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US 6,784,193 B1Granted
Mutilin derivatives and their use as antibacterials
AssigneeSandoz Ltd.
InventorsGerd Ascher, Heinz Berner, Johannes Hildebrandt
Life of this patent
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Abstract
A compound of formula (I) 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.
Claims8
A compound of formula
- wherein
- R and R2 together with the nitrogen atom to which they are attached form non-aromatic heterocyclene;
- R1 is a group of the formula
- R3, R3′, R6, R7, and R8 are independently of each other hydrogen or deuterium;
- R4 is hydrogen or alkyl;
- R5 is hydrogen or alkyl;
- R9 is amino, alkyl, aryl, heterocyclyl, or mercapto;
- and, if X is oxygen, R9 is additionally hydrogen;
- R10 is hydrogen or alkyl;
- and
- X is sulphur, oxygen, NR10, or N+(R′10)2 wherein R′10 is alkyl in the presence of an appropriate anion.
8 more elements
A compound of the formula
- wherein R3ss, R4ss, and R5ss are hydrogen or deuterium.
A compound which is
- 14-O-(1-(2-amino-isobutylcarbonyl)-piperidin-3-yl-sulfanylacetyl)mutilin;
- or
- 14-O-(1-(2-amino-isobutylcarbonyl)-piperidin-3-yl-sulfanylacetyl)-2,2,4-trideutero-mutilin.
Dependencies are inferred from the claim text.