Wakunaga Pharmaceutical Co., Ltd.

Wakunaga Seiyaku Kabushiki Kaisha

Fujisawa Pharmaceutical Company, Ltd.

Wakunaga Yakuhin Kabushiki Kaisha

Wakunaga Pharmaceuticals Co., Ltd.

Akira Yazaki

Norihiro Hayashi

Yasuhiro Kuramoto

Hirotaka Amano

Yuzo Hirao

Yoshiko Niino

Yoshihiro Ohshita

Satoshi Inoue

Masaharu Yokomoto

Shunso Hatono

Jiro Yoshida

Kenji Itoh

Susumu Yoshida

Takashi Yatsunami

Shuichiro Noda

Shunsou Hatono

Kazuo Sakane

Masayoshi Murata

Hideo Tsutsumi

Iwao Tabushi

Hiromichi Matsuura

Hiroyuki Sugimoto

Takeshi Terasawa

David Barrett

Nobuya Sakae

Jun Nomiyama

Tatsuya Hirano

Tomonori Yamaguchi

Tsuyoshi Ushiroguchi

Kuramoto Yasuhiro

Haruyo Mochizuki

Shizutoshi Nakagawa

Shinobu Maruyama

Noda Shuichiro

Hitodshi Yamamoto

Hitoshi Yamamoto

Tamae Yamane

Yoshihiro Oshita

Hitomi Takenaka

Takayuki Amago

Kazusa Yoshikai

Taichi Ueshima

Junpei Yamashita

Masayuki Sato

Yohei Kawakubo

Rumiko Shimabara

It is intended to provide a novel compound having high antitumor activity and low toxicity to normal cells. The present invention provides a pyridone carboxylic acid derivative represented by the following formula (1) or a salt thereof wherein Rrepresents a hydrogen atom, a halogen atom or the like; Rrepresents a hydrogen atom, a halogen atom or the like; Rto Reach represent a hydrogen atom or the like; Rrepresents a hydrogen atom or the like; Rrepresents a hydrogen atom, a halogen atom, the following formula (a) (wherein Rand Reach represent a hydrogen atom, a hydroxy group, an optionally substituted lower alkyl group or the like) or the like, or Rand Rtogether represent &#x2550;N&#x2014;OR(wherein Rrepresents a hydrogen atom, an optionally substituted lower alkyl group, or an aralkyl group), or Rand Rform an optionally substituted 4- to 6-membered saturated hetero ring together with the adjacent carbon atom, or the like; Rrepresents a hydrogen atom or the like; X represents a nitrogen atom or the like; and Y represents a nitrogen atom or the like. 

Pyridone carboxylic acid derivative or salt thereof

The present invention provides an agent which exhibits excellent antibacterial activity, low toxicity, improved bioavailability, and low binding rate to serum proteins. The present invention is directed to a pyridonecarboxylic acid derivative represented by formula (1): or a salt thereof, wherein Rrepresents a methyl group, a fluorine atom, or a chlorine atom; Rrepresents a hydrogen atom or a lower alkyl group; Rrepresents an isopropyl group or a tert-butyl group; Rrepresents a methyl group or a halogen atom; and Rrepresents a fluorine atom or a chlorine atom. The present invention is also directed to an antibacterial agent and a medicament containing the derivative or the salt thereof as an active ingredient.

Pyridonecarboxylic acid derivatives or salts thereof

This invention relates to 1-(6-amino-3,5-difluoropyridin-2-yl)-8-bromo-7-(3-ethylaminoazetidin-1-yl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a salt thereof, and also to a medicine containing the same. This compound has characteristic features that, when administered orally, it has extremely high blood half-life and bioavailability while retaining properties that it has extremely high antimicrobial effects and has low toxicity. It can be used widely as preventives, therapeutics and the like for various infectious diseases of human and animals.

Quinolinecarboxylic acid derivative or salts thereof

The present invention relates a 1-(6-amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-hydroxyazetidin-1-yl)-8-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or salt thereof; and drugs containing the same as the active ingredient. Since this compound or salt thereof is highly stable to light while sustaining the excellent properties inherent to quinolone antibacterial agents, an antibacterial agent comprising, as an active ingredient, the invention compound or salt thereof can be stored over a long period of time without suffering from any decrease in the drug effect and can therefore be supplied as stable preparations such as injections, eye drops and surgical medicines.

Quinolinecarboxylic acid derivative or its salt

Pyridonecarboxylic acid derivatives or salts thereof and antibacterial agents containing the same as the active ingredient

A pyridonecarboxylic acid derivative represented by the following general formula (1): ##STR1## [wherein R.sup.1 represents hydrogen atom or a carboxyl protective group; R.sup.2 represents hydroxyl group, a lower alkoxy group, or a substituted or unsubstituted amino group; R.sup.3 represents hydrogen atom or a halogen atom; R.sup.4 represents hydrogen atom or a halogen atom; R.sup.5 represents a halogen atom or an optionally substituted saturated cyclic amino group; R.sup.6 represents hydrogen atom, a halogen atom, nitro group, or an optionally protected amino group; X, Y and Z may be the same or different and respectively represent nitrogen atom, --CH.dbd. or --CR.sup.7 .dbd. (wherein R.sup.7 represents a lower alkyl group, a halogen atom, or cyano group) (with the proviso that at least one of X, Y and Z represent the nitrogen atom), and W represents nitrogen atom or --CR.sup.8 .dbd. (wherein R.sup.8 represents hydrogen atom, a halogen atom, or a lower alkyl group)] or its salt, as well as an antibacterial agent containing such compound are provided.

Pyridonecarboxylic acid derivatives or their salts, and antibacterial

Pyridonecarboxylic acid derivatives or salts thereof and drugs

Pyridonecarboxylic acid derivatives or their salts and antibacterial

Phenylenediamines and process for preparing the same

Pyridonecarboxylic acid derivatives or salts thereof and antibacterial

Quinolone derivative or salt thereof and antibacterial containing the

A tricyclic compound represented by the general formula (1) and salts thereof are disclosed. ##STR1## A method for producing the tricyclic compound and salts thereof, and an antimicrobial agent containing the tricyclic compound and salts thereof as an active ingredient are also disclosed.

Tricyclic compound or salts thereof, method for producing the same and

Certain tricyclic pyrido[3,2,1-ij]cinnoline-8-carboxylates, useful as

A tricyclic compound represented by the general formula (1) and salts thereof. ##STR1## A method for producing the tricyclic compound and salts thereof, and an antimicrobial agent containing the tricyclic compound and salts thereof as an active ingredient are also disclosed.

Growing community of inventors

Hiroshima, Japan

Akira Yazaki