Organic compounds

Abstract

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.