13552-47-1Relevant academic research and scientific papers
Metal-free synthesis of β-aminoketones by the reductive hydroamination of ynones
Fu, Rui,Liu, Yu,Wu, Tao,Zhang, Xinyu,Zhu, Yang,Luo, Jiangbin,Zhang, Zhengyu,Jiang, Yaojia
, p. 3525 - 3528 (2022/03/31)
This study describes a cascade method for the synthesis of β-aminoketones through the reductive hydroamination of alkynes under very mild metal-free conditions. It allows for the rapid conversion of ynones and amines into corresponding β-aminoketones with a broad substrate scope and diverse functionalities. This straightforward and easy-to-handle reaction process can be successfully applied for the synthesis of Proroxan and Propipocaine, offering a potential option for the synthesis of drug molecules with the β-aminoketone skeleton.
Synthesis and pharmacological investigation of aralkyl diamine derivatives as potential triple reuptake inhibitors
Zheng, Yong-Yong,Weng, Zhi-Jie,Xie, Peng,Zhu, Mei-Yu,Xing, Long-Xuan,Li, Jian-Qi
, p. 219 - 234 (2014/09/17)
A series of aralkyl diamine derivatives were designed, synthesized, and evaluated for their triple reuptake inhibitory abilities. Compounds 18c (5-HT, NE, DA, IC50 = 389, 69, 238 nM), 36a (5-HT, NE, DA, IC50 = 378, 477, 247 nM), and
GAMMA-DIKETONES AS WNT/BETA -CATENIN SIGNALING PATHWAY ACTIVATORS
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Paragraph 1714; 1715; 1716; 1726, (2014/09/03)
The present disclosure provides γ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANT
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Paragraph 0030; 0055, (2013/03/28)
Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors
Gracias, Vijaya,Ji, Zhiqin,Akritopoulou-Zanze, Irini,Abad-Zapatero, Cele,Huth, Jeffrey R.,Song, Danying,Hajduk, Philip J.,Johnson, Eric F.,Glaser, Keith B.,Marcotte, Patrick A.,Pease, Lori,Soni, Nirupama B.,Stewart, Kent D.,Davidsen, Steven K.,Michaelides, Michael R.,Djuric, Stevan W.
, p. 2691 - 2695 (2008/12/21)
We report the discovery of the pyrimido-diazepine scaffolds as novel adenine mimics. Structure-based design led to the discovery of analogs with potent inhibitory activity against receptor tyrosine kinases, such as KDR, Flt3 and c-Kit. Compound 14 exhibited low nanomolar KDR enzymatic and cellular potencies (IC50 = 9 and 52 nM, respectively).
