Aminoalkanol Derivatives

Abstract

Disclosed are compounds of formula I wherein R 1 , R 2 , R 5 and R 6 are as defined in the claims; such compounds have interesting pharmacological properties.

1 . A compound of formula I 
       
         
           
           
               
               
           
         
       
       wherein
 R 1  is C 2-8 -alkylene; 
 R 2  is C 1-20 -alkyl, optionally substituted by halogen; 
 R 5  is H or C 1-20 -alkyl; and 
 R 6  is C 1-20 alkyl or a radical of formula a) 
 
       
         
           
           
               
               
           
         
       
       wherein R 3  is C 2-8 -alkylene and R 4  is H or C 1-20 alkyl, optionally substituted by halogen, in free or salt form. 
     
     
         2 . A compound according to  claim 1 , wherein the compound is of formula II 
       
         
           
           
               
               
           
         
       
       wherein
 n is an integer from 1 to 4; 
 m is an integer from 2 to 4; 
 R′ 2  is C 6-14 -alkyl; and 
 R′ 4  is H or C 6-14 -alkyl; 
 in free or salt form. 
 
     
     
         3 . A process for producing a compound according to  claim 1 , comprising deprotecting a compound of formula III 
       
         
           
           
               
               
           
         
       
       wherein R 1 , R 2 , R 5  and R 6  are as defined in  claim 1 , and each of R, R′ and R″ is a protecting group; and recovering the resulting compound of formula I in free or salt form. 
     
     
         4 . A compound of formula III 
       
         
           
           
               
               
           
         
       
       wherein R 1 , R 2 , R 5  and R 6  are as defined in  claim 1 , and each of R, R′ and R″ is a protecting group, in free or salt form. 
     
     
         5 . A compound of formula IV 
       
         
           
           
               
               
           
         
       
       wherein R 1 , R 2 , R″ 4  and R 5  are as defined in  claim 1 , R″ 4  either has the meaning of R 4  or is —CO—C 1-19 alkyl and each of R, R′ and R″ is a protecting group, and q is an integer from 0 to 6, in free or salt form. 
     
     
         6 . A pharmaceutical composition comprising a compound according to  claim 1 , in free or pharmaceutically acceptable salt form, and a pharmaceutically acceptable diluent or carrier. 
     
     
         7 - 8 . (canceled) 
     
     
         9 . A pharmaceutical combination comprising (a) a compound according to  claim 1 , in free or pharmaceutically acceptable salt form, and (b) a second drug substance, said second drug substance being suitable for the prevention or treatment of organ or tissue transplant rejection, or an autoimmune disease or inflammatory condition. 
     
     
         10 . A method for preventing or treating organ or tissue transplant rejection, or an autoimmune disease or inflammatory condition, comprising administering to a subject a therapeutically effective amount of a compound according to  claim 1 , in free or pharmaceutically acceptable salt form.