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Claims for Patent: 4,963,590

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Claims for Patent: 4,963,590

Title: Pharmacologically active compounds, methods for the preparation thereof and compositions containing the same
Abstract:Pharmacologically active catechol derivatives of formula I ##STR1## wherein R.sub.1 and R.sub.2 independently comprise hydrogen, alkyl, acyl, optionally substituted aroyl, lower alkylsulfonyl or alkylcabamoyl or taken together form a lower alkylidene or cycloalkylidene, X comprises an electronegative substituent such as halogen, nitro, cyano, lower alkylsulfonyl, sulfonamido, aldehyde, caboxyl or trifluoromethyl and R.sub.3 comprises hydrogen, halogen, hydroxy alkyl, amino, nitro, cyano, trifluoromethyl, lower alkylsulfonyl, sulfonamide, aldehyde, alkyl carbonyl, aralkylidene carbonyl or carboxyl or a group selected from ##STR2## wherein R.sub.4 comprises hydrogen, alkyl, cyano, carboxyl or acyl and R.sub.5 comprises hydrogen, cyano, carboxyl, alkoxycarbonyl, carboxyalkenyl, nitro, acyl, optionally substituted aroyl or heteroaroyl, hydroxyalkyl or carboxyalkyl or R.sub.4 and R.sub.5 together form a five to seven membered substituted cycloalkanone ring; wherein n is 0-1 and m is 0-7 and R comprises hydroxy, alkyl, carboxyalkyl, optionally substituted alkene, alkoxy or optionally substituted amino; ##STR3## wherein R.sub.8 and R.sub.9 independently comprise hydrogen or one of the following optionally substituted groups; alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl, or together form an optionally substituted piperidyl group; wherein R.sub.10 comprises a substituted alkyl group.
Inventor(s): Backstrom; Reijo J. (Helsinki, FI), Heinola; Kalevi E. (Javenpaa, FI), Honkanen; Erkki J. (Vantaa, FI), Kaakkola; Seppo K. (Helsinki, FI), Kairisalo; Pekka J. (Helsinki, FI), Linden; Inge-Britt Y. (Helsinki, FI), Mannisto; Pekka T. (Helsinki, FI), Nissinen; Erkki A. O. (Espoo, FI), Pohto; Pentti (Helsinki, FI), Pippuri; Aino K. (Espoo, FI), Pystynen; Jarmo J. (Espoo, FI)
Assignee: Orion-yhtyma Oy (FI)
Application Number:07/126,911
Patent Claims: 1. A pharmaceutical composition for inhibiting catechol-O-methyl-transferase, said composition comprising a catechol-O-methyl-transferase inhibiting amount of a compound having the formula I ##STR54## wherein R.sub.1 and R.sub.2 independently represent hydrogen or alkylcarbonyl of 2 to 5 carbon atoms, X represents nitro or cyano and R.sub.3 represents ##STR55## 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; alkoxycarbonyl of 2 to 9 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, and a pharmaceutically acceptable carrier.

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

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

4. A pharmaceutical composition for inhibiting catechol-O-methyl-transferase, said composition comprising a catechol-O-methyl-transferase inhibiting amount of 3-(3,4-dihydroxy-5-nitrobenzylidene)-2,4-pentanedione, and a pharmaceutically acceptable carrier.

5. A pharmaceutical composition 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.

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

7. A pharmaceutical composition for inhibiting catechol-O-methyl-transferase, said composition comprising a catechol-O-methyl-transferase inhibiting amount of N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide, and a pharmaceutically acceptable carrier.

8. A method for inhibiting catechol-O-methyl-transferase in a patient, said method comprising administering a catechol-O-methyl-transferase inhibiting amount of a compound having the formula I ##STR56## wherein R.sub.1 and R.sub.2 independently represent hydrogen or alkylcarbonyl of 2 to 5 carbon atoms, X represents nitro or cyano and R.sub.3 represents ##STR57## 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; alkoxycarbonyl of 2 to 9 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, to a patient in need of such treatment.

9. The method as claimed in claim 8, wherein X is nitro.

10. The method as claimed in claim 8, wherein R.sub.4 and R.sub.5 are both alkylcarbonyl of 2 to 3 carbon atoms.

11. A method for inhibiting catechol-O-methyl-transferase in a patient, said method comprising administering a catechol-O-methyl-transferase inhibiting amount of 3-(3,4-dihydroxy-5-nitrobenzylidene)-2,4-pentanedione, to a patient in need of such treatment.

12. A method as claimed in claim 8, 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.

13. The method as claimed in claim 12, wherein R.sub.5 represents carbamoyl which is substituted with methyl, ethyl, isopropyl or hydroxypropyl.

14. A method for inhibiting catechol-O-methyl-transferase in a patient, said method comprising administering a catechol-O-methyl-transferase inhibiting amount of N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide, to a patient in need of such treatment.
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