3-ANILINO-2-CYCLOALKENONE DERIVATIVE

Japanese Patent JP3542482

B2

PROBLEM TO BE SOLVED: To obtain a novel compound having excellent inhibition for a specific phosphodiesterase and useful as a therapeutic agent against inflammatory diseases such as asthma, skin inflammation, etc., and multiple sclerosis, etc.
SOLUTION: This 3-anilino-2-cycoalkenone derivative is a compound of formula I [R1 is a (substituted) 1-8C alkyl (except for methyl having no substituents) or the like; R2 is a 1-4C alkyl; R3 is H or the like; R4 is H or the like; R5 to R8 are each H or the like; X is (CR11R12)n or the like; R11 and R12 are each H or the like; (n) is 0-2], e.g. 3-(3-cyclopentyloxy-4-methoxyanilino)-2- cyclopentene-1-one. The compound of formula I is obtained by, e.g. condensing to dehydrate an aniline derivative (e.g. 3-cyclopentyloxy-4-methoxyaniline, etc.), of formula II with a l, 3-dione (e.g. 1,3-cyclopentadione, etc.), of formula III in a solvent such as benzene using a condensing agent such as p-toluenesulfonic acid, etc. The novel compound is excellent in inhibiting phosphodiesterase IV.

Masatsugu Ina
Kenshiro Yamana
Kyoji Noda
Toshihiko Akiyama
Takahama Akane

JP36619697A

July 14, 2004

December 25, 1997

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Nikken Chemical Co., Ltd.

C07D295/12; A61K31/135; A61K31/165; A61K31/34; A61K31/341; A61K31/435; A61K31/44; A61K31/4402; A61K31/4406; A61K31/4409; A61K31/47; A61K31/535; A61K31/5375; A61P11/00; A61P17/00; A61P29/00; A61P37/08; C07C225/20; C07D211/88; C07D213/53; C07D213/74; C07D215/12; C07D307/20; (IPC1-7): C07C225/20; A61K31/135; A61K31/165; A61K31/34; A61K31/435; A61K31/44; A61K31/47; A61K31/535; A61P11/00; A61P17/00; A61P29/00; A61P37/08; C07D211/88; C07D213/53; C07D213/74; C07D215/12; C07D295/12; C07D307/20

JP10072415A

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