197385-06-1Relevant academic research and scientific papers
The discovery and optimization of benzimidazoles as selective NaV1.8 blockers for the treatment of pain
Brown, Alan D.,Bagal, Sharan K.,Blackwell, Paul,Blakemore, David C.,Brown, Bruce,Bungay, Peter J.,Corless, Martin,Crawforth, James,Fengas, David,Fenwick, David R.,Gray, Victoria,Kemp, Mark,Klute, Wolfgang,Malet Sanz, Laia,Miller, Duncan,Murata, Yoshihisa,Payne, C. Elizabeth,Skerratt, Sarah,Stevens, Edward B.,Warmus, Joseph S.
supporting information, p. 230 - 239 (2018/12/11)
The voltage gated sodium channel NaV1.8 has been postulated to play a key role in the transmission of pain signals. Core hopping from our previously reported phenylimidazole leads has allowed the identification of a novel series of benzimidazole NaV1.8 blockers. Subsequent optimization allowed the identification of compound 9, PF-06305591, as a potent, highly selective blocker with an excellent preclinical in vitro ADME and safety profile.
BICYCLIC HETEROARYL DERIVATIVES AND PREPARATION AND USES THEREOF
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Page/Page column 94; 95, (2018/10/30)
Compounds of Formula (A), where the definition of the variables are as described in the description, as well as their preparation and uses, and pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate
PEST-CONTROL COMPOSITION AND PEST-CONTROL METHOD
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Paragraph 0681, (2015/12/19)
The present invention provides a composition for controlling pests having an excellent control efficacy on pests. A composition for controlling pests comprising a compound represented by the formula (1): wherein each of symbols are the same as defined in the Description, or N-oxide thereof; and a compound represented by the formula (2): wherein each of symbols are the same as defined in the Description; shows an excellent controlling efficacy on pests.
PEST-CONTROL COMPOSITION AND PEST-CONTROL METHOD
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Paragraph 0721, (2015/12/19)
The present invention provides a composition for controlling pests having an excellent control efficacy on pests. A composition for controlling pests comprising a compound represented by the formula (1): wherein each of symbols are the same as defined in the Description, or N-oxide thereof; and one or more compounds selected from the group consisting of a group of azole-type compound, a group of strobilurin-type compound, a group of phenylamido-type compound, a group of a compound for controlling rice blast, a group of a compound for controlling sheath blight of rice, and a group of fungicidal compound selected from fludioxonil, ethaboxam, tolclofos-methyl, and captan; shows an excellent controlling efficacy on pests.
PEST CONTROL COMPOSITION AND METHOD FOR CONTROLLING PEST
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Paragraph 1128, (2015/12/30)
A composition for controlling pests includes a compound represented by the formula (1) or N-oxide thereof: and 4-oxo-4-[(2-phenylethyl)amino]-butyric acid. A method for controlling pests has a step of applying to plants, plant seeds, bulbs, or soil where plants grow an effective amount of the composition for controlling pests. The composition for controlling pests and the method for controlling pests exhibit excellent controlling efficacy on pest.
PEST-CONTROL METHOD
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Paragraph 0676, (2015/12/19)
The present invention provides a method for controlling pests which comprises applying a compound of formula (1): wherein each of symbols are the same as defined in the Description, or N-oxide thereof to plant seeds, which has an excellent controlling efficacy on pests.
PEST-CONTROL COMPOSITION AND PEST-CONTROL METHOD
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Paragraph 0709, (2015/12/19)
The present invention provides a composition for controlling pests comprising a compound represented by the formula (1): wherein each of symbols are the same as defined in the Description, or N-oxide thereof; and at least one compound selected from the group consisting of neonicotinoid compound, synthetic pyrethroid compound, phenylpyrazole compound, macrolide compound, diamide compound, and insecticidal compound selected from the group consisting of pymetrozine, pyridalyl, pyriproxyfen, spirotetramat, sulfoxaflo and flupyradifurone, which has an excellent control efficacy on pests.
FUSED HETEROCYCLIC COMPOUND AND USE THEREOF FOR PEST CONTROL
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Paragraph 0345, (2013/03/26)
There is provided a compound having an excellent controlling effect on pests represented by the formula (1):
Direct amination of nitro(pentafluorosulfanyl)benzenes through vicarious nucleophilic substitution of hydrogen
Pastyrikova, Tereza,Iakobson, George,Vida, Norbert,Pohl, Radek,Beier, Petr
supporting information; experimental part, p. 2123 - 2126 (2012/06/01)
1-Nitro-4-(pentafluorosulfanyl)benzene underwent direct amination with 1,1,1-trimethylhydrazinium iodide in the presence of tBuOK in DMSO to give 2-nitro-5-(pentafluorosulfanyl)aniline in good yield. 1-Nitro-3- (pentafluorosulfanyl)benzene, under similar
New 4-pentafluorosulfanyl and 4-perfluoroalkylthio derivatives of 1-chloro-2-nitro- and 1-chloro-2,6-dinitrobenzenes
Sipyagin, Alexey M.,Enshov, Vyacheslav S.,Kashtanov, Sergei A.,Bateman, Colin P.,Mullen, Brian D.,Tan, Ying-Teck,Thrasher, Joseph S.
, p. 1305 - 1316 (2007/10/03)
New 4-pentafluorosulfanyl and 4-perfluoroalkylthio derivatives of 1-chloro-2-nitrobenzene and 1-chloro-2,6-dinitrobenzene were prepared from the corresponding bis(4-chloro-3-nitrophenyl)disulfide and bis(4-chloro-3,5-dinitrophenyl)disulfide, respectively. The SF5 derivatives were obtained by fluorination of the disulfides with AgF2 according to Sheppard's method, while perfluoroalkylation was carried out by means of thermolytic reactions with xenon(II) bis(perfluoroalkylcarboxylates). The introduction of fluorine-containing, electron-withdrawing substituents into the aromatic ring (in the presence of other deactivating groups) reinforces the activation of the halogen substituent towards nucleophilic attack. Several nucleophilic substitution reactions have been carried out with these compounds, and as a result, some N- and S-containing groups were introduced in the benzene ring. For example, the previously unknown SF5, CF3S, and C2F5S analogues of trifluralin (Treflan) were prepared and characterized. Additional synthetic possibilities for heterocyclic chemistry are presented on the basis of reactions of the new 1-chloro-2,6-dinitrobenzene derivatives with ethyl thioglycolate wherein fluorine-containing derivatives of benzothiazole N-oxide were obtained as the main products.
