35273-90-6Relevant academic research and scientific papers
Halogenated imidazole compound as well as preparation method and application thereof
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Paragraph 0025-0031, (2020/01/25)
The invention discloses alogenated imidazole compounds as well as a preparation method and application thereof. The structure of the halogenated imidazole compounds is disclosed in the invention, wherein, C * in the formula is R-type chiral carbon, and R1 and R2 can be independently selected from H and C1-6 alkyl; R3 is a substituted or unsubstituted C1-18 saturated or unsaturated aliphatic hydrocarbon, the aliphatic hydrocarbon comprises linear, branched or cyclic aliphatic hydrocarbon groups; X is H or a halogen atom; Y is H or a halogen atom; and X and Y cannot be H at the same time. The compounds or pharmaceutically acceptable salts or solvates thereof almost have no corticoid inhibition effect, can generate a rapid reversible anesthetic effect, can be rapidly metabolized into inactivecarboxylic acid metabolites, and have good revival quality after drug withdrawal; the corticoid function of the body can be rapidly recovered after single administration or continuous administration,the occurrence rate of muscular tremor after administration is low, and the body is rapidly awakened after drug withdrawal. The compounds or the salt compounds thereof can be used for preparing central inhibitory drugs which have sedative-hypnotic and/or anesthetic effects on humans or animals.
Antiviral novel nucleoside reverse transcriptase inhibitors
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Paragraph 0253; 0254; 0256; 0257; 0258, (2019/02/25)
The invention relates to compounds of antiviral novel nucleoside reverse transcriptase inhibitors, pharmaceutical compositions containing the compounds, and preparation and use of the compounds, and particularly discloses fused pyrimidine compounds shown in formula (I) and the pharmaceutical compositions containing the compounds, pharmaceutically acceptable salts, stereoisomers, solvates, hydrates, crystal forms, prodrugs or isotope derivatives. The compounds can be used for treating and/or preventing viral infectious diseases, such as human immunodeficiency virus (HIV) and hepatitis B virus (HBV). The formula (I) is shown in the specification.
Overcoming steric effects in the coupling reaction of alkyloxycarbonyloxymethyl (AOCOM) halides with phenols: an efficient synthesis of AOCOM phenolic prodrugs
Thomas, Joshua D.,Sloan, Kenneth B.
, p. 109 - 112 (2007/10/03)
Steric hindrance is a key factor in the coupling reaction of AOCOM halides with phenols. Sterically unhindered alkoxy groups favor the formation of acylated phenol. Under phase-transfer conditions, alkylated phenol is favored regardless of steric hindrance.
BETA-LACTAMASE INHIBITOR PRODRUG
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Page 33-34, (2010/02/06)
Prodrugs of 6-?-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention, or a solvate thereof, an optional beta-lactam antibiotic and at least one pharmaceutically acceptable carrier. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a betalactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.
BETA-LACTAMASE INHIBITOR PRODRUG
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Page 32, (2010/02/09)
Prodrugs of 6-β-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, each X is methylene, and Y is 0, or wherein R is H, each X is 0 and Y is methylene, and solvates thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention, or a solvate thereof, an optional beta-lactam antibiotic and at least one pharmaceutically acceptable carrier. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in 20 a mammal by administering an effective amount of a beta-lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.
