1086398-00-6Relevant articles and documents
COMPOUNDS AND USES THEREOF
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Paragraph 1315; 1324, (2019/11/11)
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents
Yang, Shaoning,Lu, Dingqiang,Ouyang, Pingkai
, p. 1731 - 1735 (2018/05/04)
Epilepsy is a kind of disease with complicated pathogenesis. KCNQ (Kv7) is a voltage dependent potassium channel that is mostly associated with epilepsy and thus becomes an important target in the treatment of epilepsy. In this paper, a series of substituted piperidine derivatives targeting KCNQ were designed and synthesized by using scaffold hopping and active substructure hybridization. Compounds were evaluated by fluorescence-based thallium influx assay, Rb+ flow assay and electrophysiological patch-clamp assay. Results showed that some compounds possessed more potent potassium channel opening activity than Retigabine. More significantly, compound 11 was found to have good pharmacokinetic profiles in vivo.
Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists
Pasternak, Alexander,Goble, Stephen D.,Vicario, Pasquale P.,Di Salvo, Jerry,Ayala, Julia M.,Struthers, Mary,DeMartino, Julie A.,Mills, Sander G.,Yang, Lihu
, p. 994 - 998 (2008/09/19)
This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had i