911705-40-3Relevant academic research and scientific papers
Application of piperazine structure containing compound to preparation of LSD1 (Lysine Specific Demethylase 1) inhibitor
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Paragraph 0028, (2017/09/29)
The invention discloses application of a piperazine structure containing compound to the preparation of a histone lysine specific demethylase (LSD1) inhibitor. The structural general formula of the compound is as shown in the following descriptions (wherein, A is hydrogen, carbonyl or thiocarbonyl) or a configurational isomer and a pharmaceutical salt thereof, or is as shown in the following descriptions or a pharmaceutical salt thereof. The compound has an obvious inhibition effect on the LSD1, can be prepared into the LSD1 inhibitor, and is used for preventing and treating a disease related to the activity of the histone LSD1.
Discovery of novel 2-(3-phenylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3β inhibitors
Usui, Yoshihiro,Uehara, Fumiaki,Hiki, Shinsuke,Watanabe, Kazutoshi,Tanaka, Hiroshi,Shouda, Aya,Yokoshima, Satoshi,Aritomo, Keiichi,Adachi, Takashi,Fukunaga, Kenji,Sunada, Shinji,Nabeno, Mika,Saito, Ken-Ichi,Eguchi, Jun-ichi,Yamagami, Keiji,Asano, Shouichi,Tanaka, Shinji,Yuki, Satoshi,Yoshii, Narihiko,Fujimura, Masatake,Horikawa, Takashi
, p. 3726 - 3732 (2017/07/27)
We herein describe the results of further evolution of glycogen synthase kinase (GSK)-3β inhibitors from our promising compounds containing a 2-phenylmorpholine moiety. Transformation of the morpholine moiety into a piperazine moiety resulted in potent GSK-3β inhibitors. SAR studies focused on the phenyl moiety revealed that a 4-fluoro-2-methoxy group afforded potent inhibitory activity toward GSK-3β. Based on docking studies, new hydrogen bonding between the nitrogen atom of the piperazine moiety and the oxygen atom of the main chain of Gln185 has been indicated, which may contribute to increased activity compared with that of the corresponding phenylmorpholine analogues. Effect of the stereochemistry of the phenylpiperazine moiety is also discussed.
N - acyl - [...] P 2X7 adjustment
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Paragraph 0410-0412, (2017/10/28)
The present invention is directed to compounds of Formula (I), which includes enantiomer and diasteromers thereof: These compounds are suitable for use in the treatment of diseases associated with P2X7 receptor activity such as diseases of the autoimmune
Novel Phenyl-Substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 Antagonists with Robust Target Engagement in Rat Brain
Chrovian, Christa C.,Soyode-Johnson, Akinola,Ao, Hong,Bacani, Genesis M.,Carruthers, Nicholas I.,Lord, Brian,Nguyen, Leslie,Rech, Jason C.,Wang, Qi,Bhattacharya, Anindya,Letavic, Michael A.
, p. 490 - 497 (2016/05/19)
Novel 5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists were optimized to allow for good blood-brain barrier permeability and high P2X7 target engagement in the brain of rats. Compound 25 (huP2X7 IC50 = 9 nM; rat P2X7 IC50
NOVEL COMPOUNDS AS CALCIUM CHANNEL BLOCKERS
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Page/Page column 125, (2010/04/27)
The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, Ar2, L1, L2, n, R1, R4, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
