20839-81-0Relevant articles and documents
PRODRUG OF NITROXOLINE AND USE THEREOF
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Page/Page column 94-95, (2021/08/24)
The present invention relates to the prodrug of nitroxoline and use thereof. Specifically, the present invention relates to a compound of formula (I) or the pharmaceutically acceptable salt thereof, a preparation method thereof, a pharmaceutical composition comprising the same, as well as a use thereof in anti-infective and anti-tumor drugs. The compound of formula (I) has better pharmacokinetic parameters such as water solubility, blood concentration or half-life relative to nitroxoline. The compound of formula (I) can reduce the number of administrations, and has the possibility of being applied in other fields than the urinary tract field. The definition of each group in formula (I) is as defined in the description.
PYRAZOLOPYRIMIDINES AS INHIBITORS OF GLUCOCORTICOID RECEPTOR TRANSLOCATION
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Paragraph 00777, (2016/08/23)
Provided herein are compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of Glucocorticoid Receptor (GR) translocation. Furthermore, the subject compounds and compositions are useful for the treatment of diseases involved in the hypothalamic-pituitary-adrenal (HPA) axis.
Synthesis of 2-pyridones by cycloreversion of [2.2.2]- bicycloalkene diketopiperazines
Margrey, Kaila A.,Hazzard, Amy D.,Scheerer, Jonathan R.
supporting information, p. 904 - 907 (2014/03/21)
A general strategy for the conversion of [2.2.2]-diazabicyclic alkene structures to 2-pyridone aromatic heterocyclic products is reported. The reaction sequence starts from 2,5-diketopiperazine (DKP) derivatives, is compatible with both aromatic and aliphatic aldehyde components, and can intercept either intra- or intermolecular cycloaddition manifolds. Priming of one aza-bridging function in the intermediate [2.2.2]-DKP scaffold permits cycloreversion (microwave heating) and selective extrusion of cyanate derivatives leading to the formation of 2-pyridone structures. Progress toward the synthesis of louisianin A and B, antiproliferative 2-pyridone natural products, is also disclosed.