Catechol o-methyltransferase activity inhibiting compounds

Abstract

Compounds of formula (I), wherein R1 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.