720662-57-7Relevant academic research and scientific papers
MRGPRX2 ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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Paragraph 00115; 00192, (2021/05/15)
The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pha
2-(2-Oxo-morpholin-3-yl)-acetamide derivatives as broad-spectrum antifungal agents
Bardiot, Dorothée,Thevissen, Karin,De Brucker, Katrijn,Peeters, Annelies,Cos, Paul,Taborda, Carlos P.,McNaughton, Michael,Maes, Louis,Chaltin, Patrick,Cammue, Bruno P. A.,Marchand, Arnaud
supporting information, p. 1502 - 1512 (2015/03/04)
From a fungicidal screen, we identified 2-(2-oxo-morpholin-3-yl)-acetamide derivatives as fungicidal agents against Candida species, additionally characterized by antifungal activity against Aspergillus species. However, development of this series was hampered by low plasmatic stability. Introduction of a gem-dimethyl on the 6-position of the morpholin-2-one core led to considerable improvement in plasmatic stability while maintaining in vitro antifungal activity. Further optimization of the series resulted in the discovery of N-(biphenyl-3-ylmethyl)-2-(4-ethyl-6,6-dimethyl-2-oxomorpholin-3-yl)acetamide (87), which, in addition to fungicidal activity against Candida species, shows promising and broad antifungal in vitro activity against various fungi species, such as molds and dermatophytes. In vivo efficacy was also demonstrated in a murine model of systemic Candida albicans infection with a significant fungal load reduction in kidneys.
ANTIFUNGAL COMPOUNDS
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Page/Page column 37, (2012/10/08)
The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.
ANTIFUNGAL COMPOUNDS
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Page/Page column 70, (2011/07/07)
The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.
