6661-54-7Relevant academic research and scientific papers
BIPHENYL COMPOUND AS CCR2/CCR5 RECEPTOR ANTAGONIST
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Paragraph 0096, (2019/11/21)
Provided is a CCR2/CCR5 receptor antagonist and the use thereof in the preparation of a drug for treating diseases associated with the CCR2/CCR5. In particular, disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof
MANUFACTURING METHOD OF 1,1-DISUBSTITUTED HYDRAZINE COMPOUND
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Paragraph 0053-0055; 0056-0058, (2020/01/23)
PROBLEM TO BE SOLVED: To provide a manufacturing method of a 1,1-disubstituted hydrazine compound useful as a manufacturing intermediate. SOLUTION: There is provided a manufacturing method of a 1,1-disubstituted hydrazine compound represented by the formula (3) by reacting a hydrazino compound represented by the formula (1) with a compound represented by the formula (2): R-A in the presence of a correlation transfer catalyst, and a base such as alkali metal hydroxide, alkali earth metal hydroxide, and alkali metal alkoxide in a mixed solvent of water and a water insoluble organic solvent. In the formula, Q represents O, S or the like; R represents a C1 to 12 organic group which may have a substituent; A represents Cl, Br, a tosyl group or the like; Ra1 to Ra4 each independently represent H, a halogen atom, a C1 to 6 alkyl group, or the like. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT
METHODS OF MAKING SUBSTITUTED PORPHYRIN PHARMACEUTICAL COMPOUNDS AND COMPOSITIONS
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Page/Page column 28; 29, (2018/07/29)
Described herein are methods and intermediates useful for making substituted porphyrins, including Mn(III) orthoN-butoxyethylpyridylporphyrin, and compositions comprising the same. In some embodiments, a method of the present invention provides a composition having a certain percentage or yield (e.g., at least 80%, 85%, 90%, or 95% by weight) of a compound of the present invention.
Rapid transformation of sulfinate salts into sulfonates promoted by a hypervalent iodine(III) reagent
Deruer, Elsa,Hamel, Vincent,Blais, Samuel,Canesi, Sylvain
supporting information, p. 1203 - 1207 (2018/06/04)
An alternative method for forming sulfonates through hypervalent iodine(III) reagent-mediated oxidation of sodium sulfinates has been developed. This transformation involves trapping reactive sulfonium species using alcohols. With additional optimization of the reaction conditions, the method appears extendable to other nucleophiles such as electron-rich aromatic systems or cyclic ethers through a ring opening pathway.
Synthesis and biological evaluation of novel 4-hydroxybenzaldehyde derivatives as tyrosinase inhibitors
Yi, Wei,Cao, Rihui,Peng, Wenlie,Wen, Huan,Yan, Qin,Zhou, Binhua,Ma, Lin,Song, Huacan
experimental part, p. 639 - 646 (2010/04/02)
A series of novel 4-hydroxybenzaldehyde derivatives were synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were investigated. Most of target compounds had more potent inhibitory activities than the parent compound 4-hydroxybenzaldehyde (IC50 = 1.22 mM). Interestingly, compound 3c bearing a dimethoxyl phosphate was found to be the most potent inhibitor with IC50 value of 0.059 mM. The inhibition kinetics analyzed by Lineweaver-Burk plots revealed that compound 3c was a non-competitive inhibitor (KI = 0.0368 mM). In particular, compound 3c showed no side effects at dose of 1600 mg/kg in mice. These results suggested that such compounds might be served as lead compounds for further designing new potential tyrosinase inhibitors.
ELECTRON DONATING ORGANIC MATERIAL, MATERIAL FOR PHOTOVOLTAIC ELEMENT, AND PHOTOVOLTAIC ELEMENT
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Page/Page column 40-42, (2011/01/12)
The invention aims at providing a photovoltaic device with high photoelectric conversion efficiency. The aim is attained by an electron donating organic material containing a benzothiadiazole compound in which (a) a benzothiadiazole skeleton and an oligothiophene skeleton are contained, (b) a band gap (Eg) is 1.8 eV or less, and (c) the level of the highest occupied molecular orbital (HOMO) is -4.8 eV or less, wherein said benzothiadiazole compound is formed by covalently combining the benzothiadiazole skeleton and the oligothiophene skeleton alternately, the proportion between the benzothiadiazole skeleton and the oligothiophene skeleton is within a range of 1:1 to 1:2 (however, excluding 1:1), and the number of thiophene rings contained in an oligothiophene skeleton is 3 or more and 12 or less.
Inhibitory effects of 5-benzylidene barbiturate derivatives on mushroom tyrosinase and their antibacterial activities
Yan, Qin,Cao, Rihui,Yi, Wei,Chen, Zhiyong,Wen, Huan,Ma, Lin,Song, Huacan
experimental part, p. 4235 - 4243 (2009/12/24)
A series of novel 5-benzylidene barbiturate and thiobarbiturate derivatives were synthesized and evaluated as tyrosinase inhibitors and antibacterial agents. The results demonstrated that some compounds had more potent inhibitory activities than the parent compound 4-hydroxybenzaldehyde (IC50 = 1.22 mM). Particularly, compounds 1a and 2a were found to be the most potent inhibitors with IC50 value of 13.98 μM and 14.49 μM, respectively. The inhibition mechanism study revealed that these compounds were irreversible inhibitors. The circular dichroism spectra indicated that these compounds induced conformational changes of mushroom tyrosinase upon binding. In addition, these compounds exhibited selectively antibacterial activity against Staphylococcus aureus. All these results suggested that further development of such compounds may be of interest.
Cyclic peptide antifungal agents
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, (2008/06/13)
Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I STR1 where: R', R", R'", Rx1, Rx2, Ry1, Ry2, Ry3, Ry4, and R0 are as defined hereinabove; and R2 is STR2 R3 is STR3 R3a is C1 -C6 alkyl or C1 -C6 alkoxy; R3b and R3c are independently phenyl or naphthyl; R3d is C1 -C12 alkyl, C1 -C12 alkoxy or --O --(CH2)m -[O--(CH2)n ]p --O--(C1 -C12 alkyl); m is 2, 3 or 4; n is 2, 3 or 4; p is 0 or 1; or a pharmaceutically acceptable salt thereof.
Molecular Desidn of Crown Ethers. 4. Syntheses and Selective Cation Binding of 16-Crown-5 and 19-Crown-6 Lariats
Ouchi, Mikio,Inoue, Yoshihisa,Wada, Kazuhito,Iketani, Shin-ichi,Hakushi, Tadao,Weber, Edwin
, p. 2420 - 2427 (2007/10/02)
A number of new lariat 16-crown-5 and 19-crown-6 ethers posesing a variety of single or double side arm(s) were synthesized, and their cation-binding abilities were evaluated by solvent extraction technique.In general, the extractabilities of the 16-crown-5 lariats for most mono- and divalent cations increased gradually with extending oxyethylene side arm.However, sodium and silver ions, which are best size fitted to the crown cavity, showed peac extractability/selectivity at a specific length of the donating side arm.The complexation stoichiometry is 1 : 1 forall cations employed as confirmed by measurement of the extraction equilibrium constants for the single-armed 16-crown-5 (3p).The tetrasubstituted pivot carbon is shown to be a reguirement for lariat 16-crown-5 to effect extra side-arm ligation, although the second side arm of lariat ether 3e seems ineffective in extractability enhancement with reference to the single-armed analogue 3p.By contrast, the corresponding 19-crown-5 lariat with potential donor side arms at an appropiate position did not show any enhancement in extractability for most cations, which may be attributed to its flexible framework.
