- HYDROXAMATE DERIVATIVES FOR HDAC INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THEREOF
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The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.
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- HYDROXAMATE DERIVATIVES FOR HDAC INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THEREOF
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The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.
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- Synthesis of 2-aminoindole derivatives with Hantzsch ester catalyzed by Pd/C
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Catalytic hydrogenation of 2-cyano-2-(2-nitrophenyl)acetates bearing an electron withdrawing substituent to the nitrile, using Hantzsch ester catalyzed by Pd/C, affords 2-aminoindoles in good to excellent yields. Copyright
- Xing, Ruiguang,Tian, Qiuping,Liu, Qiang,Li, Yanan
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p. 263 - 266
(2013/08/24)
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- Synthesis and antiviral activity of 4,6-disubstituted pyrimido[4,5-b]indole ribonucleosides
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A series of new pyrimido[4,5-b]indole ribonucleosides bearing phenyl or hetaryl group at position 4 has been prepared by selective Pd-catalyzed cross-coupling reactions of the corresponding protected 4,6-dichloropyrimido[4, 5-b]indole ribonucleoside with (het)arylboronic acids or stannanes followed by deprotection. Further cross-couplings under harsher conditions and employing X-Phos ligand proceeded at the position 6 leading to 4,6-disubstituted pyrimido[4,5-b]indole ribonucleosides. Some of these compounds displayed antiviral activity against Dengue virus.
- Tichy, Michal,Pohl, Radek,Hocek, Michal,Xu, Hao Ying,Chen, Yen-Liang,Yokokawa, Fumiaki,Shi, Pei-Yong
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p. 6123 - 6133,11
(2020/08/20)
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- Synthesis of 2-aminoindole-3-carboxylic acid derivatives by the copper(I) iodide catalyzed reaction of N -(2-iodophenyl)formamides with malononitrile or cyanoacetates
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An efficient method for the synthesis of 2-aminoindole-3-carbonitriles and 2-aminoindole-3-carboxylates by the reaction of N-(2-iodophenyl)formamides with malononitrile and cyanoacetates, respectively, in the presence of a catalytic amount of copper(I) io
- Kobayashi, Kazuhiro,Komatsu, Toshihide,Yokoi, Yuki,Konishi, Hisatoshi
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experimental part
p. 764 - 768
(2011/04/25)
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- A simple copper-catalyzed cascade synthesis of 2-amino-1H-indole-3- carboxylate derivatives
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We have developed a simple and efficient copper-catalyzed method for the synthesis of 2-amino-1H-indole-3-carboxylate derivatives via cas-cade reactions of substituted N-(2-halophenyl)-2, 2, 2-trifluoroacetamide with alkyl 2-cyanoacetate or malononitrile under mild conditions, and the method is of wide practical application.
- Yang, Xiaobo,Fu, Hua,Qiao, Renzhong,Jiang, Yuyang,Zhao, Yufen
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supporting information; experimental part
p. 1035 - 1038
(2010/09/05)
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- Synthesis and reactivity of N-hydroxy-2-aminoindoles
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Catalytic hydrogenation of (2-nitrophenyl)acetonitriles bearing an electron-withdrawing substituent α to the nitrile, using Pd/C and (Ph 3P)4Pd, affords N-hydroxy-2-aminoindoles in good to excellent yields. (Ph3P)4Pd decreases the reduction rate of the intermediate hydroxylamine and acts as a catalyst during the cyclization onto the nitrile.
- Belley, Michel,Sauer, Effiette,Beaudoin, Daniel,Duspara, Petar,Trimble, Laird A.,Dubé, Pascal
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p. 159 - 162
(2007/10/03)
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