- Phosphazene Base tBu-P4 Catalyzed Methoxy–Alkoxy Exchange Reaction on (Hetero)Arenes
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The organic superbase tBu-P4 catalyzes methoxy-alkoxy exchange reactions on (hetero)arenes with alcohols. The catalytic reaction proceeded efficiently with electron-deficient methoxy(hetero)arenes as well as with a variety of alcohols, including 3-amino-1-propanol, β-citronellol, menthol, and cholesterol. An intramolecular version of this reaction furnished six- and seven-membered ring compounds.
- Shigeno, Masanori,Hayashi, Kazutoshi,Nozawa-Kumada, Kanako,Kondo, Yoshinori
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supporting information
p. 6077 - 6081
(2019/03/26)
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- Synthesis and antimicrobial studies of new antibacterial azo-compounds active against staphylococcus aureus and listeria monocytogenes
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Some novel (phenyl-diazenyl)phenols (4a–m) were designed and synthesized to be evaluated for their antibacterial activity. Starting from an active previously-synthesized azobenzene chosen as lead compound, we introduced some modifications and optimization of the structure, in order to improve solubility and drug conveyance. Structures of all newly-synthesized compounds were confirmed by 1H nuclear magnetic resonance (NMR), mass spectrometry, and UV-Vis spectroscopy. Antibacterial activity of the new compounds was tested with the dilution method against the bacteria strains Listeria monocytogenes, Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa PAO1. All the compounds were selectively active against Gram-positive bacteria. In particular, compounds 4d, 4h, and 4i showed the highest activity against S. aureus and Listeria monocytogenes, reaching remarkable MIC100 values of 4 μg/mL and 8 μg/mL. The relationship between antimicrobial activity and compound structure has suggested that the presence of hydroxyl groups seems to be essential for antimicrobial activity of phenolic compounds.
- Piotto, Stefano,Concilio, Simona,Sessa, Lucia,Diana, Rosita,Torrens, Gabriel,Juan, Carlos,Caruso, Ugo,Iannelli, Pio
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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
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Page/Page column 48; 50; 53; 76
(2015/06/25)
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- Fused ring compound and use thereof
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The present invention provides a compound represented by the formula: wherein the symbols are as described in the specification, or a salt thereof, which is useful for preventing/treating eicosanoid-associated diseases such as atherosclerosis, diabetes, obesity, atherothrombosis, asthma, fever, pain, cancer, rheumatism, osteoarthritis and atopic dermatitis, and which has an excellent pharmacological action, physicochemical properties, etc.
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Page/Page column 38-39
(2010/08/07)
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- AMIDE COMPOUNDS AND MEDICINAL USE THEREOF
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The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X' is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
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- Electronic dependence of C-O reductive elimination from palladium (aryl)neopentoxide complexes
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Thermal decomposition of the palladium (aryl)neopentoxide complexes [P-P]Pd(Ar)OCH2CMe3 [P-P =Tol-BINAP or BINAP; Ar p-C6H4CHO (1b), p-C6H4COPh (1c), p-C6H4NO2 (1d), o-C6H4NO2 (1e), o-C6H4CN (1F)] possessing substituents on the palladium-bound aryl group suitable for delocalization of negative charge led to quantitative (≤95%) formation of aryl ether without detectable β-hydride elimination. Thermal decomposition of 1b-f obeyed first-order kinetics, and the rate of reductive elimination decreased in the order o-NO2 > p-NO2 > p-CHO > p-COPh > o-CN. Conversely, thermal decomposition of the related derivatives [P-P]Pd(Ar)OCH2CMe3 [P-P = Tol-BINAP or BINAP; Ar p-C6H4Cl (1g), m-C6H4NO2 (1h), m-C6H4CN (1i)] which did not possess a resonance stabilizing group on the palladium-bound aryl group led to no detectable formation of aryl ether. These and related data point to the buildup of negative charge in the palladium-bound aryl group in the transition state for C-O reductive elimination and are consistent with a mechanism initiated by inner-sphere nucleophilic attack of the alkoxide ligand at the ipso-carbon atom of the palladium-bound aryl group through a zwitterionic Meisenheimer-type intermediate or transition state.
- Widenhoefer, Ross A.,Buchwald, Stephen L.
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p. 6504 - 6511
(2007/10/03)
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- Studies on antihyperlipidemic agents. III. Synthesis and biological activities of 2-chloro-3-arylpropionic acids containing a quarternary carbon atom
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A series of 2-chloro-3-(4-alkoxyphenyl)propionic acids containing a quarternary carbon atom in the alkoxy moiety was prepared and the hypolipidemic and hypoglycemic activities were evaluated. Of the 18 compounds synthesized, ethyl 2-chloro-3-[4-(2-methyl-2-phenylpropyloxy)phenyl]propionate was the best with respect to biological activity and toxicity. Its functional derivatives and optically resolved enantiomers were also prepared. Structure-activity relationships are discussed briefly.
- Kawamatsu,Asakawa,Saraie,Mizuno,Imamiya,Nishikawa,Hamuro
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p. 751 - 758
(2007/10/02)
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- α-Chlorocarboxylic acids
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α-CHLOROCARBOXYLIC ACIDS OF THE FORMULA STR1 wherein Y stands for a lower alkyl group having 1 to 6 carbon atoms or a phenyl group, a benzoyl group or a phenylalkyl group having 7 to 11 carbon atoms, which may have a lower alkyl group having 1 to 3 carbon atoms, a lower alkoxy group having 1 to 3 carbon atoms or a halogen on the phenyl rings as a substituent; R1 stands for a lower alkylene group having 1 to 4 carbon atoms or a valency bond; L stands for a lower alkyl group having 1 to 3 carbon atoms; and Z stands for a carboxyl group or a group convertible to carboxyl group, are useful as, for example, remedies for hyperlipemia, diabetes and so on of mammals including human beings.
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