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Claims for Patent: 5,112,861

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Claims for Patent: 5,112,861

Title: Method of treating Parkinson's Disease using pentanedione derivatives
Abstract:The invention concerns a method for the treatment of Parkinson's Disease. The method comprises administering a catechol-O-methyl-transferase inhibiting amount of a compound having the formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, alkylcarbamoyl of 2 to 5 carbon atoms or alkylcarbonyl of 2 to 5 carbon atoms, X represents nitro or cyano and R.sub.3 represents ##STR2## wherein R.sub.4 represents cyano or alkylcarbonyl of 2 to 5 carbon atoms and R.sub.5 represents cyano; alkylcarbonyl of 2 to 5 carbon atoms; or carbamoyl which is unsubstituted or substituted with alkyl of 1 to 8 carbon atoms, or hydroxyalkyl of 1 to 8 carbon atoms or pharmaceutically acceptable salts or esters thereof; and a sufficient amount of levodopa to treat Parkinson's Disease. A peripheral decarboxylase inhibitor such as carbidopa or benzerazide is also preferably administered.
Inventor(s): Backstrom; Reijo (Helsinki, FI), Heinola; Kalevi E. (Jarvempaa, FI), Honkanen; Erkki J. (Vantaa, FI), Kaakkola; Seppo K. (Helsinki, FI), Kairisalo; Pekka J. (Helsinki, FI), Linden; Inge-Britt Y. (Helsinki, FI), Mannisto; Pekka I. (Helsinki, FI), Nissinen; Erkki A. O. (Espoo, FI), Pohto; Pentti (Helsinki, FI), Pippuri; Aino K. (Espoo, FI), Pystynen; Jarmo (Espoo, FI)
Assignee: Orion-yhtyma Oy (Espoo, FI)
Application Number:07/587,791
Patent Claims: 1. A method for the treatment of Parkinson's Disease, said method comprising administering a catechol-O-methyl-transferase inhibiting amount of a compound having the formula I ##STR53## wherein R.sub.1 and R.sub.2 independently represent hydrogen, alkylcarbamoyl of 2 to 5 carbon atoms or alkylcarbonyl of 2 to 5 carbon atoms, X represents nitro or cyano and R.sub.3 represents ##STR54## wherein R.sub.4 represents cyano or alkylcarbonyl of 2 to 5 carbon atoms and R.sub.5 represents cyano; alkylcarbonyl of 2 to 5 carbon atoms; or carbamoyl which is unsubstituted or substituted with alkyl of 1 to 8 carbon atoms, or hydroxyalkyl of 1 to 8 carbon atoms or pharmaceutically acceptable salts or esters thereof; and a sufficient amount of levodopa to treat Parkinson's Disease, to a patient in need of such treatment.

2. The method as claimed in claim 1, wherein X is nitro.

3. The method as claimed in claim 1, wherein R.sub.4 and R.sub.5 are both alkylcarbonyl of 2 to 3 carbon atoms.

4. The method as claimed in claim 1, wherein R.sub.4 represents cyano and R.sub.5 represents carbamoyl which is unsubstituted or substituted with alkyl of 1 to 8 carbon atoms or hydroxyalkyl of 1 to 8 carbon atoms.

5. The method as claimed in claim 4, wherein R.sub.5 represents carbamoyl which is substituted with methyl, ethyl, isopropyl or hydroxypropyl.

6. The method as claimed in claim 1, further comprising administering a sufficient amount of a peripheral decarboxylase inhibitor to inhibit early dopamine formation.

7. The method as claimed in claim 4, wherein said peripheral decarboxylase inhibitor is carbidopa.

8. The method as claimed in claim 6, wherein said peripheral decarboxylase inhibitor is benzerazide.

9. A method for the treatment of Parkinson's Disease, said method comprising administering a catechol-O-methyl-transferase inhibiting amount of 3-(3,4-dihydroxy-5-nitrobenzylidene)-2,4-pentanedione; and a sufficient amount of levodopa to treat Parkinson's Disease, to a patient in need of such treatment.

10. The method as claimed in claim 9, further comprising administering a sufficient amount of a peripheral decarboxylase inhibitor to inhibit early dopamine formation.

11. The method as claimed in claim 10, wherein said peripheral decarboxylase inhibitor is carbidopa.

12. The method as claimed in claim 10, wherein said peripheral decarboxylase inhibitor is benzerazide.

13. A method for the treatment of Parkinson's Disease, said method comprising administering a catechol-O-methyl-transferase inhibiting amount of N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide; and a sufficient amount of levodopa to treat Parkinson's Disease, to a patient in need of such treatment.

14. The method as claimed in claim 13, further comprising administering a sufficient amount of a peripheral decarboxylase inhibitor to inhibit early dopamine formation.

15. The method as claimed in claim 14, wherein said peripheral decarboxylase inhibitor is carbidopa.

16. The method as claimed in claim 14, wherein said peripheral decarboxylase inhibitor is benzerazide.
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