potassium channel agonist for treating nervous system diseases. Compared to retigabine, a compound in the prior art, the compound of the present invention have the same or better therapeutic effect, are easier for synthesis and storage, and less prone to oxidate deterioration.
NOVEL COMPOUND AS KCNQ POTASSIUM CHANNEL AGONIST, PREPARATION METHOD THEREFOR AND USE THEREOF
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Paragraph 0076-0077, (2014/11/27)
The present invention provides compounds having the structure represented by general formula I, pharmaceutically acceptable salts thereofagonist, preparation methods therefor and a use thereof in the preparation of a medicine for the treatment of nervous system diseases. The compounds or pharmaceutical compositions thereof can be used as the KCNQ potassium channel agonist for treating nervous system diseases. Compared to retigabine, a compound in the prior art, the compound of the present invention have the same or better therapeutic effect, are easier for synthesis and storage, and less prone to oxidate deterioration.
IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS
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Page/Page column 90-91, (2010/04/28)
The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.
