- NOVEL CATECHOL DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, USE OF THE CATECHOL DERIVATIVE AND USE OF THE PHARMACEUTICAL COMPOSITION
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The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
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Page/Page column 17
(2011/04/25)
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- NOVEL CATECHOL DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, USE OF THE CATECHOL DERIVATIVE, AND USE OF THE PHARMACEUTICAL COMPOSITION
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The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is halo-lower alkyl, lower acyl, halo-lower alkylcarbonyl, cycloalkylcarbonyl,optionallysubstituted arylcarbonyl,lower alkoxycarbonyl or the like; R4 is lower alkyl, halo-lower alkyl, cycloalkyl, lower alkoxy-lower alkyl or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
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Page/Page column 22
(2010/11/17)
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- On the Synthesis of 2,12-Dimethoxy-6,7,8,9-tetrahydro-5H-dibenzazonine-3,11-diol and Other Bridged Biphenyldiols and the E.S.R. of Their Oxidation Products in Relation to the Biosynthesis of Erythrina Alkaloids
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An improved synthesis in described for the dibenzazonine precursor of erysodienone.Other biphenyl-4,4'-diols, bridged by two, three and five atoms, were also prepared.E.s.r. examination of the oxidation of these compounds produced spectra of the 9,10-dihydrophenanthrene-4,4'-semiquinone system, hitherto unrecorded, but semiquinone spectra could not be obtained from the other diols.
- Hewgill, Frank R.,Pass, Michael C.
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p. 537 - 554
(2007/10/02)
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- Cleavage of the Methylenedioxy Ring. III. Cleavage with Sodium Benzyloxide in Dimethyl Sulfoxide
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Cleavage of the methylenedioxy ring in aromatic formyl (1-3), nitro (4 and 5), and acetyl (30) compounds with N-sodium benzyloxide-benzyl alcohol in dimethyl sulfoxide gave 3-hydroxybenzene derivatives (19, 22-24, 26, 27, and 33).In the case of the acetyl compound 30, the 4-hydroxybenzene derivative (34) was also obtained as a minor product.Regioselective cleavage of the ring in aromatic compounds having electronwithdrawing groups with nucleophilic oxide anions is discussed.Cleavage of the ring in 1-5 and 30 with 2 N sodium methoxide in dimethyl sulfoxide-dimethylformamide was found to be useful for the practical preparation of 3-hydroxybenzene derivatives (6-10 and 31).Keywords - Cleavage of methylenedioxy ring; regioselectivity; piperonals; 3,4-methylenedioxy-nitrobenzene; 3,4-methylenedioxy-acetophenone; sodium methoxide; sodium phenoxide; sodium benzyloxide; dimethyl sulfoxide; dimethylformamide
- Kobayashi, Shigeru,Okimoto, Kazuto,Imakura, Yasuhiro
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p. 1567 - 1573
(2007/10/02)
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