Administration regime for nitrocatechols

Abstract

A compound of formula (I) where R 1 , R 2 , X, Y, n, m, R 3 , R 4 , R 5 , R 6 and R 7 are as defined herein, for use in the prophylaxis or treatment of a central and peripheral nervous system disorder, wherein the compound of formula (I) is administered prior to sleep, before bedtime or at bedtime.

1 - 60 . (canceled) 
     
     
         61 . A method for the treatment of Parkinson's disease comprising simultaneously or sequentially administering to a patient in need of treatment of Parkinson's disease
 (i) levodopa in an amount of 100 mg,   (ii) carbidopa in an amount of 25 mg or a therapeutically equivalent amount of another aromatic amino acid decarboxylase inhibitor, and   (iii) 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol in an amount ranging from 1 mg to 100 mg, wherein the proportion of 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol to carbidopa ranges from 0.04:1.0 to 4.00:1.0 by weight.   
     
     
         62 . The method according to  claim 61 , wherein said treatment comprises administering a therapeutically equivalent amount of another aromatic amino acid decarboxylase inhibitor. 
     
     
         63 . The method according to  claim 62 , wherein the aromatic amino acid decarboxylase inhibitor is benserazide. 
     
     
         64 . The method according to  claim 61 , wherein the administration is oral. 
     
     
         65 . The method according to  claim 64 , wherein said treatment comprises administering orally an oral solid dosage form. 
     
     
         66 . The method of  claim 61 , wherein the patient to be treated is an adult patient with Parkinson's disease experiencing symptoms of end-of-dose wearing off. 
     
     
         67 . The method of  claim 61 , wherein the total daily dose ranges from 3 to 8. 
     
     
         68 . The method according to  claim 61 , wherein the administration of at least levodopa and carbidopa takes place in a repeated manner. 
     
     
         69 . The method according to  claim 61 , wherein 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol is administered once a day. 
     
     
         70 . The method according to  claim 61 , wherein 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol is administered in an amount of 1 mg. 
     
     
         71 . The method according to  claim 61 , wherein 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol is administered in an amount of 5 mg. 
     
     
         72 . The method according to  claim 61 , wherein 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol is administered in an amount of 10 mg. 
     
     
         73 . The method according to  claim 61 , wherein 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol is administered in an amount of 25 mg. 
     
     
         74 . The method according to  claim 61 , wherein 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol is administered in an amount of 50 mg. 
     
     
         75 . The method according to  claim 61 , wherein 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol is administered in an amount of 100 mg. 
     
     
         76 . The method according to  claim 61 , wherein the proportion of 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol to carbidopa ranges from 0.04:1.0 to 2.00:1.0 by weight. 
     
     
         77 . The method according to  claim 61 , wherein the proportion of 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol to carbidopa is 1.0:1.0 by weight. 
     
     
         78 . A dosage form comprising
 (i) levodopa in an amount of 100 mg,   (ii) carbidopa in an amount of 25 mg or a therapeutically equivalent amount of another aromatic amino acid decarboxylase inhibitor, and   (iii) 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol in an amount ranging from 1 mg to 100 mg, wherein the proportion of 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol to carbidopa ranges from 0.04:1.0 to 4.00:1.0 by weight.   
     
     
         79 . The dosage form according to  claim 78 , wherein said dosage form comprises a therapeutically equivalent amount of another aromatic amino acid decarboxylase inhibitor. 
     
     
         80 . The dosage form according to  claim 79 , wherein the aromatic amino acid decarboxylase inhibitor is benserazide. 
     
     
         81 . The dosage form according to  claim 78 , wherein the administration of at least levodopa and carbidopa takes place in a repeated manner. 
     
     
         82 . The dosage form according to  claim 78 , wherein the proportion of 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol to carbidopa ranges from 0.04:1.0 to 2.00:1.0 by weight.