- Double - (to - alkoxybenzyl propenone) glutathione - S - transfers the sulfur of the enzyme dives inhibitors
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The invention discloses a bis-(p-alkoxy benzene acrylketone) like glutathione-S-transferase potential inhibitor. Structure and living features of the potential inhibitor are as follows: two p-alkoxy benzene acrylketone units are linked to two amino groups, alcoholic hydroxyl groups and carboxyl groups or one amino group and one alcoholic hydroxyl group which are spaced by less than 8 single bonds through amide and/or ester bond, wherein compounds obtained are substrate and inhibitor of glutathione-S-transferase, namely GST; the GST catalyzes carbon-carbon bond and reduced glutathione, namely GSH, of alpha, beta-unsaturated ketone of each p-alkoxy benzene acrylketone unit in the compounds and generates a compound, namely product, through Michael addition. The product shows a stronger inhibiting efficacy on the GST, so that the compound is a GST potential inhibitor; the product has a stronger inhibiting efficacy on human GST isozyme mu in comparison with human GST isozyme alpha and pi; and the compounds can enter into cells, and can enhance inhibiting effect of cis-platinum on drug-resistant carcinoma cell growth.
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Paragraph 0080-0083
(2020/05/08)
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- Process for lowering the viscosity of highly concentrated protein solutions
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A process of lowering the viscosity of a solution includes preparing a solution comprising a compound of formula I, at a concentration in the final formulation of between 10 and 250 mM, and a protein having at least one antibody fragment whose concentration is between 50 and 350 mg/mL and whose pH is between 5 and 8. The compound lowers the viscosity of the solution, which is difficult to inject, by a value of at least 15% relative to the viscosity of a solution of at least one protein having at least one antibody fragment of the same concentration and of the same pH not containing the compound.
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Paragraph 0369
(2014/03/21)
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- THIAZOLE DERIVATIVES AS STEAROYL COA DESATURASE INHIBITORS
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The present invention provides thiazole derivatives as Stearoyl CoA Desaturase (SCD) inhibitors. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase
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Page/Page column 35
(2010/04/03)
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