20839-81-0Relevant articles and documents
PRODRUG OF NITROXOLINE AND USE THEREOF
-
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.
NITROXOLINE PRODRUG AND USE THEREOF
-
Paragraph 0214; 0439-0441, (2021/11/26)
Provided are a nitroxoline prodrug and a use thereof. Specifically, provided are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, a composition containing the compound, and a use thereof in the preparation of anti-infective and antitumor drugs, and definitions of groups in formula (I) are as stated in the specification. The compound represented by formula (I) has better pharmacokinetic parameters such as solubility, blood medicine concentration, or half-life period than nitroxoline. The compound represented by formula (I) can reduce the frequency of drug administration, and has potential for application in other fields other than the field of urinary tracts.
PYRAZOLOPYRIMIDINES AS INHIBITORS OF GLUCOCORTICOID RECEPTOR TRANSLOCATION
-
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 the novel tetrahydropyrazolo[3,4- c ]pyridin-5-one scaffold
Howe, Nicholas J.,Blades, Kevin,Lamont, Gillian M.
supporting information, p. 228 - 232 (2015/03/03)
We report an efficient synthesis of the novel 1,4,6,7-tetra-hydropyrazolo[3,4-c]pyridin-5-one scaffold with the potential for incorporation of alkyl or aryl substituents at the C-3 and N-6 positions. The route utilises a Dieckmann condensation to install the lactam ring, followed by a hydrazine cyclisation to build the fused pyrazole ring.
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.
SYNTHESIS OF [2.2.2]-DIAZABICYCLIC RING SYSTEMS
-
Paragraph 0129-0130, (2013/11/19)
Herein we describe compositions and methods for the synthesis of [2.2.2]-diazabicyclic structures comprising a domino reaction sequence involving aldol condensation, alkene isomerization, and intramolecular hetero-Diels-Alder cycloaddition. Excellent diastereofacial control during the cycloaddition is enforced with a removable chiral phenyl aminal diketopiperazine substituent. The reaction sequence rapidly generates molecular complexity and is competent with both enolizable and non-enolizable aldehyde substrates. This method provides an efficient route to [2.2.2]-diazabicyclic structures, common to bioactive prenylated indole alkaloids such as the brevianamides and stephacidins.
Expanding the synthetic method and structural diversity potential for the intramolecular Aza Diels-Alder cyclization
Muhuhi, Joseck,Spaller, Mark R.
, p. 5515 - 5526 (2007/10/03)
New experimental facets have been examined to expand upon the known methods for an aromatic variant of the intramolecular Aza Diels-Alder cyclization. The specific transformation under study is one that uses functionalized anilines and an aldehyde-olefin tether to provide tetrahydroquinoline cycloadducts under mild acidic conditions. Variations investigated encompass the use of N-alkylated anilines, including one with ring-constrained nitrogen, in the context of glycine, phenylalanine, and glyoxyl ester bridging elements; bridge components with structural perturbations; modified dienophile segments; and different acid catalysts. Substituted tetrahydroquinolines obtained from many of the preceding experiments were obtained in good chemical yield, generally in excess of 80%. Designed as a platform for combinatorial chemical synthesis, this reaction manifold accommodates a range of starting materials with structurally and electronically distinct characteristics. The results of this report, in combination with the discoveries from previous work in this area, enhance the ability of the intramolecular Aza Diels-Alder transformation to generate a diverse array of quinolinic structures with multiple stereogenic centers, many of which resemble lignan and arylnaphthalene-type natural products.
STEREOSPECIFIC SYNTHESIS OF CHIRAL PRECURSORS OF THIENAMYCIN FROM L-THREONINE
Shiozaki, Masao,Ishida, Noboru,Hiraoka, Tetsuo,Maruyama, Hiroshi
, p. 1795 - 1802 (2007/10/02)
L-Threonine was transformed, stereospecifically, to a versatile β-lactam (5a) in 3 steps.This β-lactam was further converted to a key intermediate (25) for the synthesis of thienamycin and its biologically active analogues.Furthermore, the compound 5a was changed to iodides (18 and 23), cyanides (19 and 24), chloromethylketone (26) and aldehydes (30 and 31) which appear to have a latent potential as precursors for the syntheses of the carbapenems.
