申请人:NABRIVA THERAPEUTICS AG
公开号:US20160332963A1
公开(公告)日:2016-11-17
A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of formula
processes for the preparation of such compounds and their use as pharmaceuticals.
从14-O-[((烷基、环烷基、杂环烷基、杂环芳基或芳基)-硫基)-乙酰基]-12-epi-木替林,或14-O-[((烷基、环烷基、杂环烷基、杂环芳基或芳基)-氧基)-乙酰基]-12-epi-木替林中选择的一种化合物,其中12-epi-木替林的特征在于木替林环在位置12被两个取代基取代,木替林环在位置12的第一个取代基是一个甲基基团,该甲基基团的立体化学与天然存在的普鲁木替林环在位置12的甲基基团的立体化学相反,木替林环在位置12的第二个取代基是一个含有至少一个氮原子的碳氢基团,木替林环的所有其他取代基与天然存在的普鲁木替林环中相应位置的取代基的立体化学相同;可选地以盐和/或溶剂的形式存在,其中天然存在的普鲁木替林的化学式为
制备这类化合物的方法以及它们作为药物的用途。