618-86-0Relevant academic research and scientific papers
QUINUCLIDINES FOR MODULATING ALPHA 7 ACTIVITY
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Paragraph 0370; 0371, (2016/02/29)
Provided are substituted quinuclidine compounds, pharmaceutical compositions comprising such compounds, and methods of modulating α7 nicotinic acetylcholine receptors and treating neurological disorders using such compounds.
Novel Anthranilic Diamide Scaffolds Containing N-Substituted Phenylpyrazole as Potential Ryanodine Receptor Activators
Liu, Jing-Bo,Li, Yu-Xin,Zhang, Xiu-Lan,Hua, Xue-Wen,Wu, Chang-Chun,Wei, Wei,Wan, Ying-Ying,Cheng, Dan-Dan,Xiong, Li-Xia,Yang, Na,Song, Hai-Bin,Li, Zheng-Ming
, p. 3697 - 3704 (2016/06/01)
To discover potent insecticides targeting ryanodine receptors (RyRs), a series of novel anthranilic diamides analogues (12a-12u) containing N-substituted phenylpyrazole were designed and synthesized. These compounds were characterized by 1H NMR, 13C NMR, and HRMS, and the structure of compound 12u was confirmed by X-ray diffraction. Their insecticidal activities indicated that these compounds displayed moderate to excellent activities. In particular, 12i showed 100 and 37% larvicidal activities against oriental armyworm (Mythimna separata) at 0.25 and 0.05 mg L-1, equivalent to that of chlorantraniliprole (100%, 0.25 mg L-1; and 33%, 0.05 mg L-1). The activity of 12i against diamondback moth (Plutella xylostella) was 95% at 0.05 mg L-1, whereas the control was 100% at 0.05 mg L-1. The calcium-imaging technique experiment results showed that the effects of 12i on the intracellular calcium ion concentration ([Ca2+]i) in neurons were concentration-dependent. After the central neurons of Helicoverpa armigera were dyed by loading with fluo-5N and treated with 12i, the free calcium released in endoplasmic reticulum indicated the target of compound 12i is RyRs or IP3Rs. The activation of RyRs by natural ryanodine completely blocked the calcium release induced by 12i, which indicated that RyRs in the central neurons of H. armigera third-instar larvae is the possible target of compound 12i.
SUBSTITUTED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
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Paragraph 00069, (2015/03/13)
The present disclosure relates to pyrimidine compounds of formula (I), their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to process of preparation of these pyrimidine compounds, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders mediated by epidermal growth factor receptor (EGFR) family kinases.
PROTEIN KINASE C INHIBITORS AND USES THEREOF
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Page/Page column 64, (2011/06/23)
This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Trichloroisocyanuric acid in 98% sulfuric acid: A superelectrophilic medium for chlorination of deactivated arenes
Mendo?a, Gabriela Fonseca,Senra, M?nica Rufino,Esteves, Pierre M.,De Mattos, Marcio C.S.
experimental part, p. 176 - 181 (2012/04/04)
Trichloroisocyanuric acid (TCCA) reacts with arenes and its reactivity is highly affected by the acid strength of the reaction medium. Deactivated arenes are efficiently chlorinated by TCCA in H2SO4. Our results, along with DFT calculations and 13C NMR spectrometry suggest the formation of a monoprotonated TCCA superelectrophile as the reactive species that can efficiently transfer electrophilic Cl+ to even very weak nucleophiles, such as m-dinitrobenzene.
NEW SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS
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Page/Page column 109-110, (2008/12/07)
The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1 ), and their use as pharmaceutical compositions.
Efficient one-pot transformation of aminoarenes to haloarenes using halodimethylisulfonium halides generated in situ
Baik, Woonphil,Luan, Wanqiang,Lee, Hyun Joo,Yoon, Cheol Hun,Koo, Sangho,Kim, Byeong Hyo
, p. 213 - 219 (2007/10/03)
Halodimethylsulfonium halide 1, which is readily formed in situ from hydrohaloic acid and DMSO, is a good nucleophilic halide. This activated nucleophilic halide rapidly converts aryldiazonium salt prepared in situ by the same hydrohaloic acid and nitrite ion to aryl chlorides, bromides, or iodides in good yield. The combined action of nitrite ion and hydrohaloic acid in DMSO is required for the direct transformation of aromatic amines, which results in the production of aryl halides within 1 h. Substituted compounds with electron-donating or -withdrawing groups or sterically hindered aromatic amines are also smoothly transformed to the corresponding aromatic halides. The only observed by-product is the deaminated arene (usually 7%). The isolated aryldiazonium salts can also be converted to the corresponding aryl halides using 1. The present method offers a facile, one-step procedure for transforming aminoarenes to haloarenes and lacks the environmental pollutants that usually accompany the Sandmeyer reaction using copper halides.
Small molecules useful in the treatment of inflammatory disease
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Page column 28, (2010/02/05)
Novel compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 5-(R)-(4-bromobenzyl)-3-(3-chloro-5-nitrophenyl)-5-methylimidazoline-2,4-dione; and, 5-(R)-(4-bromobenzyl
Electrophilic Aromatic Substitution. Part 35. Chlorination of 1,3-Dinitrobenzene, 1-Chloro-2,4-dinitrobenzene, and 2,4-Dinitrotoluene with Nitric Acid and Hydrogen Chloride or Chlorine in Sulphuric Acid or Oleum
Melhuish, Martin W.,Moodie, Roy B.
, p. 667 - 674 (2007/10/02)
Solutions of sulphuric acid or oleum containing HCl or Cl2 and nitric acid have been found both to chlorinate and nitrate deactivated aromatic compounds.The kinetics and products of the chlorination of 1,3-dinitrobenzene and 1-chloro-2,4-dinitrobenzene in sulphuric acid or oleum containing HCl and nitric acid at 130 deg C, and the kinetics and products of the chlorination of 2,4-dinitrotoluene at 90 deg C in sulphuric acid or oleum containing Cl2 and nitric acid, are reported. 1,3-Dinitrobenzene and 1-chloro-2,4-dinitrobenzene were predominantly chlorinated. 2,4-Dinitrotoluene gave approximately equal amounts of 6-chloro-2,4-dinitrotoluene and 2,4,6-trinitrotoluene.The results show that under these conditions, chlorination and nitration are competing electrophilic reactions, and that chlorination is less selective than nitration.Possible mechanisms for chlorination are discussed.
