- Application of piperazine structure containing compound to preparation of LSD1 (Lysine Specific Demethylase 1) inhibitor
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The invention discloses application of a piperazine structure containing compound to the preparation of a histone lysine specific demethylase (LSD1) inhibitor. The structural general formula of the compound is as shown in the following descriptions (wherein, A is hydrogen, carbonyl or thiocarbonyl) or a configurational isomer and a pharmaceutical salt thereof, or is as shown in the following descriptions or a pharmaceutical salt thereof. The compound has an obvious inhibition effect on the LSD1, can be prepared into the LSD1 inhibitor, and is used for preventing and treating a disease related to the activity of the histone LSD1.
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Paragraph 0020
(2017/09/29)
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- METHOD FOR SPECIFIC CLEAVAGE OF C Alpha-C BOND AND SIDE CHAIN OF PROTEIN AND PEPTIDE, AND METHOD FOR DETERMINING AMINO ACID SEQUENCE
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The present invention provides a method for specifically cleaving a Cα-C bond of a peptide backbone and/or a side chain of a protein and a peptide, and a method for determining amino acid sequences of protein and peptide. A method for specifically cleaving a Cα-C bond of a peptide backbone and/or a side chain bond of a protein or a peptide, comprising irradiating a protein or a peptide with laser light in the presence of at least one hydroxynitrobenzoic acid selected from the group consisting of 3-hydroxy-2-nitrobenzoic acid, 4-hydroxy-3-nitrobenzoic acid, 5-hydroxy-2-nitrobenzoic acid, 3-hydroxy-5-nitrobenzoic acid, and 4-hydroxy-2-nitrobenzoic acid. A method for determining an amino acid sequence of a protein or a peptide, comprising irradiating a protein or a peptide with laser light in the presence of the above specific hydroxynitrobenzoic acid to specifically cleave a Cα-C bond of a peptide backbone and/or a side chain bond, and analyzing generated fragment ions by mass spectrometry.
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- Amyl nitrite-mediated conversion of aromatic and heteroaromatic primary amides to carboxylic acids
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A series of aromatic and heteroaromatic primary amides were converted directly to carboxylic acids by heating with amyl nitrite in acetic acid. Most conversions proceeded to give reasonable to excellent yields on a range of substrates containing various functional groups. This reagent system is thus applicable for the direct hydrolysis of a range of different primary carboxamides. The reaction with a phenolic aromatic substrate afforded two alternative nitration products as major outcomes, evidencing alternative reaction pathways resulting from the free phenolic OH.
- Potter, Garrett T.,Jayson, Gordon C.,Miller, Gavin J.,Gardiner, John M.
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supporting information
p. 5153 - 5156
(2015/08/19)
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- ORGANIC COMPOUNDS
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The present invention relates to quinazolinone compounds of the formula wherein R2, R3, R5, R6 R7 and R8 are as defined in the specification and in the claims, in free form or in salt form , processes for their preparation and their use as pharmaceuticals, particularly in the treatment of disorders ameliorated by administration of TRPV1 antagonists.
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Page/Page column 56-57
(2008/06/13)
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- Substituted aryloximes
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The present invention relates to substituted aryl oximes and methods of using them.
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Page/Page column 24
(2010/02/11)
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- Inhibitors of serine proteases, particularly HCV NS3 protease
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The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be
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