4151-60-4Relevant academic research and scientific papers
Pharmaceutical composition containing amide compound and application of pharmaceutical composition
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Paragraph 0155-0159, (2020/02/14)
The invention provides a pharmaceutical composition containing an amide compound and an application of the pharmaceutical composition. The pharmaceutical composition comprises an effective component Aand an effective component B; the effective component A
Amide type compound as well as preparation method and application thereof
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Paragraph 0155; 0157; 0158; 0159, (2018/10/11)
The invention provides an amide type compound as well as a preparation method and application thereof. The amide type compound provided by the invention has a structure shown as a formula I, has a remarkable effect on prevention and control of agricultura
2,5-DIALKYL-4-H/HALO/ETHER-PHENOL COMPOUNDS
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Paragraph 0148, (2016/12/22)
The present disclosure provides phenolic compounds useful in the treatment of neurological conditions such as convulsions and tremors, having the structure of Formula (I): wherein R2, R4, R5, and R6, are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating neurological conditions.
2,5-DIALKYL-4-H/HALO/ETHER-PHENOL COMPOUNDS
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Paragraph 0186, (2015/06/03)
The present disclosure provides phenolic compounds useful in the treatment of neurological conditions such as convulsions and tremors, having the structure of Formula (I): wherein R2, R4, and R5, are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating neurological conditions.
Highly active chiral ruthenium catalysts for asymmetric ring-closing olefin metathesis
Funk, Timothy W.,Berlin, Jacob M.,Grubbs, Robert H.
, p. 1840 - 1846 (2007/10/03)
The synthesis of olefin metathesis catalysts containing chiral, monodentate N-heterocyclic carbenes and their application to asymmetric ring-closing metathesis (ARCM) are reported. These catalysts retain the high levels of reactivity found in the related
4-hydroxy-5,6-dihydropyrones. 2. Potent non-peptide inhibitors of HIV protease
D.tait, Bradley
, p. 3781 - 3792 (2007/10/03)
The 4-hydroxy-5,6-dihydropyrone template was utilized as a flexible scaffolding from which to build potent active site inhibitors of HIV protease. Dihydropyrone 1c (5,6-dihydro-4-hydroxy-6-phenyl-3-[(2- phenylethyl)thio]-2H-pyran-2-one) was modeled in the active site of HIV protease utilizing a similar binding mode found for the previously reported 4-hydroxybenzopyran-2-ones. Our model led us to pursue the synthesis of 6,6- disubstituted dihydropyrones with the aim of filling S1 and S2 and thereby increasing the potency of the parent dihydropyrone 1c which did not fill S2. Toward this end we attached various hydrophobic and hydrophilic side chains at the 6-position of the dihydropyrone to mimic the natural and unnatural amino acids known to be effective substrates at P2 and P2'. Parent dihydropyrone 1c (IC50 = 2100 nM) was elaborated into compounds with greater than a 100-fold increase in potency [18c, IC50 = 5 nM, 5-(3,6- dihydro-4-hydroxy-6-oxo-2-phenyl-5-[2-phenylethyl)thio]-2H-pyran-2- yl)pentanoic acid and 12c, IC50 = 51 nM, 5,6-dihydro-4-hydroxy-6-phenyl-6- (2-phenylethyl)-3-[(2-phenyl-ethyl)thio]-2H-pyran-2-one]. Optimization of the 3-position fragment to fill S1' and S2' afforded potent HIV protease inhibitor 49 [IC50 = 10 nM, 3-[(2-tert-butyl-5-methylphenyl)sulfanyl]-5,6- dihydro-4-hydroxy-6-phenyl-6-(2-phenylethyl)-2H-pyran-2-one]. The resulting low molecular weight compounds (475) have one or no chiral centers and are readily synthesized.
