[EN] GOLD (I)-PHOSPHINE COMPOUNDS AS ANTI-BACTERIAL AGENTS<br/>[FR] COMPOSÉS À BASE D'OR (I)-PHOSPHINE EN TANT QU'AGENTS ANTI-BACTÉRIENS
申请人:AUSPHERIX LTD
公开号:WO2015181550A1
公开(公告)日:2015-12-03
A compound of formula (I) for use in the prevention or treatment of a bacterial infection wherein RP1 is either methyl, ethyl, isopropyl, cyclohexyl or phenyl; RP2 is selected from methyl, ethyl, isopropyl, cyclohexyl and phenyl; RP3 is either ethyl, isopropyl, cyclohexyl, phenyl or pyridyl; A is either S or Se; RA is selected from wherein each of Y1, Y2, Y3, Y4 and Y9 is independently selected from CH or N, wherein at least three of Y1, Y2, Y3, Y4 and Y9 are CH; V is selected from O, CH-ORO1, N-CO2-RC2 or N-RN2; one of Y5, Y6, Y7 and Y8 is selected from CH and N, and the others are CH; X is selected from NH, S or O; RC1 is selected from O-RO2 or NHRN1; RO1 is selected from H and C1-3 unbranched alkyl; RO2 is C1-3 unbranched alkyl; RN1 is selected from H and C1-3 unbranched alkyl; RN2 is C1-3 unbranched alkyl; RC2 is either C1-3 unbranched alkyl or C3-4 branched alkyl; RC3 is selected from C1-3 unbranched alkyl and C2H4CO2H; RC4 is either H or Me; RC5 is either H or Me; RC6 represents one or two optional methyl substituents; and n is an integer from 2 to 8.
公式(I)的化合物用于预防或治疗细菌感染,其中RP1为甲基、乙基、异丙基、环己基或苯基之一;RP2从甲基、乙基、异丙基、环己基和苯基中选择;RP3为乙基、异丙基、环己基、苯基或吡啶基之一;A为S或Se;RA从Y1、Y2、Y3、Y4和Y9中选择,其中Y1、Y2、Y3、Y4和Y9中至少有三个是CH;V从O、CH-ORO1、N-CO2-RC2或N-RN2中选择;Y5、Y6、Y7和Y8中的一个从CH和N中选择,其余为CH;X从NH、S或O中选择;RC1从O-RO2或NHRN1中选择;RO1从H和C1-3直链烷基中选择;RO2为C1-3直链烷基;RN1从H和C1-3直链烷基中选择;RN2为C1-3直链烷基;RC2为C1-3直链烷基或C3-4支链烷基之一;RC3从C1-3直链烷基和C2H4CO2H中选择;RC4为H或Me;RC5为H或Me;RC6代表一个或两个可选的甲基取代基;n为2到8之间的整数。