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US 8,796,264 B2Granted
2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections
AssigneeEcole Polytechnique Federale De Lausanne (Epfl)
InventorsVadim Makarov, Stewart Cole
Life of this patent
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Abstract
The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria.
Claims10
A compound of the formula
- wherein
- R1 is NO2, NH2, NHOR4, COOR4, CONR5R6, or CHO;
- R2 is halogen, SO2NR5R6, lower alkoxy, COOR4, CONR5R6, CHO, OCF3, or mono-, di- or trifluoromethyl;
- R3 is a saturated or unsaturated, halogenated or unhalogenated, linear, branched or cyclic alkyl having 3-12 carbon atoms, where optionally one or two of methylene groups when present are substituted by O, S or NR4, or
- wherein
- X is saturated or unsaturated, linear or branched aliphatic radical having 1-6 carbon atoms;
- Y is O, S, or NR4;
- Z is direct bond, linear or branched aliphatic radical having 1-3 carbon atoms;
- Q is phenyl, naphtyl, pyridyl, chinolyl, pyrazinyl, pyrimidyl, pyrazolyl, triazinyl, imidazolyl, furanyl, or thienyl and optionally, where one to three hydrogen atoms are substituted by a R7 group;
- R4 is H or C1-3-alkyl;
- n=0, 1, 2, 3, or 4
- R5 and R6 are, independently each from other selected from H, C1-4-alkyl, OC1-4-alkyl, halogen, COOR5, CONR6R7, OCF3, CF3 or CN;
- R7 group is halogen, saturated or unsaturated, linear or branched aliphatic radical having 1-3 carbon atoms, SO2NR5R6, lower alkoxy, COOR4, CONR5R6, CHO, OCF3, mono-, di- or trifluoromethy, or phenyl,
- and/or a pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.