Novel catechol derivative, pharmaceutical composition...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 205/61 (2006.01) A61K 31/192 (2006.01) A61K 31/24 (2006.01) A61K 31/277 (2006.01) A61K 31/351 (2006.01) A61K 31/381 (2006.01) A61K 31/40 (2006.01) A61K 31/42 (2006.01) A61K 31/425 (2006.01) A61K 31/4453 (2006.01) A61K 31/495 (2006.01) A61K 31/5375 (2006.01) A61K 31/55 (2006.01) A61P 9/12 (2006.01) A61P 25/16 (2006.01) A61P 25/24 (2006.01) A61P 43/00 (2006.01) C07C 255/56 (2006.01) C07C 255/57 (2006.01) C07D 261/08 (2006.01) C07D 277/24 (2006.01) C07D 295/10 (2006.01) C07D 309/06 (2006.01) C07D 333/22 (

Patent

CA 2729405

The present invention provides compounds represented by general formula (I): (see formula I) or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

L'invention porte sur un composé représenté par la formule générale (I) (dans laquelle R1 et R2 représentent chacun un hydrogène, un acyle inférieur, un alcoxycarbonyle inférieur ou similaire ; R3 représente un alkyle inférieur, un alkyle inférieur halogéné, un cycloalkyle, un hétérocycloalkyle, un aryle éventuellement substitué, un hétéroaryle éventuellement substitué ou similaire ; et R4 représente un cyano, un alcoxycarbonyle inférieur, un carboxy ou similaire) ayant une forte activité inhibitrice de COMT ou un sel pharmacologiquement acceptable de celui-ci. L'invention porte également sur une composition pharmaceutique contenant le composé ou un sel de celui-ci, et sur les utilisations du composé, du sel et de la composition.

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