申请人:Ciabatti Romeo
公开号:US20050106691A1
公开(公告)日:2005-05-19
The invention regards a process for the production of ramoplanin-like derivatives of formula (I): RAMO-NC—CO—R (I), wherein the radical R represents a hydrocarbon radical and the portion RAMO-NH— represents deacylated ramoplanin, any of its factors or ramoplanose. The compound of Formula (I) are obtained by reacting a carboxylic acid R—COOH with deacylated ramoplanin, any of its factors or ramoplanose protected on the ornitine amino groups. New compounds wherein the hydrocarbon radical R is different form those characaterizing the ramoplanin and ramoplanose natural products and their tetrahydro-derivatives are calimed. The new compounds have the same or better antinfective activity, lower haemolytic effect and better tolerability profile than ramoplanin.
该发明涉及一种制备公式(I)RAMO-NC-CO-R的类似于拉莫普兰(ramoplanin)的衍生物的过程,其中基团R代表一个碳氢基团,RAMO-NH-部分代表去酰化的拉莫普兰、其任何因子或拉莫普兰糖。通过将羧酸R-COOH与保护在鸟氨酸氨基上的去酰化拉莫普兰、其任何因子或拉莫普兰糖反应得到公式(I)的化合物。声明了新的化合物,其中碳氢基团R与拉莫普兰和拉莫普兰糖天然产物及其四氢衍生物所特征的基团不同。新化合物具有与拉莫普兰相同或更好的抗感染活性,较低的溶血效应和更好的耐受性特征。