1239331-90-8Relevant academic research and scientific papers
Novel pyrrolidine or piperidine derivatives having activity for T-type calcium channel
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Paragraph 0299-0302; 0349-0352, (2020/04/23)
A pyrrolidine or piperidine compound having activity for T - type calcium channel, wherein the pyrrolidine or piperidine compound of Formula 1 according to the present invention has an excellent antagonistic activity to, T-type calcium channel, and can be used as a preventive or therapeutic agent, for pain diseases, or cancer related to cancer, or cancer such as, epilepsy and,hepatic pain, angina. (by machine translation)
Synthesis and biological evaluation of pyrrolidine-based T-type calcium channel inhibitors for the treatment of neuropathic pain
Yang, Hak Kyun,Son, Woo Seung,Lim, Keon Seung,Kim, Gun Hee,Lim, Eun Jeong,Gadhe, Changdev G.,Lee, Jae Yeol,Jeong, Kyu-Sung,Lim, Sang Min,Pae, Ae Nim
, p. 1460 - 1471 (2018/09/26)
The treatment of neuropathic pain is one of the urgent unmet medical needs and T-type calcium channels are promising therapeutic targets for neuropathic pain. Several potent T-type channel inhibitors showed promising in vivo efficacy in neuropathic pain a
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR)
Takeuchi, Craig S.,Kim, Byung Gyu,Blazey, Charles M.,Ma, Sunghoon,Johnson, Henry W. B.,Anand, Neel K.,Arcalas, Arlyn,Baik, Tae Gon,Buhr, Chris A.,Cannoy, Jonah,Epshteyn, Sergey,Joshi, Anagha,Lara, Katherine,Lee, Matthew S.,Wang, Longcheng,Leahy, James W.,Nuss, John M.,Aay, Naing,Aoyama, Ron,Foster, Paul,Lee, Jae,Lehoux, Isabelle,Munagala, Narsimha,Plonowski, Arthur,Rajan, Sharmila,Woolfrey, John,Yamaguchi, Kyoko,Lamb, Peter,Miller, Nicole
, p. 2218 - 2234 (2013/05/22)
A series of novel, highly potent, selective, and ATP-competitive mammalian target of rapamycin (mTOR) inhibitors based on a benzoxazepine scaffold have been identified. Lead optimization resulted in the discovery of inhibitors with low nanomolar activity and greater than 1000-fold selectivity over the closely related PI3K kinases. Compound 28 (XL388) inhibited cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates. Furthermore, this compound displayed good pharmacokinetics and oral exposure in multiple species with moderate bioavailability. Oral administration of compound 28 to athymic nude mice implanted with human tumor xenografts afforded significant and dose-dependent antitumor activity.
