6 results about "Nitroethylene" patented technology

The present in vention is directed to methods of treating a metabolic disorder in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a nitro-vinyl benzene compound and administering to the subject a therapeutically effective amount of a GLP-1 agonist or analog. The present invention is also directed to kits and / or pharmaceutical compositions suitable for practicing the claimed methods.

The application discloses a 2-((naphthalene-2-ylmethyl)amino)acetamide compound or a pharmaceutically acceptable salt thereof with a structure as shown in formula I: wherein R 1 is H or CH3; R 2 is H or CH3; X is O, S or NH; A ring is 3-6-membered cycloalkyl, 4-6-membered heterocyclyl, aryl or heteroaryl; R 3 is H, halogen, methyl, trifluoromethyl, methoxy, cyano, nitro, vinyl or ethynyl. The compound of the application has good reversible inhibitory effect on MAOs, especially, the MAO-B inhibitory activity is significantly better than that of the third generation MAO-B inhibitor safinamide, and has reversible inhibitory effect on MAO-B, and can be used for treating neurodegenerative diseases such as Parkinson's disease and Alzheimer's disease.

The invention discloses a method for detecting related substances in N-methyl-1-methylthio-2-nitrovinylamine. The method comprises the following steps: (1) preparing a test solution; (2) preparing a contrast solution; (3) chromatographic detection, wherein chromatographic analysis conditions are as follows: octadecylsilane chemically bonded silica is adopted as a chromatographic column of a filler; carrying out gradient elution by using the mobile phase A and the mobile phase B; and the detection wavelength is 352 nm. According to the present invention, the efficient and accurate high performance liquid chromatography is adopted to perform determination, the impurity separation ability is significantly improved through the optimized gradient elution program and the design of the detection wavelength, the accurate quantification of the related substance is achieved by using the self-contrast method, and the method has advantages of strong specificity, high sensitivity, simple operation and good reproducibility.

The application discloses a preparation method of a monoamine oxidase B inhibitor, and comprises the following steps: 6-fluoroindole and 1-(dimethylamino)-2-nitroethylene are subjected to trifluoroacetic acid catalysis to generate 6-fluoro-3-[(E)-2-nitrovinyl]-1H-indole, and then subjected to sodium borohydride and iron powder / hydrochloric acid reduction to generate 6-fluoro-tryptamine; under an acidic condition, Pictet-Spengler reaction is carried out between 6-fluoro-tryptamine and ethyl glyoxylate to generate ethyl 7-fluoro-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-1-carboxylate and 7-fluoro-4,9-dihydro-3H-pyrido[3,4-b]indole-1-carboxylate, and then subjected to oxidative dehydrogenation aromatization reaction to generate ethyl 7-fluoro-9H-pyrido[3,4-b]indole-1-carboxylate; under the catalysis of aluminum trichloride, amine ester exchange reaction is carried out between ethyl 7-fluoro-9H-pyrido[3,4-b]indole-1-carboxylate and 3-fluorobenzylamine to generate a target compound. The method has high overall yield.

The present application provides the use of aromatic nitroethylenes, in particular, the present application provides the use of a compound represented by formula (I), a stereoisomer or a pharmaceutically acceptable salt thereof for preparing a medicament for modulating the dimer activity of nuclear receptor RXR or treating neurodegenerative diseases.