- 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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- ANTIFUNGAL COMPOUNDS AND PROCESSES FOR MAKING
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Provided are polymorphic forms of compound 5 or 5*, or mixtures thereof, and polymorph forms of compound 14 or 14*, or mixtures thereof. Also provided are methods of preparing compound 5 or 5*, or mixtures thereof, and methods of preparing compound of 14 or 14*, or mixtures thereof, which are useful as antifungal agents. In particular, provided is new methodology for preparing polymorphs of the compounds described and substituted derivatives thereof.
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Page/Page column 32; 33
(2017/04/11)
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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 80; 81
(2017/07/31)
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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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Page/Page column 69
(2016/01/29)
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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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Page/Page column 56
(2015/11/11)
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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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Page/Page column 53; 54
(2015/11/10)
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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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Page/Page column 38
(2015/11/10)
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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 or la and substituted derivatives thereof.
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Page/Page column 51; 56
(2016/01/28)
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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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Page/Page column 82; 88; 89
(2015/11/10)
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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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Page/Page column 73; 74; 75
(2015/11/10)
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- 2-(2,4-DIFLUOROPHENYL)-1,1-DIFLUORO-1-(5-SUBSTITUTED-PYRIDIN-2-YL)-3-(1H-TETRAZOL-1-YL)PROPAN-2-OLS AND PROCESSES FOR THEIR PREPARATION
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Provided herein are 2-(2,4-difluorophenyl)-1,1-difluoro-1-(5-substituted-pyridin-2- yl)-3-(1H-tetrazol-1-yl)propan-2-ols and 1-(2,4-difluorophenyl)-2,2-difluoro-2-(5-substituted-pyridin-2-yl)ethanones and processes for their preparation.
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Page/Page column 21; 22
(2015/11/10)
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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 87; 88
(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. Living organisms have developed tightly regulated processes that specifica
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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 48-50
(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 48
(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 58
(2013/07/05)
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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 51
(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 34-35
(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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