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US 6,281,226 B1Granted
Pleuromutilin derivatives as antimicrobials
AssigneeSmithKline Beecham Corporation
InventorsValerie Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt
Life of this patent
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Abstract
The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.
Claims15
A compound of general formula (IA) or (IB):
- in which:
- each of n and m is independently 0, 1 or 2;
- and
- X is selected from —O—, —S(O)—, —SO2—, —CO.O—, —NH—, —CONH—, —NHCONH— and a bond;
- or
- n is 1 or 2 and m is 2 and X is —S—;
- and
- R1 is vinyl or ethyl;
- R2 is optionally substituted quinuclidinyl, azabicyclo[2.2.1]heptyl, azabicyclo[4,3,0]nonyl, azabicyclo[3.2.1]octyl, azabicyclo[3,3,0]octyl, azabicyclo[2.2.2]octyl, azabicyclo[3.2.1]octenyl, azabicyclo[3.3.1]nonyl or azabicyclo[4.4.0]decyl;
- R3 is H or OH;
- or
- the moiety R2(CH2)mX(CH2)nCH2COO at position 14 of (IA) or (IB) is replaced by RaRbC=CHCOO in which one of Ra and Rb is hydrogen and the other is R2 or Ra and Rb together form R2;
- or
- a pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.