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US 7,534,814 B2Granted
Mutilin derivatives and their use as antibacterials
AssigneeNabriva Therapeutics AG
InventorsGerd Ascher, Heinz Berner, Johannes Hildebrandt
Life of this patent
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Abstract
A compound of formula wherein R2 is arylene or heterocyclene; or R and R2 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.
Claims6
A compound of formula
- wherein
- R is hydrogen or alkyl;
- R1 is hydrogen or a group of formula
- wherein
- X is sulphur, oxygen, NR10, wherein R10 is hydrogen or alkyl, or N+(R′10)2 wherein
- R′10 is alkyl in the presence of an appropriate anion;
- R9 is amino, alkyl, aryl, heterocyclyl or mercapto;
- and, if X is oxygen, R9 is additionally hydrogen;
- R2 is phenylene;
- R4 is hydrogen or alkyl;
- R5 is hydrogen or alkyl;
- and
- R3, R3′, R6, R7 and R8 independently of each other are hydrogen or deuterium.
10 more elements
A compound of formula
- wherein R1s is hydrogen or a group of formula
- wherein R6s is hydrogen or deuterium;
- R2s is hydrogen, methyl or tert-butyl;
- R7s is hydrogen or methyl;
- and
- R3s, R4s and R5s are hydrogen or deuterium.
3 more elements
A compound which is selected from the group consisting of
- 14-O-(3-amino)phenyl-sulfanylacetyl)-mutilin;
- 14-O-(3-amino)phenyl-sulfanylacetyl)-2,2,4-trideutero-mutilin;
- 14-O-(3-(piperidin-2-yl-carbonylamino)-phenyl-sulfanylacetyl)mutilin;
- 14-O-(3-(piperidin-2-yl-carbonylamino)-phenyl-sulfanylacetyl)-2,2,4-trideutero-mutilin;
- 14-O-(3-(piperidin-2-yl-carbonylamino)-2,5-dimethyl-phenylthio-methylcarbonyl)mutilin;
- 14-O-(3-(piperidin-2-yl-carbonylamino)-2,5-dimethyl-phenylthio-methylcarbonyl)-2,2,4-trideutero-mutilin;
- 14-O-(3-(piperidin-2-yl-carbonylamino)-5 -tert.butyl-phenyl-sulfanylacetyl)mutilin;
- and
- 14-O-(3-(piperidin-2-yl-carbonylamino)-5-tert.butyl-phenyl-sulfanylacetyl)-2,2,4-trideutero-mutilin.
6 more elements
Dependencies are inferred from the claim text.