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Conventionally known color filter may be formed from a colored resin composition [a], the resistance is not sufficiently satisfactory in some cases. [Solution] the compound of the present invention, formula (1) is represented. [Drawing] no (by machine translation)

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Disclosed is a compound which is useful in preventing and treating cardiac arrhythmia such as atrial fibrillation. A compound represented by formula (1) or a pharmaceutically acceptable salt of the same. In formula (1), ring X represents benzene or pyridine; R1 represents an optionally substituted alkyl group; R2 represents an optionally substituted aryl group, an optionally substituted heterocyclic group, an optionally substituted arylalkyl group or an optionally substituted heterocyclic group-substituted alkyl group; R3, R4, R5, R6, R7, R8 and R9 represent each hydrogen or an alkyl group, provided that R3 and R5 may be bonded to each other to form, together with the carbon atom adjacent thereto, a cycloalkyl group; and m represents 0 or 1.

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A series of 3-arylthio-1,3-disubstituted-oxindoles were prepared in good yields by the reaction of alpha-diazocarbonyl compounds and sulfenamides. The reaction involves a Rh-catalyzed thia-Sommelet-Hauser-type rearrangement.(Figure Presented)

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The HIV-1 CA protein has gained remarkable attention as a promising therapeutic target for the development of new antivirals, due to its pivotal roles in HIV-1 replication (structural and regulatory). Herein, we report the design and synthesis of three series of benzenesulfonamide-containing phenylalanine derivatives obtained by further structural modifications of PF-74 to aid in the discovery of more potent and drug-like HIV-1 CA inhibitors. Structure-activity relationship studies of these compounds led to the identification of new phenylalanine derivatives with a piperazinone moiety, represented by compound 11l, which exhibited anti-HIV-1NL4-3 activity 5.78-fold better than PF-74. Interestingly, 11l also showed anti-HIV-2ROD activity (EC50 = 31 nM), with almost 120 times increased potency over PF-74. However, due to the higher significance of HIV-1 as compared to HIV-2 for the human population, this manuscript focuses on the mechanism of action of our compounds in the context of HIV-1. SPR studies on representative compounds confirmed CA as the binding target. The action stage determination assay demonstrated that these inhibitors exhibited antiviral activities with a dual-stage inhibition profile. The early-stage inhibitory activity of compound 11l was 6.25 times more potent as compared to PF-74 but appeared to work via the accelerating capsid core assembly rather than stabilization. However, the mechanism by which they exert their antiviral activity in the late stage appears to be the same as PF-74 with less infectious HIV-1 virions produced in their presence, as judged p24 content studies. MD simulations provided the key rationale for the promising antiviral potency of 11l. Additionally, 11l exhibited a modest increase in HLM and human plasma metabolic stabilities as compared to PF-74, as well as a moderately improved pharmacokinetic profile, favorable oral bioavailability, and no acute toxicity. These studies provide insights and serve as a starting point for subsequent medicinal chemistry efforts in optimizing these promising HIV inhibitors.

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The present invention provides ras farnesyl transferase inhibiting compounds of Formula I. The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I

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Chiral tridentate P,N,N ligands have been demonstrated to be highly efficient for the coppercatalyzed enantioselective propargylic amination of propargylic acetates with both primary and secondary amines as nucleophiles, affording the corresponding propargylic amines in high yields and with excellent enantioselectivities (up to 97% ee for secondary amines, and up to 96% ee for primary amines). Furthermore, the present catalytic system was also effective for the more challenging aliphatic propargylic acetate substrates.

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Two classes of molecules were designed and synthesized based on a 6-CH 3 cyclopenta[d]pyrimidine scaffold and a pyrrolo[2,3-d]pyrimidine scaffold. The pyrrolo[2,3-d]pyrimidines were synthesized by reacting ethyl 2-cyano-4,4-diethoxybutanoate and acetamidine, which in turn was chlorinated and reacted with the appropriate anilines to afford 1 and 2. The cyclopenta[d]pyrimidines were obtained from 3-methyladapic acid, followed by reaction with acetamidine to afford the cyclopenta[d]pyrimidine scaffold. Chlorination and reaction with appropriate anilines afforded (±)-3?HCl-(±)-7?HCl. Compounds 1 and (±)-3?HCl had potent antiproliferative activities in the nanomolar range. Compound (±)-3?HCl is significantly more potent than 1. Mechanistic studies showed that 1 and (±)-3?HCl cause loss of cellular microtubules, inhibit the polymerization of purified tubulin, and inhibit colchicine binding. Modeling studies show interactions of these compounds within the colchicine site. The identification of these new inhibitors that can also overcome clinically relevant mechanisms of drug resistance provides new scaffolds for colchicine site agents.

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N-Aryl-N-methylaminocyclohexanols 10-12 were synthesised and their crystal structures were studied by X-ray diffraction. Compound 10 crystallizes in the monoclinic space group Cc with cell parameters of a = 13.7366(2) A, b = 13.7234(2) A, c = 26.9057(5) A, beta = 93.0900(5), V = 5064.70(14) A3 and Z = 16. Compound 11 crystallizes in the trigonal space group P 3 with cell parameters of a = b = 25.4429(4) A, c = 9.6417(2) A, V = 5405.27(16) A3 and Z = 18. Compound 12 crystallizes in the monoclinic space group P21/n with cell parameters of a = 9.9511(2) A, b = 11.5777(2) A, c = 20.5968(4) A, beta = 95.5037(9), V = 2362.04(8) A3 and Z = 8. All three structures were characterised by arrays of hydrogen bonding interactions and these crystallographic studies revealed conformations of 10-12 which gave valuable information into the mechanism of the reaction during their formation. Graphical Abstract: Crystals of (RS,RS,RS)-3-[N-methyl-N-(4′-methoxyphenyl) amino]cyclohexane-1,2-diol, (RS,RS,RS)-3-(N-methyl-N-phenylamino)cyclohexane-1, 2-diol and (RS,RS,RS)-2-fluoro-6-(N-methyl-N-phenylamino)cyclohexan-1-ol were synthesised and their structures were studied by X-ray diffraction.[Figure not available: see fulltext.].

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Racemic pyrrolo [2,3-b]indoles were efficiently synthesized by the reaction of aromatic hydrazines with 4-chloro-2-methylbutanal. A formal total synthesis of physostigmine was achieved.

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In the presence of a Na-exchanged Y faujasite, the reaction of primary aromatic amines 1 with 2-(2-methoxyethoxy)methylethyl carbonate [MeO(CH2)2O(CH2)2 OCO2Me, 2a] yields the corresponding mono-N-methyl derivatives ArNHMe with selectivity up to 95%, at substantially quantitative conversions. At 130C, the reaction can be run under diffusion-free conditions and is strongly affected by the solvent polarity: for instance, in going from xylene (epsilonr = 2.40) to triglyme (epsilonr = 7.62) as the solvent, the pseudo-first-order rate constant for the aniline (1a) disappearance shows a 5-fold decrease. In DMF (epsilonr = 38.25), the same reaction does not occur at all. Competitive adsorption of the solvent and the substrate onto the catalytic sites accounts for this result. The behavior of alkyl-substituted anilines ZC6H4NH2 [Z = p-Me, p-Et, p-Pr, p-(n-Bu) (1b-e); Z = 3,5-di-tert-butyl- and 2,4,6-tri-tert-butylanilines (1f,g)] and p-alkoxyanilines p-ZC6H4NH2 [Z = OMe, OEt, OPr, O-n-Bu (1b?-e?)] clearly indicates a steric effect of ring substituents: as diffusion of the amine into the catalytic pores is hindered, the reaction hardly proceeds and the mono-N-methyl selectivity (SM/D) drops as well. Moreover, the strength of adsorption of the amine onto the catalyst influences the rate and the selectivity as well: the reaction of p-anisidine and p-toluidine – despite the higher nucleophilicity of these compounds – is slower and even less selective with respect to aniline. From a mechanistic viewpoint, the intermediacy of carbamates ArN(Me)CO2R [R = MeO-(CH2)2O(CH2)2] is suggested. At 90C, the reaction of benzylamine (7) – a model for aliphatic amineswith dimethyl carbonate shows that the reaction outcome can be improved by tuning the amphoteric properties of the catalyst: in going from CsY to the more acidic LiY zeolite, methylation is not only more selective (SM/D ratio increases from 77% to 84%) but even much faster (CsY, conversion of 36% after 22 h; LiY, conversion of 43% after 7 h).

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