Suntory Limited

Daiichi Suntory Pharma Co., Ltd.

Tetsuo Shimamoto

Akira Mizuno

Norio Inomata

Makoto Shibata

Tomoe Iwamori

Kyoko Nakanishi

Yasuhiro Hayashi

Hidekazu Inoue

Masaji Ishiguro

Takashi Nakatsuka

Rie Tanaka

Takuro Yoshida

An azetidinone derivative represented by the general formula (1)(wherein ORis a protected hydroxyl group; Ris a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group or a substituted or unsubstituted aromatic group) is reacted with an ester compound represented by the formula (2)(wherein CORis an esterified carboxyl group; X and Y are the same or different and represent individually a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted alkyloxy group, a substituted or unsubstituted alkenyloxy group, a substituted or unsubstituted aralkyloxy group, a substituted or unsubstituted aryloxy group, a substituted or unsubstituted silyloxy group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic-thio group, a substituted or unsubstituted heterocyclic-oxy group, a substituted or unsubstituted acyl group, a substituted or unsubstituted ester group, a substituted or unsubstituted thio ester group, a substituted or unsubstituted amide group, a substituted or unsubstituted amino group, a hydrogen atom or halogen atom, or are taken together with each other to form a substituted or unsubstituted cycloalkan-2-on-1-yl group) in the presence of zinc and copper compounds to synthesis a 4-substituted azetidinone derivative represented by the formula (3)(wherein OR, COR, X and Y are as defined above).

Process for synthesizing 4-substituted azetidinone derivatives

Pyrroloazepine derivatives

1-aryl-1,8-naphthylidin-4-one derivative as type IV phosphodiesterase inhibitor

A 1-cycloalkyl-1,8-naphthylidin-4-one derivative having the formula (I):

1-cycloalkyl-1,8-naphthyridin-4-one derivative as type IV phosphodiesterase inhibitor

A 1-aryl-1,8-naphthylidin-4-one derivative having the formula (I):

A method for treating a circulatory disease or condition in a mammal, which entails administering to the mammal an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof:

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Suita, Japan

Tetsuo Shimamoto