- Pyridine compound, preparation method and application thereof, and pharmaceutical composition
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The invention provides a pyridine compound as well as a preparation method and application thereof, and belongs to the technical field of medical chemistry. The pyridine compound provided by the invention has excellent in-vitro antiviral activity and potential druggability, and is expected to become a clinical candidate molecule for overcoming influenza.
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Paragraph 0214-0216
(2021/02/10)
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- AZO COMPOUND, INK COMPOSITION, RECORDING METHOD AND COLORED MATERIAL
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PROBLEM TO BE SOLVED: To provide a dye which has extremely excellent ozone gas resistance, extremely high print density, excellent color rendering property, and a high-quality black hue with low saturation, and to provide an ink composition containing the dye. SOLUTION: The present invention provides an azo compound represented by formula (1) or a tautomer thereof, or a salt thereof [R1 is a (C1-C4) alkyl group or the like; R2 is a cyano group or the like; R3 and R4 independently represent H, a carboxy group and the like (one of them is a carboxy group); R5 and R7 independently represent a (C1-C4) alkylthio group or the like; R6 and R8 independently represent a (C1-C4) alkylcarbonyl amino group; R9 is a sulfo (C1-C4) alkoxy group; R10 is a methyl group or the like; R11-R13 independently represent H, a sulfo group or the like). SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
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Paragraph 0110; 0111
(2017/01/02)
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- AZO COMPOUND, INK COMPOSITION, RECORDING METHOD AND COLORED MATERIAL
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PROBLEM TO BE SOLVED: To provide a dye which has extremely excellent ozone gas resistance, extremely high print density, low color rendering property, and a high-quality black hue with low saturation, and to provide a black ink composition for inkjet recording containing the dye. SOLUTION: The present invention provides an azo compound represented by the following formula or a salt thereof [R1 is a C1-4 alkyl group or the like; R2 is a cyano group or the like; R5-R7 independently represent H, a C1-4 alkyl group, C1-4 alkoxy group or the like; R8-R10 independently represent H, a C1-4 alkylcarbonylamino group, C1-4 alkylthio group or the like; R11 is a C1-4 alkylthio group or the like; R12 and R13 independently represent H, a C1-8 alkylcarbonylamino group or the like; group A is a substituted naphthyl group]. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
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Paragraph 0133-0134
(2017/01/05)
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- AZO COMPOUND, INK COMPOSITION, RECORDING METHOD AND COLORED MATTER
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PROBLEM TO BE SOLVED: To provide a dye having a high-quality black hue with very excellent (ozone) gas resistance, a very high print density, low color rendering properties, and a low saturation, when recorded on inkjet exclusive paper, and an ink composition comprising the dye. SOLUTION: The present invention provides an azo compound represented by formula (1) or a tautomer thereof, or a salt thereof [R1 is a (C1-C4) alkyl group or the like; R2 is a cyano group; R3 and R4 independently represent H, a sulfo group or the like; R5 and R7 independently represent a (C1-C4) alkylthio group or the like; R6 and R8 independently represent an acetylamino group; R9 is a sulfo (C1-C4) alkoxy group; R10 is a methyl group; and at least one of R11-R13 is a cyano group]. SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0098-0099
(2017/04/28)
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- AZO COMPOUND, INK COMPOSITION, RECORDING METHOD AND COLORED MATTER
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PROBLEM TO BE SOLVED: To provide a dye having a high-quality black hue with excellent gas resistance, printability, and color rendering properties, and a low saturation, and an inkjet recording black ink composition comprising the dye. SOLUTION: The present invention provides an azo compound represented by formula (1) or a tautomer thereof, or a salt thereof (R1 is a (C1-C4) alkyl group or the like; R2 is a cyano group; R3 and R4 independently represent H, a sulfo group or the like; R5 and R7 independently represent a (C1-C4) alkylthio group or the like; R6 and R8 independently represent a (C1-C4) alkylcarbonyl amino group; R9 is a sulfo (C1-C4) alkoxy group; R10 is a methyl group; R11-R13 are H, a sulfo group, or a nitro group; and at least one of R11-R13 is a nitro group). SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0099
(2017/04/14)
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- AZO COMPOUND, INK COMPOSITION, RECORDING METHOD AND COLORED MATTER
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PROBLEM TO BE SOLVED: To provide a dye having a high-quality black hue with excellent ozone resistance, light resistance, humidity resistance and the like. SOLUTION: The present invention provides an azo compound represented by formula (1) or a tautomer thereof, or a salt thereof (R1 is a (C1-C4) alkyl group or the like; R2 is a cyano group; R3 and R4 are H, a sulfo group or the like; R5 and R7 are a (C1-C4) alkylthio group or the like; R6 and R8 is a (C1-C4) alkylcarbonyl amino group; R9 is a sulfo (C1-C4) alkoxy group; R10 is a methyl group; R11-R13 are H, a sulfo group, a halogen atom; and at least two of R11-R13 are a halogen atom). SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0098-0099
(2017/04/14)
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- Azo compound, composition, and method for recording the colored material (by machine translation)
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PROBLEM TO BE SOLVED: jet only when, in a very light resistance, very high density, excellent color rendering properties, and low saturation, hue of high quality black pigment, and the ink composition containing a pigment, especially black ink-jet recording. SOLUTION: eq. (1) or an azo compound expressed by tautomerically isomer, or their salts. ( In the formula, R 1 the alkyl group or the like (C1-C4), R 2 cyano group or, R 3 and R 4 each represent a hydrogen atom, or the like; sulfocarboxylic, R 5 and R 7 like sulfocarboxylic, R 6 and R 8 each independently the, one halogen atom, one alkyl group (C1-C4) arylsulfonylaminocarbonylamino, R 9 and R 10 which are each independently, such as alkyl group such as (C1-C4), R 11 from R 13 each represent a hydrogen atom, a sulfo group or the l ) Selected drawing: no (by machine translation)
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Paragraph 0132-0133
(2016/10/10)
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- Trisazo compd. dye, ink composition, recording method and colored material
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A coloring matter for black ink which is highly soluble in water-based media, and ink compositions containing the same. The ink compositions can produce black recorded images which exhibit excellent light fastness and ozone gas fastness. The coloring matter consists of at least one trisazo compound represented by general formula (1), tautomers thereof, and salts of both. In general formula (1), R1 is unsubstituted C1-4 alkyl or the like; R2 is cyano or the like; R3 is a chlorine atom or the like; R5 to R7 are a hydrogen atom, unsubstituted C1-4 alkyl, sulfo-substituted C1-4 alkoxy, or the like; R8 to R10 are a hydrogen atom, unsubstituted C1-4 alkyl, sulfo-substituted C1-4 alkylthio, or the like; A is sulfo-substituted 2-naphthothiazolyl or the like; and a to d represent the positions at which the ring is substituted with R3 and sulfo.
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Paragraph 0222; 0223
(2016/12/26)
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- Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors
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By combining the scaffolds of UI-125 and Sorafenib, a series of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine moiety were designed and synthesized as novel DFG-out B-RafV600E inhibitors. Among them, 20c-e, 20g and 21h displayed potent antiproliferative activities against melanoma A375 (B-RafV600E) cell lines with IC50 values of 3.190, 2.276, 1.856, 1.632 μM and 1.839 μM, respectively, comparable with the positive control Vemurafenib (IC50 Combining double low line 3.32 μM). Selected compounds were tested for the ERK inhibition in human melanoma A375 (B-RafV600E) and SK-MEL-2 (B-RafWT) cell lines by Western blot. The results revealed that our compounds inhibited the proliferation of melanoma A375 cells (B-RafV600E) through ERK pathway, without paradoxical activation of ERK in melanoma SK-MEL-2 cells (B-RafWT). Eventually, 20g and 21h were selected to confirm their inhibitory effects on tumor growth in A375 xenograft models in mice. Compound 20g exhibited equivalent antitumor efficacy in vivo (T/C Combining double low line 44.37%), compared to Sorafenib (T/C Combining double low line 37.35%), by 23-day repetitive administration of a single dose of 50 mg/kg without significant body weight loss.
- Yang, Weimin,Chen, Yadong,Zhou, Xiang,Gu, Yazhou,Qian, Wenqi,Zhang, Fan,Han, Wei,Lu, Tao,Tang, Weifang
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supporting information
p. 581 - 596
(2014/12/12)
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- Design and synthesis of tag-free photoprobes for the identification of the molecular target for CCG-1423, a novel inhibitor of the Rho/MKL1/SRF signaling pathway
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CCG-1423 and related analogues represent a new class of inhibitors of Rho/MKL1/SRF-mediated gene transcription, a pathway that has been implicated in both cancer and fibrosis. The molecular target for these compounds is unknown. To facilitate its identification, a series of tag-free photoaffinity probes was designed and synthesized, each one containing a photoactivatable group and an acetylenic end group for subsequent attachment to a fluorescent tag using click chemistry. All were confirmed to maintain biological activity in a cell-based assay for inhibition of SRE-Luc expression. The functional activity of the most potent probe 24 was further confirmed in an assay for PC-3 cell migration. Photolysis of 24 in intact PC-3 cells followed by cell lysis, click ligation of a fluorescent dye, and gel electrophoresis revealed specific labeling of a single 24 kDa band that could be blocked with an active competitor. Future work will focus on identifying the labeled protein(s).
- Bell, Jessica L.,Haak, Andrew J.,Wade, Susan M.,Sun, Yihan,Neubig, Richard R.,Larsen, Scott D.
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supporting information
p. 966 - 973
(2013/07/11)
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- AZO COMPOUND, INK COMPOSITION, RECORDING METHOD AND COLORED MATERIAL
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Provided are: a dye which exhibits extremely excellent (ozone) gas resistance, extremely high print density, low color rendering properties, low color saturation, and high-quality black hue when is recorded on a paper only for inkjet printing purposes, i.e., an azo compound represented by formula (1), a tautomer of the azo compound, or a salt of the azo compound or the tautomer; and an ink composition containing the dye, particularly a black ink composition for inkjet recording applications. In the formula, R1 represents a (C1-C4) alkyl group, or the like; R2 represents a cyano group, or the like; R3 and R4 independently represent a hydrogen atom, a sulfo group, a (C1-C4) alkoxy group, or the like; R5 and R7 independently represent a (C1-C4) alkylthio group, or the like; R6 and R8 independently represent a (C1-C4) alkylcarbonylamino group; R9 and R10 independently represent a (C1-C4) alkoxy group, or the like; and R11 to R13 independently represent a hydrogen atom, a sulfo group, or the like.
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Paragraph 0162
(2013/11/05)
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- Ink, ink cartridge and ink jet recording method
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Provided is an ink capable of recording an image that is excellent in ozone resistance, hardly causes blurring or color change even in a high-humidity environment, and is excellent in humidity resistance. The ink includes a coloring material and a lithium ion. The coloring material includes a compound represented by the following general formula (I) and a content of the lithium ion in the ink is 3.5 times or more in terms of molar ratio with respect to a content of the compound represented by the general formula (I).
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Paragraph 0108
(2014/01/08)
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- An efficient catalytic method for the Beckmann rearrangement of ketoximes to amides and aldoximes to nitriles mediated by propylphosphonic anhydride (T3P)
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An efficient method for the Beckmann rearrangement of ketoximes to amides mediated by a catalytic amount (15 mol %) of propylphosphonic anhydride (T3P) is described. Aldoximes underwent second order Beckmann rearrangement to provide the corresponding nitriles in excellent yields on reacting with T3P (15 mol %) at room temperature. The main advantages of this environmentally friendly protocol include procedural simplicity, and particularly ease of isolation of the products.
- Augustine, John Kallikat,Kumar, Rajesha,Bombrun, Agnes,Mandal, Ashis Baran
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scheme or table
p. 1074 - 1077
(2011/03/22)
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- Simple and efficient method for acetylation of alcohols, phenols, amines, and thiols using anhydrous NiCl2 under solvent-free conditions
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Solvent-free acetylation of alcohols, phenols, amines, and thiols with acetic anhydride (Ac2O) in the presence of 0.1mol% (13mg) anhydrous NiCl2, an inexpensive and easily available catalyst, is described. Excellent yields, short reaction time, and mild reaction conditions are important features of this method.
- Meshram, Gangadhar,Patil, Vishvanath D.
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experimental part
p. 4384 - 4395
(2010/04/29)
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- HETEROCYCLIC MODULATORS OF NUCLEAR RECEPTORS
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Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. In certain embodiments, the compounds are thiazolidinone derivatives.
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- Synthesis of N-(3-azido-4-chlorophenyl)-N'-[3H-methyl]thiourea, an efficient photoaffinity probe for the urea carrier
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Starting from commercial 4-chloro-3-nitroaniline, through a 5 step synthesis, was prepared 3-azido-4-chlorophenylisothiocyanate 5 which was reacted with [3H]-methylamine. The latter was obtained by three methods: i- [3H]-LiAlT4 reduction of benzylcarbamate gave rise to [3H][-methylamine (S.A.: >70 Ci/mmol). ii- Catalytic reduction of HCN with 3H2 lead to [3H]-CH3NH2 (S.A.: 0.7 Ci/mmol). iii- Schmidt rearrangement of [3H]-sodium acetate gave [3H]-CH3NH2 (S.A.: 29 Ci/mmol). Compound 7 at the highest specific activity had a self radiolysis rate precluding its practical use in biological studies whilst 29 Ci/mmol [3H]-7 was satisfactory.
- Lamotte,Degeilh,Neau,Ripoche,Rousseau
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p. 289 - 295
(2007/10/02)
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- A Comparison of the Reactions of Some Ethyl N-Arylcarbamates with Those of the Corresponding Acetanilides. I. Nitration
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The reactions of some ethyl N-arylcarbamates and of the corresponding acetanilides towards 1 equiv. of sodium nitrate in concentrated sulfuric acid at 0-5 deg have been compared with one another and have been found to exhibit significant differences.Except in the case of the unsubstituted analogues, nitration of the carbamates was found to occur significantly more quickly than that of the acetanilides as shown by (i) a representative competitive nitration, and (ii) the fact the carbamates containing a nitro group are nitrated smoothly whereas the corresponding nitroacetanilides are slow to react.On the basis of competitive reactions, it is suggested that this difference in reactivity is due to steric factors.
- Rosevear, Judi,Wilshire, John F. K.
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p. 723 - 733
(2007/10/02)
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