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US 2010/0035832 A1Published application
Macrolides
AssigneeAlpharma Aps
InventorsAudun Heggelund, Kjell Undheim
Life of this patent
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Abstract
This invention relates to a novel class of antibiotic agents, more specifically to macrolides comprising an oxazolidinone structure, their preparation, pharmaceutical compositions containing them, their use and methods of treatment using them.
Claims15
A macrolide of Formula I, and pharmaceutically acceptable polymorphs, salts, prodrugs and solvates thereof,
- in which formula
- X and Y independently represent hydrogen, hydroxy, cyano, carboxy, COOR13 (wherein R13 represents an optionally substituted aliphatic group), halogen, optionally substituted alkyl, optionally substituted alkoxy, or nitro, the benzene ring is optionally further substituted in the 2 and/or 6 position;
- Z represents hydrogen or halogen;
- R represents:
- (i) Morpholino, thiomorpholino, piperidino, or piperazino, said rings are optionally substituted on ring C atom(s) and/or ring N atom (such as with hydrogen, alkyl, alkoxy, —CO2-alkyl, —CO-alkyl-OH, —CO-alkanediyl-OH, -alkanediyl-O-alkyl, -alkanediyl-halogen, -alkenyl-O-alkyl, -alkenyl-halogen (any said groups being optionally substituted));
- (ii) optionally substituted alkanoyl;
- (iii) —N(R8)R9, wherein R8 and R9 independently represent hydrogen or optionally substituted alkyl;
- or R8 and R9 together represent the group -alkanediyl-R11-alkanediyl-, which group is optionally substituted, and R11 represents CH2, S, O, SO, SO2, SNR12, S(O)NR12 or NR12, wherein R12 represents hydrogen or optionally substituted alkyl (such as with halogen, hydroxy, alkoxy, amino, alkylamino, or dialkylamino) or p-toluenesulfonyl;
- or
- (iv) —N(R8)R9, wherein R8 and R9 independently represent hydrogen or optionally substituted alkyl;
- or R8 and R9 together represent the group -alkenyl-R11-alkenyl-, which group is optionally substituted, and R11 represents CH2, S, O, SO, SO2, SNR12, S(O)NR12 or NR12, wherein R12 represents hydrogen or optionally substituted alkyl (such as with halogen, hydroxy, alkoxy, amino, alkylamino, or dialkylamino) or p-toluenesulfonyl;
- R represents, together with the vicinal X:
- (i) —CO-alkanediyl-, which is optionally substituted;
- (ii) —NR5-alkanediyl-, which is optionally substituted and wherein R5 represents optionally substituted alkanoyl;
- (iii) —CO-alkenyl-, which is optionally substituted
- (iv) —NR5-alkenyl-, which is optionally substituted and wherein R5 represents optionally substituted alkanoyl;
- R6 represents hydrogen or optionally substituted alkyl;
- and R7 represents hydrogen, a hydroxy-protecting group or optionally substituted alkanoyl;
- or R6 and R7 together represent —CO—.
16 more elements
5-13. (canceled)
15-17. (canceled)
24-25. (canceled)
Dependencies are inferred from the claim text.