- Fungal lanosterol 14α-demethylase (CYP51) inhibitor Treatment of recurrent vulvovaginal candidiasis Treatment of onychomycosis
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Developing a rationally designed, more selective azole antifungal agent that specifically targets the fungal CYP51 over the host CYP51 is a severe unmet need considering a massive shortfall in novel antifungal agents. In this context, oteseconazole (VT-1161) represents a very exciting new development targeting serious fungal infections caused by a wide variety of fungal pathogens including multidrug-resistant Candida responsible for recurrent vulvovaginal candidiasis. This monograph details the various in vitro and in vivo properties exhibited by oteseconazole as well as its current status in clinical trials.
- Chopra, S.,Dasgupta, A.,Thakare, R.
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p. 855 - 868
(2020/01/21)
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- Deuterated azole alcohol compound, preparation method and uses thereof
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The present invention discloses a deuterated azole alcohol compound represented by a formula (I), and a pharmaceutically acceptable salt thereof, a preparation method and uses thereof, and a prodrug.According to the present invention, the deuterated azole alcohol compound has good antifungal activity and good metabolic stability, and can be used for preparing antifungal drugs. The formula (I) isdefined in the specification.
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Paragraph 0077-0079
(2019/05/02)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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- ANTIFUNGAL COMPOUND PROCESS
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The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
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- ANTIFUNGAL COMPOUND PROCESS
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The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
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- Design and optimization of highly-selective fungal CYP51 inhibitors
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While the orally-active azoles such as voriconazole and itraconazole are effective antifungal agents, they potently inhibit a broad range of off-target human cytochrome P450 enzymes (CYPs) leading to various safety issues (e.g., drug-drug interactions, li
- Hoekstra, William J.,Garvey, Edward P.,Moore, William R.,Rafferty, Stephen W.,Yates, Christopher M.,Schotzinger, Robert J.
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p. 3455 - 3458
(2014/07/22)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 90; 91
(2015/01/09)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 59
(2013/07/05)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The present disclosure describes compounds having agricultural fungicidal activity.
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Page/Page column 35
(2013/07/31)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 33
(2013/07/31)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 21
(2013/02/28)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 52
(2013/02/28)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 35
(2011/11/06)
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- New antifungal 1,2,4-triazoles with difluoro(heteroaryl)methyl moiety
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New 1,2,4-triazoles (1) having a difluoro(heteroaryl)methyl moiety were designed and synthesized via 1-aryl-2,2-difluoro-2- (heteroaryl)ethanones (2), which were prepared by two routes starting from the reaction of ethyl 2,2- difluoro(heteroaryl)acetate with phenyllithiums (Route A) and from the reaction of chlorodifluoro(heteroaryl)methane with benzaldehydes (Route B). The compounds 1 except for 1g show antifungal activities against yeasts and filamentous fungi in vitro, especially (+)-If have equal or superior activities compared to those of itraconazole.
- Eto, Hiromichi,Kaneko, Yasushi,Sakamoto, Takao
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p. 982 - 990
(2007/10/03)
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