Meiji Seika Kaisha, Ltd.

Taisho Pharmaceutical Co., Ltd.

Meiji Seika Pharma Co., Ltd.

Ken Chikauchi

Takao Abe

Masato Kashimura

Eiki Shitara

Tomoaki Miura

Toshiaki Kudo

Tomohiro Sugimoto

Akihiro Morinaka

Kenichi Kanemoto

Yukiko Hiraiwa

Kanako Yamamoto

Jun Kurosaka

Naoki Sasamoto

Mizuyo Ida

Tomohiro Ozawa

Haruhisa Ogita

Dai Kubota

Madoka Kawamura

Akira Manaka

A new metallo-&#x3b2;-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of &#x3b2;-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-&#x3b2;-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of &#x3b2;-lactam antibiotics against metallo-&#x3b2;-lactamase producing bacteria by combining the compound of the general formula (I) with &#x3b2;-lactam antibiotics. 

Metallo-&#x3b2;-lactamase inhibitors

A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci). 

10a-Azalide compound crosslinked at 10a- and 12-positions

[Object]: To provide a compound having a novel structure effective againstand erythromycin resistant bacteria (for example, resistant pneumococci and streptococci) as well as against conventional erythromycin sensitive bacteria. [Solution]: A novel 10a-azalide compound represented by the formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof, or an intermediate for the preparation of the same. The compound of the present invention has superior antibacterial activity against, erythromycin resistant pneumococci and the like, and therefore, the compound can be used as a therapeutic agent of infectious diseases.

10a-Azalide compound

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Kanagawa, Japan

Ken Chikauchi