- Synthetic method of aromatic ring group or aromatic heterocyclic tetrazole
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The synthetic method comprises the following steps: (1) reacting 1.0 eq of ArI or HArI with 1.2 eq of ethyl 2, 2-difluoroacetate in the presence of DMSO as a solvent and 4.0 eq of Cu under the protection of nitrogen at 30 DEG C and 50 DEG C, and purifying to obtain a first intermediate compound; (2) dissolving 1.0 eq of the first intermediate compound in a mixed solvent of THF and water, adding 2.0 eq of LiOH, reacting at room temperature for 2 hours, spin-drying the solvent, adding HCl until the pH value is equal to 3, and filtering to obtain a second intermediate compound; and (3) reacting 1.0 eq of the second intermediate compound with 2.0 eq of diphenyl azide phosphate in the presence of 2.5 eq of triethylamine by taking tert-butyl alcohol as a solvent to generate aromatic ring group or aromatic heterocyclic tetrazole. The invention provides a novel synthetic method of aromatic ring group or aromatic heterocyclic tetrazole, wherein a target compound can be more conveniently obtained, and reagents participating in the reaction are low in toxicity, mild in reaction condition, simple and safe in aftertreatment, good in product quality and suitable for large-scale production.
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Paragraph 0036-0042; 0051
(2020/12/30)
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- 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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- 1,4-THIAZINE DIOXIDE AND 1,2,4-THIADIAZINE DIOXIDE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
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The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2', R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.
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Page/Page column 74; 73
(2018/07/05)
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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 79; 80
(2017/07/31)
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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 31; 32
(2017/04/11)
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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 55; 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 52; 53
(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 82; 85; 86
(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 70; 71; 72
(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 37
(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 49; 55; 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 67; 68
(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 57; 58
(2015/11/10)
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- Manufacturing method of making heteroarylacetic compd. defluoromethyl
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PROBLEM TO BE SOLVED: To provide a method for easily producing a difluoromethyl heteroaryl compound with high yield at low cost. SOLUTION: In the method for producing the difluoro methyl heteroaryl compound, a halogenated heteroaryl compound and a α-silyldifluoro acetate ester compound are reacted with each other in the presence of a metal halogenated compound. COPYRIGHT: (C)2012,JPOandINPIT
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Paragraph 0074-0076; 0078-0080
(2018/10/03)
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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
-
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 9; 10; 11
(2015/11/10)
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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
(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 58
(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 34
(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
-
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 20-21
(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
(2011/11/06)
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- 4 ( 1H) -PYRIDINONE DERIVATIVES AND THEIR USE AS ANTIMALARIA AGENTS
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4-pyridone (4-pyridinone) derivatives of Formula (I) and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
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Page/Page column 66-67
(2010/08/08)
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- OPHTHALMIC COMPOSITIONS FOR TREATING OCULAR HYPERTENSION
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This invention relates to potent potassium channel blocker compounds of structural Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
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Page/Page column 20
(2008/06/13)
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- Ophthalmic compositions for treating ocular hypertension
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This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relate
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- Copper-mediated reaction of 2-halopyridines with ethyl bromodifluoroacetate
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A facile process for the preparation of substituted ethyl 2′-pyridyldifluoroacetates 3 is described starting from readily available ethyl bromodifluoroacetate 2 and substituted 2-bromo or 2-chloropyridines 1. This process features a copper-mediated cross-coupling reaction in DMSO and is the first to utilise pyridylbromides or chlorides with ethyl bromodifluoroacetate 2 in this reaction.
- Ashwood, Michael S.,Cottrell, Ian F.,Cowden, Cameron J.,Wallace, Debra J.,Davies, Antony J.,Kennedy, Derek J.,Dolling, Ulf H.
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p. 9271 - 9273
(2007/10/03)
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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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