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|Title:||Pharmacologically active compounds, methods for the preparation thereof and compositions containing the same|
|Abstract:||Catechol compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3 and X are as described herein are effective Catechol-O-methyltransferase inhibitors.|
|Inventor(s):||Backstrom; Reijo J. (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 J. (Espoo, FI)|
|Assignee:||Orion-yhtyma Oy (Espoo, FI)|
|Filing Date:||Dec 07, 1992|
|Claims:||1. A compound according to formula I ##STR52## wherein R.sub.1 and R.sub.2 independently represent hydrogen, carbamoyl which is substituted by an alkyl of 1 to 4 carbon atoms, alkylcarbonyl of 2 to 5 carbon atoms or phenyl carbonyl, X represents halogen nitro or cyano and R.sub.3 represents ##STR53## 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 alkoxycarbonyl of 2 to 9 carbon atoms, or pharmaceutically acceptable salts thereof. |
2. The compound according to claim 1, wherein the compound is 3-(3,4-dihydroxy-5-nitrobenzylidene)-2,4-pentanedione.
3. The compound according to claim 1, wherein the compound is ethyl 2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylate or ethyl 3,4-dihydroxy-5-nitrobenzylcyanoacetate.