308823-88-3Relevant academic research and scientific papers
Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents
Yang, Shaoning,Lu, Dingqiang,Ouyang, Pingkai
supporting information, 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.
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARα/γ dual agonists
Kim, Eunkyung,Park, Chan Sun,Han, Taedong,Bae, Myung-Ho,Chong, Wonee,Lee, Choong Hyun,Shin, Young Ah,Ahn, Byung-Nak,Kim, Mi Kyung,Shin, Chang Yell,Son, Moon Ho,Kim, Jin Kwan,Moon, Ho Sang,Shim, Hyun Joo,Kim, Eun Jung,Kim, Soon Hoe,Lim, Joong In,Lee, Chun Ho
scheme or table, p. 4993 - 4996 (2009/05/26)
Aryl-tetrahydropyridine derivatives were prepared and their PPARα/γ dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARα/γ dual agonist with an EC50 of 1.73 and 0.64 μM in hPPARα and γ, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.
3-AMINOCYCLOPENTANECARBOXAMIDES AS MODULATORS OF CHEMOKINE RECEPTORS
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Page/Page column 32, (2008/06/13)
The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
Substituted piperidines and methods of use
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Page 42, (2010/02/05)
Selected substituted piperidine compounds are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
