936339-60-5Relevant academic research and scientific papers
HETEROCYCLE SUBSTITUTED PYRIDINE DERIVATIVE ANTIFUNGAL AGENTS
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, (2020/12/29)
Described herein are heterocycle substituted pyridine derivative antifungal agents and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.
Synthesis of analogs of the Gwt1 inhibitor manogepix (APX001A) and in vitro evaluation against Cryptococcus spp
Trzoss, Michael,Covel, Jonathan A.,Kapoor, Mili,Moloney, Molly K.,Soltow, Quinlyn A.,Webb, Peter J.,Shaw, Karen Joy
, (2019/11/11)
Fosmanogepix (APX001) is a first-in-class prodrug molecule that is currently in Phase 2 clinical trials for invasive fungal infections. The active moiety manogepix (APX001A) inhibits the novel fungal protein Gwt1. Gwt1 catalyzes an early step in the GPI anchor biosynthesis pathway. Here we describe the synthesis and evaluation of 292 new and 24 previously described analogs that were synthesized using a series of advanced intermediates to allow for rapid analoging. Several compounds demonstrated significantly (8- to 32-fold) improved antifungal activity against both Cryptococcus neoformans and C. gattii as compared to manogepix. Further in vitro characterization identified three analogs with a similar preliminary safety and in vitro profile to manogepix and superior activity against Cryptococcus spp.
HETEROCYCLE SUBSTITUTED PYRIDINE DERIVATIVE ANTIFUNGAL AGENTS
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, (2019/06/23)
Described herein are heterocycle substituted pyridine derivative antifungal agents and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.
PYRIDINE DERIVATIVES SUBSTITUTED WITH HETEROCYCLIC RING AND gamma-GLUTAMYLAMINO GROUP, AND ANTIFUNGAL AGENTS CONTAINING SAME
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Page/Page column 30-31, (2010/05/13)
The present invention provides an antifungal agent which has excellent antifungal action, and which is also excellent in terms of its properties, and in particular its solubility in water and safety. The present invention discloses a compound represented
An effective synthesis of a (pyridin-3-yl)isoxazole via 1,3-dipolar cycloaddition using ZnCl2: Synthesis of a (2-aminopyridin-3-yl) isoxazole derivative and its antifungal activity
Tanaka, Keigo,Inoue, Satoshi,Murai, Norio,Shirotori, Syuji,Nakamoto, Kazutaka,Abe, Shinya,Horii, Takaaki,Miyazaki, Mamiko,Hata, Katsura,Watanabe, Naoaki,Asada, Makoto,Matsukura, Masayuki
scheme or table, p. 1033 - 1035 (2011/01/10)
We described a rare example of an effective isoxazole synthesis via a 1,3-dipolar cycloaddition using ZnCl2, which allowed us to synthesize novel (2-aminopyridin-3-yl)isoxazole derivatives effectively. In addition, these compounds demonstrated potent antifungal activity in vitro against both Candida albicans and Aspergillus fumigatus.
PROCESS FOR PRODUCTION OF HETEROCYCLE-SUBSTITUTED PYRIDINE DERIVATIVE
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Page/Page column 42, (2010/09/17)
It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I): the meth
PYRIDINE DERIVATIVES SUBSTITUTED BY HETEROCYCLIC RING AND PHOSPHONOAMINO GROUP, AND ANTI-FUNGAL AGENT CONTAINING SAME
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Page/Page column 52, (2009/04/24)
Anti-fungal agent having excellent anti-fungal action physicochemical properties including safety and water solubility. Compound represented by formula (I), or salt thereof: wherein R1 represents hydrogen, halogen, amino, R11-NH- wherein R11 represents C1-6 alkyl, hydroxy C1-6 alkyl, C1-6 alkoxy C1-6 alkyl, or C1-6alkoxycarbonyl C1-6 alkyl, R12-(CO)-NH- wherein R12 represents C1-6 alkyl group or C1-6 alkoxy C1-6 alkyl, C1-6 alkyl, hydroxy C1-6 alkyl, cyano C1-6 alkyl, C1-6 alkoxy, or C1-6 alkoxy C1-6 alkyl or a phosphonoamino group; R2 represents hydrogen, C1-6 alkyl, amino, or a di C1-6 alkylamino group or a phosphonoamino group; one of X and Y is nitrogen while the other is nitrogen or oxygen; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom or 1 or 2 C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, oxygen, sulfur, -CH2O-, -OCH2-, -NH-, -CH2NH-, -NHCH2-, -CH2S-, or -SCH2-; R3 represents hydrogen or halogen or C1-6 alkyl, C3-8 cycloalkyl, C6-10 aryl, a 5- or 6-member heteroaryl group or a 5- or 6-member nonaromatic heterocyclic group which may have 1 or 2 substituents; and R4 represents hydrogen or halogen; provided that either R1 or R2 represents a phosphonoamino group.
HETEROCYCLIC RING AND PHOSPHONOXYMETHYL GROUP SUBSTITUTED PYRIDINE DERIVATIVES AND ANTIFUNGAL AGENT CONTAINING SAME
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Page/Page column 11, (2009/09/28)
The present invention provides compounds that have excellent antifungal action, and are also excellent in terms of properties, such as solubility in water and safety. The compounds are represented by formula (I): The present invention is also directed to
HETEROCYCLE-SUBSTITUTED PYRIDINE DERIVATIVE'S SALT OR CRYSTAL THEREOF
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Page/Page column 10, (2008/12/08)
There is provided a heterocycle-substituted pyridine derivative's salt or a crystal thereof. The present invention provides an acid addition salt of 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-yl amine or a crystal thereof as well as
Heterocycles substituted pyridine derivatives and antifungal agent containing thereof
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Page/Page column 54, (2010/11/27)
An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkoxy C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group or a di C1-6 alkylamino group; one of X and Y is a nitrogen atom while the other is a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom, or 1 or 2 C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, —CH2O—, —OCH2—, —NH—, —CH2NH—, —NHCH2—, —CH2S—, or —SCH2—; R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, a 5- or 6-member heteroaryl group, or 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and R4 represents a hydrogen atom or a halogen atom.
