Daiichi Sankyo Company, Limited

Junichi Kuroyanagi

Makoto Takemura

Hisashi Takahashi

Rie Miyauchi

Hiroshi Takeshita

Issei Achiwa

Isao Hayakawa

Toshiyuki Konosu

Yuko Yamamoto

Yoshiko Kagoshima

Masatoshi Nagamochi

Takuya Uchida

Tsuyoshi Soneda

Tetsunori Fujisawa

Aki Yokomizo

Nobuhisa Masuda

Kazuo Kanai

Tetsuji Noguchi

Takafumi Hosokawa

Satoshi Komoriya

Katsuhiro Kawakami

Yasuyuki Takeda

Takao Horiuchi

Syozo Kobayashi

Yuichi Sugimoto

To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.

Imidazole carbonyl compound

An antibiotic compound having a novel mechanism of action, weak cytotoxicity, high solubility in water, effective in inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and having antibacterial activity.

A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), which exhibit higher safety, and which has a structure of formula (I): 

Substituted pyrrolidine derivative

The present invention provides a method for effectively producing an optically active form of tetrasubstituted-5-azaspiro[2.4]heptane derivative, which serves as a useful production intermediate for quinolonecarboxylic acid antibacterial agents, and intermediates for the derivative. The present invention is directed to a method for producing a compound (VII) according to the following scheme. 

Process for preparation of tetrasubstituted 5-azaspiro[2.4]- heptane derivatives and optically active intermediates thereof

A 1,6-&#x3b2;-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-&#x3b2;-glucan synthesis inhibition. Also provided is a drug, a salt or hydrate thereof, especially an antifungal that contains the compound. Concretely, provided is a compound of the following formula (I), its salt or hydrate, and a drug or antifungal containing, as the active ingredient, the compound, its salt or hydrate: 

Antifungal bicyclic hetero ring compounds

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Edogawa-ku, Japan

Junichi Kuroyanagi