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US 7,612,103 B2Granted
Pleuromutilin derivatives as antimicrobials
AssigneeNabriva Therapeutics AG
InventorsHeinz Berner, Gabriele Kerber
Life of this patent
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Abstract
Compounds of formula wherein R1 and R1′ are hydrogen or deuterium, R2, R3 and R4 are hydrogen or deuterium, R5 is the residue of an amino acid, X is S or N-ALK, is piperidinyl or tetrahydropyridinyl, ALK is (C1-4)alkyl, and R6 is hydrogen, hydroxy or (C2-12)acyloxy, and their use as antimicrobials.
Claims8
A compound of formula
- wherein
- R1 and R1′ are hydrogen or deuterium,
- R2, R3 and R4 are hydrogen or deuterium,
- R5 is the residue of an alpha amino acid, wherein the N which is part of the ring in formula I is acylated by the carboxylic group of said amino acid and wherein the carbonyl group of said amino acid is bound to the nitrogen of the group of formula
- and the —OH group of said amino acid function is missing,
- X is S or N-ALK, the group of formula
- is piperidinyl or tetrahydropyridinyl,
- ALK is (C1-4)alkyl, and
- R6 is hydrogen, hydroxy or (C2-12)acyloxy,
- with the proviso that if the group
- is piperidinyl and X is S, then R6 is other than hydrogen.
8 more elements
A compound of formula
- wherein
- R1 and R1′ are hydrogen or deuterium,
- R2, R3 and R4 are hydrogen or deuterium,
- R7 is a protecting group or the residue of an alpha amino acid, wherein the N which is part of the ring in formula II is acylated by the carboxylic group of said amino acid and wherein the carbonyl group of said amino acid is bound to the nitrogen of the group of formula
- and said amino acid function is devoid of the —OH group, and wherein the amino group is protected,
- X is S or N-ALK, the group of formula
- is piperidinyl or tetrahydropyridinyl,
- ALK is (C1-4)alkyl, and
- R8 is hydrogen, hydroxy or (C2-12)acyloxy,
- with the proviso that if the group of formula
- is piperidinyl and X is S, then R8 is other than hydrogen.
8 more elements
Dependencies are inferred from the claim text.