Catechol o-methyltransferase activity inhibiting compounds

Abstract

Compounds of formula (I), wherein R 1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.

1 - 27 . (canceled) 
     
     
         28 . A method for the treatment of a disease or condition comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I, 
       
         
           
           
               
               
           
         
       
       wherein R 1  is (C 2 -C 6 )alkenyl, or a pharmaceutically acceptable salt or ester thereof. 
     
     
         29 . The method of  claim 28 , wherein the compound of formula I is (E)-4,5-dihydroxy-2-(pent-1-enyl)isophthalonitrile, (E)-2-(3,3-dimethylbut-1-enyl)-4,5-dihydroxyisophthalonitrile, (Z)-4,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile, (E)-4,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile, (Z)-2-(but-2-enyl)-4,5-dihydroxyisophthalonitrile, 4,5-dihydroxy-2-(3-methylbut-2-enyl)isophthalonitrile, (E)-2-(but-2-enyl)-4,5-dihydroxyisophthalonitrile, 4,5-dihydroxy-2-(2-methylprop-1-enyl)isophthalonitrile, 4,5-dihydroxy-2-vinylisophthalonitrile, 4,5-dihydroxy-2-(prop-1-en-2-yl)isophthalonitrile, 2-allyl-4,5-dihydroxyisophthalonitrile, 4,5-dihydroxy-2-(3-methylbut-2-en-2-yl)isophthalonitrile or (E)-4,5-dihydroxy-2-(4-methylpent-1-enyl)isophthalonitrile. 
     
     
         30 . The method of  claim 28 , wherein the disease or condition is hypertension, heart failure, depression, diabetic vascular dysfunction, pain, or restless leg syndrome. 
     
     
         31 . The method of  claim 28 , wherein the mammal is a human.