Nabriva Therapeutics Ag

Sandoz Gmbh

Biochemie Gesellschaft M.b.h

Heinz Berner

Gerd Ascher

Johannes Hildebrandt

Rosemarie Mang

Rosemarie Riedl

Georg Laber

Gabriele Kerber

Friederike Turnowsky

Hermann Vyplel

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

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

Compounds of formula wherein is piperidinyl or tetrahydropyridinyl,

Pleuromutilin derivatives as antimicrobials

A compound of formula (I) wherein R and Rand the attached nitrogen atom form pyrrolidinyl or piperidinyl. Ris a group of formula (II). Rand R'are hydrogen, deuterium or halogen. R, Rand Rare independently of each other hydrogen or alkyl. R, Rand Rare hydrogen or deuterium. Ris amino, alkyl, aryl, heterocyclyl or mercapto. If X is oxygen, Ris additionally hydrogen; R&#x2032;is alkyl, X is sulphur, oxygen, NR, or N+(R&#x2032;); Y is sulphur or oxygen, and m is 0,1 or 2, with the proviso that, when R and Rand the attached nitrogen atom form piperidinyl, m is O, Y is S and Y is attached in position 3 of the piperidine ring, that group of formula (I) which is attached to the piperidine ring via the residue Y is either in the (S)-configuration or in the (R)-configuration, preferably in the (S)-configuration which is useful as antimicrobial, antibacterial.

Antibacterial mutilins

A compound of formula wherein Ris arylene or heterocyclene; or R and Rtogether with the nitrogen atom to which they are attached form non-aromatic heterocyclene; and the other residues have various meanings, useful as pharmaceuticals, e.g. antimicrobials.

Mutilin derivatives and their use as antibacterials

A compound of formula (I) wherein R is arylene or heterocyclene; or R and R together with the nitrogen atom to which they are attached form non-aromatic heterocyclene; and the other residues have various meanings, useful as pharmaceuticals, e.g. antimicrobials.

A compound selected from 14&mdash;O&mdash;&lsqb;(cycloalkyl-sulfanyl)acetyl&rsqb;mutilins; 14&mdash;O&mdash;&lsqb;(cycloalkyl-alkyl-sulfanyl)acetyl&rsqb; mutilins; 14&mdash;O&mdash;&lsqb;(cycloalkoxy)acetyl&rsqb; mutilins; and 14&mdash;O&mdash;&lsqb;(cycloalkyl-alkoxy)acetyl&rsqb; mutilins and its use as a pharmaceutical.

Pleuromutilin derivatives having antibacterial activity

A compound of formula I ##STR1## wherein R.sub.1 represents ethyl or vinyl and

Pleuromutilin derivatives process for their preparation and their use

Novel pleuromutilin derivatives of formula I, ##STR1## in which R.sub.1 is ethyl or vinyl,

Growing community of inventors

Vienna, Austria

Heinz Berner