2-phenylmorpholin-5-one derivatives and pharmaceutical...

Details 2-phenylmorpholin-5-one derivatives and pharmaceutical... 2-phenylmorpholin-5-one derivatives and pharmaceutical...

C - Chemistry, Metallurgy

07

D

C07D 265/32 (2006.01) A61K 31/535 (2006.01) C07D 413/06 (2006.01)

Patent

CA 2264685

2-Phenylmorpholin-5-one derivatives represented by formula (I) (wherein R1 represents an alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, or an indanyl group; R2 represents an alkyl group having 1 to 4 carbon atoms; R3 represents H, an alkyl group having 1 to 5 carbon atoms, or the like; R4 represents H or an alkyl group having 1 to 6 carbon atoms; and R5 and R6 represent each H, an alkyl group having 1 to 5 carbon atoms, or the like), optical isomers or pharmaceutically acceptable salts thereof, or hydrates or solvates thereof, and a pharmaceutical composition comprising the same. The compounds have a potent phosphodiesterase (PDE) IV inhibitory activity, and bronchodilatory and anti-inflammatory activities.

Dérivés du 2-phénylmorpholin-5-one qui répondent à la formule (I): (I) (où R¿1? représente un groupe alkyle ayant de 1 à 8 atomes de carbone, un groupe cycloalkyle qui comprend de 3 à 7 atomes de carbone ou un groupe indanyle; R¿2? représente un groupe alkyle ayant de 1 à 4 atomes de carbone; R¿3? représente H, un groupe alkyle ayant de 1 à 5 atomes de carbone, ou un groupe semblable; R¿4? représente H, un groupe alkyle ayant de 1 à 6 atomes de carbone; et où R¿5? et R¿6? représentent chacun H, un groupe alkyle ayant de 1 à 5 atomes de carbone, ou un groupe semblable), leurs isomères optiques ou leurs sels pharmaceutiquement acceptables, ou leurs hydrates ou solvates ainsi qu'une composition pharmaceutiques les comprenant. Les composés se caractérisent par une forte activité d'inhibition de phosphodiestérase (PDE) IV et par une activité bronchodilatatoire et anti-inflammatoire.

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