- GABAA Receptor allosteric enhancement compounds and their preparation and use
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A GABA A receptor allosteric enhancer compound and preparation and a use thereof are disclosed. The compound has a structure represented by formula (1). R 1 and R 2 are each independently selected from isopropyl and n-propyl; and when R 1 is n-propyl, R 2 is not isopropyl.
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Paragraph 0085-0086; 0090-0091
(2020/03/17)
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- DIPHENYL DERIVATIVE AND USES THEREOF
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The present invention relates to a biphenyl derivative and use thereof, and the biphenyl derivative has a structure represented by the formula (I) as defined in the specification. The use refers the use of the biphenyl derivative or a pharmaceutically acceptable salt or solvate thereof, or a pharmaceutical composition comprising the biphenyl derivative or a pharmaceutically acceptable salt or solvate thereof in the preparation of a medicament for the treatment and/or prevention of ischemic stroke.
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Paragraph 0105-0110
(2018/06/04)
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- Water-Accelerated Claisen Rearrangements
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Allyl aryl ethers undergo accelerated Claisen and [1,3] rearrangements in the presence of a mixture of trialkylalanes and water or aluminoxanes. The ratio of ortho-, meta-, and pora-Claisen products depends to a large extent on the presence of water and to a much lesser extent on the nature of the alane.
- Wipf, Peter,Rodriguez, Sonia
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p. 434 - 440
(2007/10/03)
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- Synthesis, Biological Evaluation, and Preliminary Structure-Activity Considerations of a Series of Alkylphenols as Intravenous Anesthetic Agents
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Following our discovery of the intravenous (iv) anesthetic activity of 2,6-diethylphenol in mice, a series of alkylphenols was examined in this species and the most active analogues were further evaluated in rabbits.The synthesis of compounds which were not commercially available was accomplished by adaptations of standard ortho-alkylation procedures for phenols.Structure-activity relationships were found to be complex, but, in general, potency and kinetics appeared to be a function of both the lipophilic character and the degree of steric hindrance exerted by ortho substituents.The most interesting compounds were found in the 2,6-dialkyl series, and the greatest potency was associated with 2,6-di-sec-alkyl substitution.In particular, 2,6-diisopropylphenol (ICI 35868) emerged as a candidate for further development and has subsequently been shown to be an effective iv anesthetic agent in man.
- James, Roger,Glen, John B.
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p. 1350 - 1357
(2007/10/02)
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