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V-ATPASE ACTIVITY INHIBITOR, ANTIBACTERIAL AGENT, MEDICINE, ANTIBACTERIAL METHOD AND SCREENING METHOD

Foreign code F200010262
File No. J1038-01WO
Posted date 2020年11月9日
Country 世界知的所有権機関(WIPO)
International application number 2020JP001047
International publication number WO2020149295
Date of international filing 令和2年1月15日(2020.1.15)
Date of international publication 令和2年7月23日(2020.7.23)
Priority data
  • 特願2019-006819 (2019.1.18) JP
Title V-ATPASE ACTIVITY INHIBITOR, ANTIBACTERIAL AGENT, MEDICINE, ANTIBACTERIAL METHOD AND SCREENING METHOD
Abstract An activity inhibitor of Na+-transporting V-ATPase that comprises a compound represented by formula (1). (R1 represents a group which is selected from among a hydroxy group, an alkoxy group and a haloalkoxy group each bonded to the adjacent phenyl group via oxygen or selected from among a dialkylamino group, a heterocyclic amine and a carboxylic acid amide group each bonded to the adjacent phenyl group via nitrogen, or represents bromine, iodine or a linear hydrocarbon group. R2 represents hydrogen or a haloalkoxy group. Z1 represents an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aromatic hydrocarbon group or a heterocyclic group, which optionally has an arbitrary substituent and has a structure containing a double bond represented by any of formulae (1-1) to (1-3) between the same and the adjacent phenyl group. * represents a bond to the adjacent phenyl group.)
Outline of related art and contending technology BACKGROUND ART
V-ATPase is a supramolecular complex which exists in organelle membranes of eukaryotic organisms and is composed of complex subunit structures. V-ATPase has a function as an ion transporting molecular motor, and transports ions between the inside and outside of the membrane while a specific detailed unit rotates in the membrane by hydrolysis energy of ATP. V-ATPase is also known to be present in prokaryote (bacteria), and sometimes referred to as A-ATPase.
V-ATPase is necessary for cells to grow in a particular environment. For example, in Enterococcus, V-ATPase has the function of hydrolyzing ATP to transport intracellular sodium ions (Na +) out of the cell, which allows Enterococcus to grow under high salt concentrations and high pH conditions.
In addition, V-ATPase similar to Enterococcus is present in various pathogenic microorganisms, and plays an important role in the growth under alkaline conditions. Accordingly, the compound inhibiting the ion transport function of V-ATPase is useful as an antibacterial agent for pathogenic bacteria causing diseases, and is expected as a new therapeutic agent.
Various compounds have been known as antibacterial agents. For example, Patent Document 1 describes that 2-substituted benzimidazole having a specific structure is useful as an antibacterial agent.
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
  • Inventor
  • MURATA Takeshi
  • SHIMIZU Kouki
  • YAKUSHIJI Fabiana Lica
  • MORIYAMA Katsuhiko
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JO JP KE KG KH KN KP KR KW KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN WS ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
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