Nabriva Therapeutics Ag

Nabriva Therapeutics Forschungs Gmbh

Rodger Novak

Werner Heilmayer

Rosemarie Mang

Mathias Ferencic

Gerd Ascher

Dirk B Strickmann

Klaus Thirring

Rosemarie Riedl

Atchyuta Rama Chandra Murty Bulusu

Rudolf Badegruber

Susanne Paukner

Dirk Strickmann

Matthias Ferencic

Disclosed are pleuromutilin derivatives of formula (I) and their use in the treatment of diseases mediated by microbes.

Pleuromutilin derivatives for the treatment of diseases mediated by microbes

A pleuromutilin derivative compound of general formula (I) 

14-O&#x2014;[(((C)Alkoxy-(C)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O&#x2014;[(((C)Mono- or dialkylamino-(C)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.

Organic compounds

The present invention relates to Compounds of general formula (I), wherein R is hydrogen and Ris hydroxy or acyloxy, or R is acyl and Ris hydroxy or acyloxy, X is sulphur, oxygen or NR, wherein Ris hydrogen or (C)alkyl; Y is sulphur or oxygen; Ris hydrogen or one or more substituents, e.g. including substituents such as conventional in organic, e.g. (pleuro)mutilin, chemistry; Ris hydrogen or (C)alkyl; Ris hydrogen or (C)alkyl; Rand R' are hydrogen, deuterium, or halogen; R, Rand Rare hydrogen, halogen or deuterium; m is a number selected from 0 to 4, n is a number selected from 0 to 10, and p is a number selected from 0 to 10; with the proviso that n plus p are at least 1. These Compounds are usef&#xfc;l as pharmaceuticals, particularly as antimicrobials. 

Pleuromutilin derivatives containing a hydroxyamino- or acyloxyaminocycloalkyl group

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Vienna, Austria

Rodger Novak