3183-22-0Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors
Yu, Jianjun,Xu, Lei,Hong, Duidui,Zhang, Xiaotuan,Liu, Jieyu,Li, Daqiang,Li, Jia,Zhou, Yubo,Liu, Tao
, p. 543 - 558 (2018/11/10)
A series of novel phenol ether derivatives were designed, synthesized, and evaluated as non-covalent proteasome inhibitors. Most compounds exhibited moderate to excellent proteasome inhibitory activity. In particular, compound 18x proved to be the most po
BENZOPYRAZOLE COMPOUNDS AND ANALOGUES THEREOF
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Page/Page column 107, (2017/12/27)
Disclosed are compounds of formula (I), and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula (I), and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity.
HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE COMPRISING SAME
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Paragraph 0370; 0371, (2016/12/01)
The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
Ammonolysis of morpholine-2,5-diones: Participation of the primary amide group. Part 2
Arcelli, Antonio,Bongini, Alessandro,Porzi, Gianni,Rinaldi, Samuele
experimental part, p. 132 - 141 (2012/05/04)
The ammonolysis of three morpholine-2,5-dione derivatives was investigated and the mechanism ascertained by kinetic studies and theoretical calculations. The kinetics, followed by high-performance liquid chromatography analysis, evidenced the presence of two intermediates, which were isolated and characterized. The ammonolysis occurs with a complex mechanism involving two consecutive reactions followed by two parallel ones. The second step of the whole reaction involves an anchimeric assistance of the primary amide group. The pseudo-first-order rate constants were calculated by appropriate equations, which describe the single steps of the process. Computational density functional theory investigations of vicinal primary amide group participation were performed using a model compound, and the transition states were generated. The theoretical calculations evidenced the essential role exerted by ammonia, which acts as a proton transfer.
Equimolar CO2 capture by N-substituted amino acid salts and subsequent conversion
Liu, An-Hua,Ma, Ran,Song, Chan,Yang, Zhen-Zhen,Yu, Ao,Cai, Yu,He, Liang-Nian,Zhao, Ya-Nan,Yu, Bing,Song, Qing-Wen
supporting information, p. 11306 - 11310 (2013/01/15)
Steric bulk controls CO2 absorption: N-substituted amino acid salts in poly(ethylene glycol) reversibly absorb CO2 in nearly 1:1 stoichiometry. Carbamic acid is thought to be the absorbed form of CO 2; this was supported by NMR and in situ IR spectroscopy, and DFT calculations. The captured CO2 could be converted directly into oxazolidinones and thus CO2 desorption could be sidestepped. Copyright
Synthesis, characterization and biological activities of novel (E)-3-(1-(alkyloxyamino)ethylidene)-1-alkylpyrrolidine-2,4-dione derivatives
Zhu, Zhao-Yong,Shi, Qing-Ming,Han, Bao-Feng,Wang, Xian-Feng,Qiang, Sheng,Yang, Chun-Long
experimental part, p. 2467 - 2472 (2010/12/18)
Twenty novel tetramic acid derivatives (E)-3-(1-(alkyloxyamino)ethylidene)- 1-alkylpyrrolidine-2,4-diones were synthesized by the reaction of 3-(1-hydroxyethylidene)pyrrolidine-2,4-diones with O-alkyl hydroxylamines. The title compounds were confirmed by
Poly (ADP-Ribose) Polymerase (PARP) Inhibitors
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Page/Page column 84, (2010/08/07)
Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS
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Page/Page column 82; 83, (2009/09/04)
Chemical entities that modulate PD kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.
Development of a practical synthesis of novel, pyrrole-based HMG-CoA reductase inhibitors
Pfefferkorn, Jeffrey A.,Bowles, Daniel M.,Kissel, William,Boyles, David C.,Choi, Chulho,Larsen, Scott D.,Song, Yuntao,Sun, Kuai-Lin,Miller, Steven R.,Trivedi, Bharat K.
, p. 8124 - 8134 (2008/02/08)
This paper describes the development of an efficient and scalable second generation synthesis of novel, pyrrole-based HMG-CoA reductase inhibitors. Compound 1 was identified as part of a discovery program aimed at finding improved treatments for hypercholesterolemia. Herein, we describe an efficient synthesis of its highly functionalized pyrrole core followed by attachment of the 3,5-dihydroxyhexanoic acid side chain via ylide olefination chemistry.
Microwave-assisted solvent-free intramolecular 1,3-dipolar cycloaddition reactions leading to hexahydrochromeno[4,3-b]pyrroles: scope and limitations
Pospí?il, Ji?í,Potá?ek, Milan
, p. 337 - 346 (2007/10/03)
We report the microwave-assisted solvent-free synthesis of hexahydrochromeno[4,3-b]pyrroles. Intramolecular 1,3-dipolar cycloadditions proceed under these conditions within 15-40 min in 16-84% yields. An influence of the microwave irradiation upon various [3+2] cycloaddition reaction intermediates was studied. Additionally, a scope and limitations of these reactions including an influence of the dipolarophile geometry upon the cycloaddition selectivity and steric demands of the dipole upon its reactivity were also disclosed. These observations led us to postulate a preferable transition state of the reaction. Finally, an influence of the microwave irradiation to the isomerization of activated olefins was also described.
