发明名称 NEW ANTI-CLOSTRIDIUM COMPOUNDS
摘要 The present invention relates to compounds having a backbone structure for use as antibiotic, more specifically use against infections with Gram positive bacteria, preferably Clostridium, more preferably C. difficile or C. perfringens. The compounds of the invention are particularly useful against spores of these bacteria.;
申请公布号 US2017035750(A1) 申请公布日期 2017.02.09
申请号 US201515304456 申请日期 2015.04.14
申请人 Nederlandse Organisatie voor toegepast-natuurweten schappelijk Onderzoek TNO 发明人 SCHUREN Frank Henri Johan;MONTIJN Roy Christiaan
分类号 A61K31/4745 主分类号 A61K31/4745
代理机构 代理人
主权项 1. A method to effect antibiotic activity which method comprises contacting bacteria with a compound of formula (I) wherein S1, S2, S3, S4 are independently H, F, Cl, Br, I, hydroxy-, thiol-, thioether, NH2, nitro-, cyano-, isocyano-, carboxylic acid, alkyl-, hydroxyalkyl-, alkoxy-, alkoxyalkyl-, a carbocyclic- or a heterocyclic group, orwherein S5-S9 is independently H or F; wherein Y1 and Y2 are selected from the group consisting of CH, CF, C-alkyl, C-alkoxy, C-alkoxyalkyl, C-carbocycle, C-heterocycle or N; n, m are independently 0-8; Pn1, Pn2, Qm1, Qm2 are independently H, halogen, alkyl, alkoxy, alkoxyalkyl, carbocycle or heterocycle; wherein if n=0 or 1, then X1 is H, OX3, wherein if m=0 or 1, then X2 is H, OX3,and wherein if n is 2-8, then X1=OX3,and wherein if m=2-8, then X2=OX3, wherein one of Y3, Y4 and Y5 is C or N, and the others of Y3, Y4 and Y5 are C, and that if Yn═N, the R-group on that N-atom is void; wherein R1-R5 are independently H, OH, alkyl, alkoxy, alkoxyalkyl, carbocycle or heterocycle; wherein X3=H, alkyl or (—CO)—R6, wherein R6=alkyl; and wherein R7-R20 are independently H, F, Cl, Br, I, hydroxy-, thiol-, thioether, NH2, nitro-, cyano-, isocyano-, carboxylic acid, alkyl-, hydroxyalkyl-, alkoxy-, alkoxyalkyl-, a carbocyclic- or a heterocyclic group; or a pharmaceutically acceptable salt thereof.
地址 s-Gravenhage NL