| 发明名称 |
12-EPI PLEUROMUTILINS |
| 摘要 |
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. |
| 申请公布号 |
US2016332963(A1) |
申请公布日期 |
2016.11.17 |
| 申请号 |
US201515111390 |
申请日期 |
2015.01.21 |
| 申请人 |
NABRIVA THERAPEUTICS AG |
发明人 |
Thirring Klaus;Heilmayer Werner;Riedl Rosemarie;Kollmann Hermann;Ivezic-Schoenfeld Zrinka;Wicha Wolfgang;Paukner Susanne;Strickmann Dirk |
| 分类号 |
C07C323/52;C07D211/58;A61K31/4468;C07D295/13;A61K31/5375;C07D295/192;A61K31/495;C07D211/26;A61K31/445;A61K31/4465;C07D213/56;A61K31/4409;C07D211/54;C07D249/14;A61K31/4196;C07D473/38;A61K31/52;A61K31/4458;C07D213/32;A61K31/44;A61K31/216 |
主分类号 |
C07C323/52 |
| 代理机构 |
|
代理人 |
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| 主权项 |
1. 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 |
| 地址 |
Wien AT |
