- SMALL MOLECULE STIMULATORS OF THE CORE PARTICLE OF THE PROTEASOME
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This present disclosure relates to series compounds and methods of use for the treatment of a disease caused by abnormal regulation of the ubiquitin-proteasome system (UPS), and wherein said compound is an effective stimulator of the 20S core particle (CP) of the UPS. Composition matters and methods of uses are within the scope of this disclosure.
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Paragraph 00101
(2021/02/26)
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- Use of miconazole and derivatives thereof as TGR5 agonists (by machine translation)
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The invention belongs to the technical field of medicines, and relates to novel application TGR5 of miconazole and derivatives thereof in treatment, of diseases and conditions of a biological pathologic process involved in treatment, and. The miconazole and the analogues thereof can activate TGR5 active, for use TGR5 in the treatment or prevention of diseases associated with, activity modulation. (by machine translation)
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Paragraph 0031; 0036; 0037-0040
(2020/05/02)
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- Anti-staphylococcal biofilm activity of miconazoctylium bromide
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We designed and synthesized miconazole analogues containing a substituted imidazolium moiety. The structural modification of the miconazole led to a compound with high potency to prevent the formation and disrupt bacterial biofilms, as a result of accumulation in the biofilm matrix, permeabilization of the bacterial membrane and generation of reactive oxygen species in the cytoplasm.
- Tessier, Jérémie,Golmohamadi, Mahmood,Wilkinson, Kevin J.,Schmitzer, Andreea R.
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p. 4288 - 4294
(2018/06/22)
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- METHOD FOR PRODUCING PULVERIZED ORGANIC COMPOUND PARTICLE
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Disclosed is a method for producing pulverized particles of a crystalline organic compound which is poorly water-soluble. Also disclosed is a pulverized organic compound particle produced by such a method. Specifically disclosed is a method for producing a poorly water-soluble organic compound particle for medical use, which is characterized in that a poorly water-soluble organic compound for medical use is mixed with a physiologically acceptable salt and a physiologically acceptable polyol, and subjected to wet milling. Also specifically disclosed is a poorly water-soluble organic compound particle for medical use, which is produced by such a production method.
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