- POLYMER FILM, RETARDATION FILM, POLARIZING PLATE, LIQUID CRYSTAL DISPLAY, AND COMPOUND
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Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Qa, Qb, and Qc are a single bond or a divalent linking group. Ra, Rb, and Rc, are hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, cyano group, halogen group, or heterocyclic group. X2 is a single bond or a divalent linking group. X1 is a single bond or a predetermined divalent linking group. R1 and R2 are a hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, or heterocyclic group Formula (1)
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Paragraph 0370-0374
(2016/06/28)
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- HAIR DYE AGENT COMPRISING AMINOPYRIMIDINE DERIVATIVES
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The application relates to agents for dyeing keratin fibers. The agent can be present in a cosmetic carrier and includes at least one compound of formula (I) and/or a physiologically compatible salt of this compound, in which R1 is a C1-C4 alkyl group, R2 is a hydrogen atom, a C1-C8 alkyl group, a C2-C6 alkenyl group, a C1-C6 hydroxyalkyl group, a C2-C6 polyhydroxyalkyl group, a C1-C6 alkoxy group, a C1-C6 alkylamino group, a di-C1-C6 alkylamino group, a C1-C6 polyalkoxy group, a C1-C6 alkylamido-(C1-C6) alkyl group, wherein the amide function can be substituted by one or two groups X, or is an aryl group, Y is an NH2 or an OH group, at least one coupler component selected from 3-amino-2-methylamino-6-methoxypyridine, 3-amino-6-methylphenol, 3-amino-2-hydroxypyridine, 1,3 -bis-(2,4-diaminophenoxy)propane, 2,7-dihydroxynaphthalene, 2-methylresorcinol, 2,5-dimethylresorcinol, 4-chlororesorcinol, 3-aminophenol, 2-amino-3-hydroxypyridine, 2-chloro-6-methyl-3-aminophenol, 2,6-dihydroxy-3,4-dimethylpyridine, 2-({3-[(2-hydroxyethyl)amino]-4-methoxy-5-methylphenyl}amino)ethanol, 2-({3-[(2-hydroxyethyl)amino]-2-methoxy-5-methylphenyl}amino)ethanol, 1-methoxy-2-amino-4-beta-hydroxy-ethylaminobenzene (Lehmann's blue), 2,4-diaminophenoxyethanol, 5-amino-4-chloro-o-cresol, 2,4-dichloro-m-aminophenol, 2,6-dihydroxy-3,4-dimethylpyridine and/or a physiologically compatible salt of these compounds.
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Paragraph 0239; 0240; 0241; 0242; 0243
(2015/08/04)
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- Imidazopyridine- and purine-thioacetamide derivatives: Potent inhibitors of nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1)
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Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) belongs to the family of ecto-nucleotidases, which control extracellular nucleotide, nucleoside, and (di)phosphate levels. To study the (patho)physiological roles of NPP1 potent and selective inhibitors with drug-like properties are required. Therefore, a compound library was screened for NPP1 inhibitors using a colorimetric assay with p-nitrophenyl 5′-thymidine monophosphate (p-Nph-5′-TMP) as an artificial substrate. This led to the discovery of 2-(3H-imidazo[4,5-b]pyridin-2-ylthio)-N-(3,4-dimethoxyphenyl)acetamide (5a) as a hit compound with a Ki value of 217 nM. Subsequent structure-activity relationship studies led to the development of purine and imidazo[4,5-b]pyridine analogues with high inhibitory potency (Ki values of 5.00 nM and 29.6 nM, respectively) when assayed with p-Nph-5′-TMP as a substrate. Surprisingly, the compounds were significantly less potent when tested versus ATP as a substrate, with Ki values in the low micromolar range. A prototypic inhibitor was investigated for its mechanism of inhibition and found to be competitive versus both substrates.
- Chang, Lei,Lee, Sang-Yong,Leonczak, Piotr,Rozenski, Jef,De Jonghe, Steven,Hanck, Theodor,Müller, Christa E.,Herdewijn, Piet
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p. 10080 - 10100
(2015/02/05)
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- Synthesis and biological evaluation of 5-substituted O4- alkylpyrimidines as CDK2 inhibitors
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CDK2 inhibitory structure-activity relationships have been explored for a range of 5-substituted O4-alkylpyrimidines. Variation of the 5-substituent in the 2,6-diaminopyrimidine series confirmed the 5-nitroso substituent as optimal, and showed that 5-formyl and 5-acetyl substituents were also tolerated at this position. A series of O4-alkyl-N 2-aryl-5-substituted-6-aminopyrimidines revealed interesting structure-activity relationships. In the 5-nitroso series, the optimum O 4-alkyl substituents were cyclohexylmethyl or sec-butyl, combined with a 2-sulfanilyl group. By contrast, in the N2-arylsulfonamido-5- formyl series, the cyclohexylmethyl compound showed relatively poor activity compared with the sec-butyl derivative (22j, (R)-4-(4-amino-6-sec-butoxy-5- formylpyrimidin-2-ylamino)benzenesulfonamide; CDK2 IC50 = 0.8 nM). Similarly, in the N2-arylsulfonamido-5-(hydroxyiminomethyl) series the O4-sec-butyl substituent conferred greater potency than the cyclohexylmethyl (23c, (rac)-4-(4-amino-6-sec-butoxy-5-(hydroxyiminomethyl) pyrimidin-2-ylamino)benzenesulfonamide; CDK2 IC50 = 7.4 nM). The 5-formyl derivatives show selectivity for CDK2 over other CDK family members, and are growth inhibitory in tumour cells (e.g.22j, GI50 = 0.57 μM).
- Marchetti, Francesco,Cano, Celine,Curtin, Nicola J.,Golding, Bernard T.,Griffin, Roger J.,Haggerty, Karen,Newell, David R.,Parsons, Rachel J.,Payne, Sara L.,Wang, Lan Z.,Hardcastle, Ian R.
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supporting information; experimental part
p. 2397 - 2407
(2010/07/09)
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- Novel antiallergic agents. Part I: Synthesis and pharmacology of pyrimidine amide derivatives
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We have synthesized many pyrimidine amide derivatives. Novel pyrimidine bis-glycolic amide derivatives showed moderate inhibition in the rat passive cutaneous anaphylaxis (PCA) assay by oral administration. Among these compounds, 2,4-bis(methoxyacetylamino)-6-piperidinopyrirnidine (2i) exhibited significant inhibition. However the compound (2i) did not inhibit antigen-induced histamine or SRS-A release from lung fragments of the guinea-pig at less than 10-4 M. Derivatives of 2i have also notable or moderate activity in the rat PCA assay. Compound 2h which has no oxygen atom at the α-position of the amide carbonyl group and, compound 17 which has no amide carbonyl group, showed no inhibition in the rat PCA assay. We supposed that both the amide carbonyl group and the oxygen atom at α-position of the amide carbonyl group play an important role in inhibiting the rat PCA reaction. These pyrimidine bis-glycolic amide derivatives have a novel structure and unique activity which suggests they may be potentially useful in the treatment of allergic diseases. Copyright (C) 1998 Elsevier Science Ltd.
- Ban, Masakazu,Taguchi, Hiroaki,Katsushima, Takeo,Aoki, Shoichi,Watanabe, Akihiko
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p. 1057 - 1067
(2007/10/03)
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- Synthesis of Some Substituted Guanidinopyrimidines and their Structural Assignment by 13C and 1H NMR
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A series of substituted 2- and 4-guanidinopyrimidines were prepared by reaction of halopyrimidines with guanidine; alkylamino and amino substituents were introduced by subsequent halogen replacement by primary amines or ammonia or the catalytic reduction of nitro groups.Structural assignments were made on the basis of 13C and 1H nmr.A guanidinopteridine and a bispyrimidinylguanidine were also synthesized.Some unsuccessful reaction illustrated the low nucleophilic reactivity and thermal instability of the guanidine group.
- Ladd, David L.
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p. 917 - 921
(2007/10/02)
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