C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
167/179, 260/515
C07C 205/00 (2006.01) A61K 31/00 (2006.01) C07C 43/23 (2006.01) C07C 45/56 (2006.01) C07C 45/67 (2006.01) C07C 45/74 (2006.01) C07C 47/565 (2006.01) C07C 47/575 (2006.01) C07C 49/835 (2006.01) C07C 49/84 (2006.01) C07C 59/56 (2006.01) C07C 59/64 (2006.01) C07C 59/68 (2006.01) C07C 205/22 (2006.01) C07C 205/23 (2006.01) C07C 205/26 (2006.01) C07C 205/34 (2006.01) C07C 205/37 (2006.01) C07C 205/43 (2006.01) C07C 205/45 (2006.01) C07C 205/56 (2006.01) C07C 205/57 (2006.01) C07C 255/38 (2006.01) C07D 207/333 (2
Patent
CA 1334967
Disclosed and claimed are pharmacologically active catechol derivatives of formula (I): (I) Image or a salt thereof, in which R1 and R2 independently represent hydrogen, optionally substituted acyl or aroyl, lower alkylcarbamoyl, X represents an electronegative substituent such as halogen, nitro, cyano, aldehyde and trifluoromethyl; and R3 represents alkyl substituted by lower alkoxy lower alkoxy, carboxy lower alkyl, thio or pyrrole group, or a group selected from: Image Image (A) or wherein R4 represents cyano or acyl and R5 represents cyano, alkoxycarbonyl, carboxyalkenyl, nitro, acyl, hydroxyalkyl, carboxyalkyl, one of the following optionally substituted groups: carbamoyl, aroyl or heteroaroyl, or R4 and R5 form together a five to seven membered, optionally substituted cycloalkanone ring; (B) (CH2)m-COR wherein m is 2-7 and R represents hydroxy, alkyl, carboxyalkyl, optionally substituted alkene, alkoxy or optionally substituted amino; (C) Image wherein R8 represents hydrogen and R9 represents an optionally substituted adamantyl group. These new derivatives of formula (I) are active as catechol-0-methyl- transferase (COMT) inhibitors and can be used as such or as pharmaceutical compositions in the treatment of depression, heart failure and/or hypertension.
552987
Backstrom Reijo
Heinola Kalevi
Honkanen Erkki
Kaakkola Seppo
Kairisalo Pekka
Orion-Yhtyma Oy
Robic
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