ORGANIC COMPOUNDS
A compound of formula (I) wherein n is 0 to 4; R is ethyl or vinyl; R 1 is hydrogen or (C 1-6 )alkyl, R 2 is hydrogen or cycloalkyl including (C 3-6 )cycloalkyl, or unsubstituted (C 1-6 )alkyl, or (C 1-6 )alkyl substituted by one or more of hydroxy; preferably one or two, halogen, (C 3-6 )cycloalkyl, or R 1 is hydroxy and R 2 is formyl.
1 . A compound of formula (I)
wherein
n is 0 to 4;
R is ethyl or vinyl;
R 1 is hydrogen or (C 1-6 )alkyl,
R 2 is hydrogen or
cycloalkyl including (C 3-6 )cycloalkyl, or
unsubstituted (C 1-6 )alkyl, or
(C 1-6 )alkyl substituted by one or more of
hydroxy; preferably one or two,
halogen,
(C 3-6 )cycloakyl, or
R 1 is hydroxy and R 2 is formyl.
2 . A compound of formula (II)
wherein n, R 1 and R 2 are as defined in claim 1 .
3 . A compound of formula (III)
wherein n, R 1 and R 2 are as defined in claim 1 .
4 . A compound of formula (IV)
wherein n, R 1 and R 2 are as defined in claim 1 .
5 . A compound according to claim 1 , selected from the group consisting of
14-O-{[(1R, 2R, 4R)-4-Amino-2-hydroxy-cyclohexylsulfanyl]-acetyl }-mutilin and the (1S, 2S 4S) diastereomer thereof
14-O-{[(1R, 2R, 5S)-5-Amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin and the (1S, 2S, 5R) diastereomer thereof
14-O-{[(1R, 2R, 4S)-4-Amino-2-hydroxy-cyclohexylsulfanyl]-acetyl }-mutilin and the (1S, 2S, 4R) diastereomer thereof
14-O-{[(1R, 2R, 5R)-5-Amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin and the (1S, 2S, 5S) diastereomer thereof
14-O-{[(1R, 2R, 3R)-3-Amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin and the (1S, 2S, 3S) diastereomer thereof
14-O-{[(1R, 2R, 4R)-4-Diethylamino-2-hydroxy-cyclohexylsulfanyl]-acetyl }-mutilin and the (1S, 2S, 4S) diastereomer thereof
14-O-{[(1R, 2R, 4R)-4-Ethylamino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin and the (1S, 2S, 4S) diastereomer thereof
14-O-{[(1R, 2R, 5S)-5-Ethylamino-2-hydroxy-cyclohexylsulfanyl]-acetyl }-mutilin and the (1S, 2S, 5R) diastereomer thereof
14-O-{[(1R, 2R, 5S)-5-Diethylamino-2-hydroxy-cyclohexylsulfanyl]-acetyl }-mutilin and the (1S, 2S, 5R) diastereomer thereof
14-O-{[(1R, 2R, 4S)-4-Diethylamino-2-hydroxy-cyclohexylsulfanyl]-acetyl }-mutilin and the (1S, 2S, 4R) diastereomer thereof
14-O-{[(1R, 2R, 5R)-5-Diethylamino-2-hydroxy-cyclohexylsulfanyl]-acetyl }-mutilin and the (1S, 2S, 5S) diastereomer thereof
14-O-{[(1R, 2R, 3R)-3-Ethylamino-2-hydroxy-cyclohexylsulfanyl]-acetyl }-mutilin and the (1S, 2S, 3S) diastereomer thereof
14-O-{[(1R, 2R, 3R)-3-Diethylamino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin and the (1S, 2S, 3S) diastereomer thereof
14-O-{[(1R, 2R, 4S)-4-(Formyl-hydroxy-amino)-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin and the (1S, 2S, 4R) diastereomer thereof
14-O-{[(1R, 2R, 5S)-5-(Formyl-hydroxy-amino)-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin and the (1S, 2S, 5R) diastereomer thereof
and
14-O-{[(1R, 2R, 3R/S)-3-(Formyl-hydroxy-amino)-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin and the (1S, 2S, 3R/S) diastereomer thereof.
6 . The compound according to claim 1 the form of a salt and/or solvate.
7 . A compound according to claim 1 for use as a pharmaceutical drug substance.
8 . A method of treatment of diseases mediated by microbes which comprises administering to a subject in need of such treatment an effective amount of a compound of claim 1 .
9 . A pharmaceutical drug composition comprising a compound of claim 1 , in association with at least one pharmaceutical excipient.
10 . A pharmaceutical drug composition according to claim 9 , further comprising another pharmaceutically active agent.