40 results about "Monoamine Oxidase Type B" patented technology

The invention provides a compound of formula I:wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.

The present invention provides an ex vivo method for aiding the diagnosis of Alzheimer's disease in a patient, the method comprising the steps of determining the level of expression of at least four platelet proteins in a platelet sample from the patient selected from monoamine oxidase-B, coagulation factor Xllla, total tropomyosin (a and 13), WD-repeat protein 1 and apolipoprotein E4; and comparing the result of (i) to a control value, wherein a result higher than the control value is indicative of Alzheimer's disease. Preferably, the method of the invention further comprises determining the level of expression of wild-type GSTO-1 or mutant GSTO-1.

The invention discloses coumarin / pyridone heterozygous derivatives represented by a formula (I) shown in the description or a pharmaceutically-acceptable salt of the derivatives. The preparation method of the coumarin / pyridone heterozygous derivatives comprises the following steps: one pyridone derivative represented by a formula 3 shown in the description is obtained by a series of synthesis by using one hydroxypyrone with different substituent groups represented by a formula 1 shown in the description as a raw material; and a compound represented by a formula 4 shown in the description is subjected to a condensation reaction to obtain a compound represented by a formula 5 shown in the description, one-step bromination is performed to obtain a compound represented by a formula 6 shown inthe description, the compound represented by the formula 6 and the pyridone derivative represented by the formula 3 are subjected to a one-step nucleophilic substitution reaction to obtain a compoundrepresented by a formula 7 shown in the description, and finally an alkyl protecting group in a pyridone structure is removed to obtain one target compound represented by the formula (I). The compounds provided by the invention are a novel series of single-molecular multi-target series drugs, and have iron chelation, targeted MAO-B inhibitory activity, antioxidant activity, unique advantages for an Alzheimer disease with complicated pathogenesis, a clear mechanism of action and excellent activity.

The present invention relates to uses of 5-(3,4-methylenedioxy phenyl)-2E,4E pentadienoic acid propylamine amide in preparation of medicinal compositions for treatment and / or prevention of neuron diseases requiring neuroprotection effects and / or nerve regeneration. The 5-(3,4-methylenedioxy phenyl)-2E,4E pentadienoic acid propylamine amide provides good treatment effects for depressions caused by various causes, provides significant anti-depression activity for a pharmacological depression model, provides a good protection effect for SH-SY5Y cells damaged by glutamic acid, and provides a selective inhibition effect for monoamine oxidase B (MAO-B).

The invention discloses a diarylethene compound as well as a medicine composition and application thereof and relates to the technical field of medicines. The invention provides the diarylethene compound, and the structural formula (I) of the diarylethene compound is shown in the specification. The diarylethene compound disclosed by the invention has a remarkable monoamine oxidase B (MAO-B) inhibition function, and can be used for preparing monoamine oxidase inhibitors B and Parkinson's disease prevention medicines. The invention further provides the medicine composition with the diarylethenecompound as an active component. The medicine composition can be used as a monoamine oxidase B (MAO-B) inhibitor and a Parkinson's disease treatment medicine. In addition, the diarylethene compound disclosed by the invention is novel in structure, easy in chemical synthesis, low in cost and small in side effect.

The invention provides a diarylethene type compound, a medicine composition using the diarylethene type compound as an active ingredient and application of the diarylethene type compound in preparation of a MAO-B (Monoamine Oxidase B) inhibitor and preparation of PD (Parkinson's Disease) treatment medicine. The MAO-B is proved to have close relationship with the PD pathogenesis and is a classic target for PD medicine development. The diarylethene type compound provided by the invention can be used for preparing the MAO-B inhibitor. In vitro kinase activity experiments prove that the series ofcompounds have the obvious MAO-B inhibition effect.

The present invention relates to uses of 5-(3,4-methylenedioxy phenyl)-2E,4E pentadienoic acid propylamine amide in preparation of medicinal compositions for treatment and / or prevention of neuron diseases requiring neuroprotection effects and / or nerve regeneration. The 5-(3,4-methylenedioxy phenyl)-2E,4E pentadienoic acid propylamine amide provides good treatment effects for depressions caused by various causes, provides significant anti-depression activity for a pharmacological depression model, provides a good protection effect for SH-SY5Y cells damaged by glutamic acid, and provides a selective inhibition effect for monoamine oxidase B (MAO-B).

The invention discloses a preparation method and application of a two-photon ratio fluorescent probe for accurately measuring monoamine oxidase B in tumor cells. Based on the mechanism of fluorescence resonance energy transfer, the probe uses enzymatic oxidative deamination reaction to generate corresponding iminium ions, which are eliminated after hydrolysis and re-release hydroxyl groups, resulting in proportional changes in fluorescence emission signals. The advantage is that the fluorescent spectrum distance between the energy donor and the acceptor is larger, the interference between the spectra is smaller, and the sensitivity is higher, effectively avoiding the interference of various environmental conditions on the analysis. It provides a potential tool for clinical detection of important marker enzymes of Alzheimer's disease in vivo.

The invention discloses an amine alkoxychalcone compound and its preparation method and use, comprising the following steps: (1) using 3-hydroxybenzaldehyde as a starting material, under a first solvent and a first basic condition , react with dibromo compound to obtain bromoalkoxybenzaldehyde; (2) bromoalkoxybenzaldehyde reacts with secondary amine under the second solvent and the second basic condition to obtain amine alkoxybenzaldehyde; (3 ) amine alkoxy benzaldehyde and 2-hydroxyacetophenone under the third solvent and the third basic condition, obtain the target compound amine alkoxy chalcone compound. The compound of the present invention has selective butyrylcholinesterase inhibitory activity, selective monoamine oxidase B inhibitory activity, selective metal ion chelation activity, and Aβ aggregation inhibitory activity in vitro, and can be used for treating and / or preventing neurodegenerative related diseases.

The present invention provides an ex vivo method for aiding the diagnosis of Alzheimer's disease in a patient comprising: (i) determining the number of alleles of ApoE4 in the patient's genome; (ii) determining the combined expression level of at least three platelet proteins in a platelet sample from the patient; and (iii) comparing the resulting value of step (ii) to a control value, wherein the at least three platelet proteins include at least one isoform of alpha-tropomyosin containing exon 1a and at least two platelet proteins selected from monoamine oxidase-B, coagulation factor XIIIa, wild-type GSTO-1 or mutant GSTO-1, wherein a result higher than the control value is indicative of Alzheimer's disease.The invention also provides a solid support comprising one or more ligands of at least one isoform of alpha-tropomyosin containing exon 1a, and one or more ligands of at least two platelet proteins selected from monoamine oxidase-B, coagulation factor XIIIa, wild-type GSTO-1 protein and / or mutant GSTO-1 protein immobilized thereon.

The invention discloses the application of a triazine compound shown as a structural formula (I) in the preparation of a monoamine oxidase inhibitor. Through in vitro enzyme activity experimental measurement, the compound has good inhibitory activity for monoamine oxidase-B, so that reference is provided for developing a novel MAO inhibitor, and a new thought is inspired.