Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists
作者:Amy B. Dounay、Nancy S. Barta、Brian M. Campbell、Corey Coleman、Elizabeth M. Collantes、Lynne Denny、Satavisha Dutta、David L. Gray、Dongfeng Hou、Rathna Iyer、Samarendra N. Maiti、Daniel F. Ortwine、Al Probert、Nancy C. Stratman、Rajendra Subedi、Tammy Whisman、Wenjian Xu、Kim Zoski
DOI:10.1016/j.bmcl.2009.12.023
日期:2010.2
Preclinical studies suggest that compounds with dual norepinephrine reuptake inhibitor (NRI) and 5-HT1A partial agonist properties may provide an important new therapeutic approach to ADHD, depression, and anxiety. Reported herein is the discovery of a novel chemical series with a favorable NRI and 5-HT1A partial agonist pharmacological pro. le as well as excellent selectivity for the norepinephrine transporter over the dopamine transporter. (C) 2009 Elsevier Ltd. All rights reserved.
Copper-catalyzed highly regioselective 2-aryloxylation of 2,x-dihalopyridines
2,x-Dihalopyridines reacted with phenols catalyzed by CuI/TMEDA in the presence of Cs2CO3 in DMSO at 110 degrees C under nitrogen atmosphere for 24 h to afford 2-aryloxypyridines in good to high yields except p-nitrophenol. To expand this methodology, a vanilloid receptor ligand used in treatments was prepared in good yield. This method has potential utility in the synthesis of pharmaceuticals, agrochemicals and even natural products. (C) 2012 Elsevier Ltd. All rights reserved.
[EN] COMPOUNDS AND COMPOSITIONS THAT INHIBIT PIKFYVE<br/>[FR] COMPOSÉS ET COMPOSITIONS QUI INHIBENT PIKFYVE
申请人:[en]KINETA, INC.
公开号:WO2023107557A1
公开(公告)日:2023-06-15
Pyrazolo[1,5-a]pyrimidines are disclosed. These compounds may be useful in the treatment of neurological disorder, including frontotemporal dementia, chronic traumatic encephalopathy, Alzheimer's disease, limbic-predominant age-related TDP-43 encephalopathy, or frontotemporal lobar degeneration. Further, the invention features a method of inhibiting toxicity in a cell related to a protein TDP-43 or C9orf72. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Base-regulated tunable synthesis of pyridobenzoxazepinones and pyridobenzoxazines
作者:Chaoren Shen、Xiao-Feng Wu
DOI:10.1039/c5cy00798d
日期:——
A base-regulated one-pot protocol for the tunable synthesis of pyridobenzoxazepinones and pyridobenzoxazines has been developed. Pyridobenzoxazepinones and pyridobenzoxazines were produced in good yields selectively.