PURPOSE: To obtain the subject new compound having excellent phosphodiesterase IV-inhibitory activity leading to bronchodilative activity and anti-inflammatory activity, thus useful as a medicine for asthma, etc.
CONSTITUTION: This compound is expressed by formula I {R1 is a 1-4C alkyl-; R2 is tetrahydrophenyl, a l-7C (halo)alkyl, a 2-7C alkenyl, etc.; A is CO, CS, SO2 or a group of formula II (R4 is a 1-4C alkyl), Y is O, S, O-N=CH, etc.; R3 is a (substituted) 1-7C alkyl, a group of formula,(CH2)n-B [ B is (substituted) phenyl, etc.; (n) is 0-4], etc.}, an optical antipode, salt, N-oxide derivative, hydrate, and solvate thereof, e.g. 3-(3-cyclopentyloxy-4-methoxyphenyl)-l-(3-2- pyridylmethylaminocarbonyl)pyrrolidine. The compound of the formula I is obtained by reaction between a compound of formula III and a compound of formula IV (X1 is a halogen) in an organic solvent in the presence of a base such as pyridine at 0 150°C.
YAMAMOTO AKIHIRO
AMEMORI AKIRA
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