48 results about "MAO inhibitors" patented technology

A mechanism of monoamine oxidases (MAOs) driven epithelium-to-mesenchymal transition (EMT) is disclosed. Also disclosed are methods for treating cancer by inhibiting or suppressing MAOs in cancer cells. Novel MAOs inhibitors, such as small molecules, siRNA, shRNA, antisense oligonucleotides, aptamers, decoys, and pharmaceutical compositions useful for treating cancer by disrupting the workings of MAOs are provided. In particular, a class of conjugates formed by covalently conjugating near infrared dye 783, IR-780, and MHI-148 to a MAO inhibitor, such as clorgyline, with and without encapsulation it in a nanoparticle is provided. Other aspects of the invention include methods for forming the nano-conjugates, method for monitoring treatment progress in a cancer patient by monitoring the changes in MAO activity, methods for screening patients who are at risk of cancer or differentiating different forms of cancer by assaying the level and location of MAO activity.

One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group consisting of D-1 agonists, D-2 agonists, D-3 agonists, D-4 agonists, irreversible monoamine inhibitors, reversible monoamine inhibitors, monoamine transporter inhibitors, COMT inhibitors, MAO inhibitors, and dopamine transporter inhibitors. Moreover, the present invention also relates to combinatorial libraries of polypharmacophoric compounds. Another aspect of the present invention relates to the use of a polypharmacophoric compound in a method of treating a mammal in need thereof. For example, a polypharmacophoric compound of the present invention may be used in a method of treating a mammal afflicted with Alzheimer's Disease, Huntington's Disease, depression, attention deficit disorder, autism, obesity, or inflammation.

The invention provides use of propargyl imine compounds in the preparation of a monoamine oxidase inhibitor and new propargyl imine compounds. The propargyl imine compounds have a structural formula (I). The invention has the advantages that: (1) equipment required for the preparation of the propargyl imine compounds is simple, the operation process is simple and convenient, the raw material sources are commercialized and readily available and the compounds serving as the monoamine oxidase inhibitor are stable in nature and high in purity (over 99 percent); and (2) compared with the traditional monoamine oxidase inhibitor, the monoamine oxidase inhibitor prepared from the new propargyl imine compounds has a simpler structure, a higher inhibition activity, higher MAO-A selectivity and higher MAO-B selectivity.

A pharmaceutical composition and method for treating brain cancer are provided. The method includes administering to a patient in need thereof an effective amount of one or more compounds that include moclobemide, clorgyline, clorgyline's Near-infra-red dye Monoamine Oxidase Inhibitor (NMI), and MHI 148- clorgyline, and their salt thereof. The composition and method are particularly effective in reducing the size of glioblastomas that are temozolomide (TMZ) resistant.

The invention discloses a purpose of a coumarin compound shown as a general formula (I) in preparation of a monoamine oxidase inhibitor, which belongs to the technical field of a medicine. Through in-vitro enzyme activity tests, the compound has good inhibition activity for monoamine oxidases A and B, and provides reference and novel thinking for developing the novel MAO inhibitor.

The invention provides application of a traditional Chinese medicine composition to preparation of a monoamine oxidase (MAO) inhibitor. The traditional Chinese medicine composition is prepared from 20 parts of delavay raspberry, 18 parts of galium verum, 12 parts of blumea balsamifera roots, 15 parts of wintersweet roots or stems and 10 parts of roots of multibract raspberry. Compared with the conventional monoamine oxidase MAO inhibitor, the monoamine oxidase MAO inhibitor provided by the invention has the advantages that the inhibitory activity and the selectivity on MAO-A and MAO-B of the monoamine oxidase MAO inhibitor are both greatly improved, that is, a great improvement is achieved.

The invention provides application of Norsampsone B in preparing a MAO (monoamine oxidase) inhibitor, compared with the existing MAO inhibitor, the inhibitory activity and the selectivity of MAO-A and MAO-B of the Norsampsone B are greatly improved. The application of the Norsampsone B in preparing the MAO inhibitor is disclosed for the first time, and the inhibitory activity to the MAO is high, the Norsampsone B has outstanding substantive features, and obviously has remarkable improvement for treating diseases relevant to imbalance of the MAO at the same time.

The invention provides application of Kadcoccitones A in preparing a monoamine oxidase (MAO) inhibitor. Compared with the existing MAO inhibitor, the Kadcoccitones A has greatly higher activity and selectivity for MAO-A and MAO-B. The application of the Kadcoccitones A in preparing the MAO inhibitor is disclosed for the first time; and the Kadcoccitones A has high activity for inhibiting MAO, has the characteristic of outstanding materiality, and apparently has marked progresses when being used for treating MAO maladjustment related diseases.

The invention provides the application of Lathyranone A. in the preparation of monoamine oxidase (MAO) inhibitors. Compared with the existing monoamine oxidase inhibitors, its inhibitory activity and selectivity to MAO‑A and MAO‑B are greatly improved. The use of Lathyranone A. involved in the present invention in the preparation of monoamine oxidase (MAO) inhibitors is disclosed for the first time. Since the skeleton type belongs to a new skeleton type, and its inhibitory activity against monoamine oxidase is unexpectedly strong, there is no inspiration from other compounds It is possible, has outstanding substantive features, and at the same time, it is obviously a significant progress in the treatment of diseases related to monoamine oxidase disorders.

The invention provides application of Gypensapogenin B to preparation of a MAO (monoamine oxidase) inhibitor. Compared with the existing MAO inhibitor, the MAO inhibitor provided by the invention has greatly improved inhibitory activity and selectivity on MAO-A and MAO-B. The application of Gypensapogenin B to preparation of the MAO inhibitor is firstly publicized; and as a framework type belongs to a brand-new framework type, the framework type has unexpectedly strong inhibitory activity on the MAO inhibitor without any possibility shown by other compounds, and has outstanding substantial characteristics and remarkable progress for treating the diseases related to MAO unbalance at the same time.

The invention provides application of ieodoglucomides B to prepare a monoamine oxidase (MAO) inhibitor, and compared with a known monoamine oxidase inhibitor, the monoamine oxidase (MAO) inhibitor is greatly improved in inhibition activity and selectivity on MAO-A and MAO-B. The related purpose of ieodoglucomides B to prepare the monoamine oxidase (MAO) inhibitor is disclosed for the first time. Because the l type belongs to a brand-new framework type and the inhibition activity of the inhibitor on monoamine oxidase (MAO) is unexpected, there is not the possibility that other compounds give any enlightenment, the technical scheme possesses prominent substantive features, and also treatment on monoamine oxidase (MAO) imbalance related diseases obviously possesses notable progress.

The invention relates to a novel use of Daphnilongeranin A in preparation of a monoamine oxidase (MAO) inhibitor. Compared with the exciting monoamine oxidase inhibitor, the Daphnilongeranin A has higher inhibition activity and MAO-A and MAO-B selectivity. The use of Alistonitrine A in preparation of a MAO inhibitor is disclosed first. The skeleton type of the Daphnilongeranin A belongs a novel skeleton type, the Daphnilongeranin A has unexpected monoamine oxidase inhibition activity, is free of any enlightenment provided by other compounds and has prominent substantive features, and the use of Daphnilongeranin A in treatment on monoamine oxidase disorder-related diseases has substantial progress.