12-epi pleuromutilins

US9701628B2 · kind B2 · utility

Assignee

• NABRIVA THERAPEUTICS GMBH · AT

Inventors

• Klaus Thirring · Wien, AT
• Werner Heilmayer · Staprijk, AT
• Rosemarie Riedl · Wien, AT
• Hermann Kollmann · Linz, AT
• Zrinka Ivezic-Schoenfeld · Stockerau, AT
• Wolfgang Wicha · Trautmannsdorf, AT
• Susanne Paukner · Wien, AT
• Dirk Strickmann · Wien, AT

Key dates

• Filing date: Jan 21, 2015
• Grant date: Jul 11, 2017
• Expiry date: Jan 21, 2035

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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 formulaprocesses for the preparation of such compounds and their use as pharmaceuticals.