- HISTONE ACETYLTRANSFERASE (HAT) INHIBITOR AND USE THEREOF
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The present invention relates to a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof in the treatment of various HAT-related diseases or conditions.
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Paragraph 0043-0044
(2021/02/25)
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- IDH1 mutant micromolecule inhibitor, and preparation method and application thereof
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The invention discloses an IDH1 mutant micromolecule inhibitor, and a preparation method and application thereof. The structure of the inhibitor is as shown in a formula I, and the definition of the substituent groups is as described in the specification
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Paragraph 0271-0272; 0275
(2019/07/16)
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- PYRIDINES AND PYRIMIDINES AND USE THEREOF
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The present disclosure provides pyridines and pyrimidines of Formula I and pharmaceutically acceptable salts and solvates thereof: wherein A, G, W1, W2, W3, and R5 are defined as set forth in the specification. The present disclosure also provides uses of the compounds of Formula I and pharmaceutically acceptable salts and solvates thereof. In certain embodiments, Compounds of the present disclosure are useful for treating pain. In another embodiment, Compounds of the present disclosure are useful for treating a disorder responsive to blockade of sodium channels, or alleviating symptoms of the disorder.
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Paragraph 0281; 0282
(2017/01/31)
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- Synthesis of 4,4′-Disubstituted and Spiro-tetrahydroquinolines via Photochemical Cyclization of Acrylanilides and the First Synthesis of (±)- trans -Vabicaserin
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The synthesis of vabicaserin analogues bearing a quaternary center or spiro substitution at the 4-position has been studied via a [6π]-acrylanilide cyclization employing flow photochemistry in a mesoscale and microfluidic flow photoreactor. The method is also used to synthesize 4,4′-disubstituted tetrahydroquinolines and, furthermore, enables the first synthesis of (±)-trans-vabicaserin.
- Koolman, Hannes F.,Braje, Wilfried M.,Haupt, Andreas
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p. 2561 - 2566
(2016/11/11)
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- PYRIDINES AND PYRIMIDINES AND USE THEREOF
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The present disclosure provides pyridines and pyrimidines of Formula I and pharmaceutically acceptable salts and solvates thereof: wherein A, G, W1, W2, W3, and R5 are defined as set forth in the specification. The present disclosure also provides uses of the compounds of Formula I and pharmaceutically acceptable salts and solvates thereof. In certain embodiments, Compounds of the present disclosure are useful for treating pain. In another embodiment, Compounds of the present disclosure are useful for treating a disorder responsive to blockade of sodium channels, or alleviating symptoms of the disorder.
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Page/Page column 71-72
(2015/08/06)
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- Benzene-fused heterocycle derivatives and drugs containing the same as the active ingredient
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A benzene-fused heteroring derivative of formula (I) 1, wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is
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- Inhibitors of farnesyl protein transferase
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The present invention comprises benzodiazepine compounds having farnesyl transferase inhibitory activity.
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- Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase
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2,3,4,5-Tetrahydro-1-(imidazol-4-ylalkyl)-1,4-benzodiazepines were found to be potent inhibitors of farnesyltransferase (FT). A hydrophobic substituent at the 4-position of the benzodiazepine, linked via a hydrogen bond acceptor, was important to enzyme i
- Ding, Charles Z.,Batorsky, Roberta,Bhide, Rajeev,Chao, Hannguang J.,Cho, Young,Chong, Saeho,Gullo-Brown, Johnni,Guo, Peng,Kim, Soong Hoon,Lee, Frank,Leftheris, Katerina,Miller, Arthur,Mitt, Toomas,Patel, Manorama,Penhallow, Becky A.,Ricca, Carol,Rose, William C.,Schmidt, Robert,Slusarchyk, William A.,Vite, Gregory,Yan, Ning,Manne, Veeraswamy,Hunt, John T.
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p. 5241 - 5253
(2007/10/03)
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