Nabriva Therapeutics Ag

Nabriva Therapeutics Forschungs Gmbh

Rosemarie Mang

Werner Heilmayer

Rodger Novak

Mathias Ferencic

Gerd Ascher

Heinz Berner

Atchyuta Rama Chandra Murty Bulusu

Dirk B Strickmann

Rudolf Badegruber

Dirk Strickmann

The present invention relates to compounds selected from the group consisting of 14-0-[((Mono- or dialkylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[((Cycloalkyl- or heterocyclylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioaceyl or -imino-oxy]-mutilins, 14-O-[((Heterocyc-N-yl-cycloalkyl)-sulfanyl- or -oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Mono- or dialkylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Cycloalkyl- or heterocyclylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and 14-O-[((Heterocyc-N-yl-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and their use as pharmaceuticals.

Organic compounds

Compounds of formula (I), which are 14-O-{[(optionally substituted hydroxy)cyclohexyl)sulfanyl]acetyl}mutilins further substituted at the cyclohexyl group by an acylated amino group, salts and solvates thereof, pharmaceutical compositions comprising such compounds and their use as a pharmaceutical, e.g. for the treatment of diseases mediated by microbes and for the treatment of inflammation where microbes are mediating said inflammation. 

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 method of preventing or treating diseases caused bycomprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.

Tuberculosis treatment using pleuromutilin derivatives

A pleuromutilin derivative compound of general formula (I) 

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. 

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Vienna, Austria

Rosemarie Mang