957121-38-9Relevant academic research and scientific papers
Difluorophenylglycinols as New Modulators of Proteolytic Processing of Amyloid Precursor Proteins
Chen, Chia-Yu,Liao, Yung-Feng,Chang, Ming-Yun,Hu, Ming-Kuan
, p. 161 - 173 (2014/03/21)
Synthesis and evaluation of difluorophenylglycinols as new modulators of proteolytic processing of the amyloid-β precursor proteins for Alzheimer's therapies were described. A range of N-substituted (R)- and (S)- difluorophenylglycinols, structured on the amino alcohol framework, were explored by incorporating the arylsulfonyl moieties and various N-substituents. Evans' chiral auxiliary strategy was employed for the asymmetric synthesis of these enantiomeric difluorophenylglycinols. Compounds with effects on the γ-secretase inhibition and ERK-mediated signaling pathways were evaluated on cell-based assays. Among them, N-cyclopropylmethyl derivatives R-12c and R-13c showed modest γ-secretase inhibition as well as ERK-dependent activation. A range of N-substituted (R)- and (S)-difluorophenylglycinols, structured on the amino alcohol framework, were explored by incorporating the arylsulfonyl moieties and various N-substituents. Compounds with effects on γ-secretase inhibition and ERK-mediated signaling pathways were evaluated on cell-based assays. The N-cyclopropylmethyl derivatives R-12c and R-13c showed modest γ-secretase inhibition and ERK-dependent activation.
Substituted monocyclic CGRP receptor antagonists
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Page/Page column 40, (2008/06/13)
Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
