Eisai Company, Limited

Toshihiko Naito

Shigeto Negi

Isao Sugiyama

Hiroshi Yamauchi

Yuuki Komatu

Takashi Kamiya

Yoshimasa Machida

Takaharu Nakamura

Kanemasa Katsu

Yasunobu Kai

Seiichiro Nomoto

Kyosuke Kitoh

Hitoshi Oinuma

Akihiko Tsuruoka

Itaru Tsukada

Sachiyuki Hamano

Yoshiharu Daiku

Kazumasa Nara

Katsura Hata

Kenichi Nomoto

Takashi Hasegawa

Tadanobu Takamura

Yumiko Kaku

Manabu Yanagisawa

Toshio Toyosawa

Naoyuki Shimomura

Seiichi Kobayashi

Osamu Asano

Kenji Hayashi

Manabu Murakami

Nobuhisa Watanabe

Tsutomu Kawata

Hitoshi Harada

Takashi Inoue

Toshikazu Shimizu

Manabu Sasho

Nobuyuki Yasuda

Junsaku Nagaoka

Tatsuo Horizoe

Seiji Yoshikawa

Isao Tanaka

Naoki Ozeki

Hiroe Minami

Kaya Ohashi

Toyokazu Haga

Hiroshi Akamatsu

The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action. That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I);(wherein Rrepresents e.g. an amino group which may be substituted with an alkyl group; Rrepresents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; Rrepresents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.

Condensed imidazole compounds and a therapeutic agent for diabetes mellitus

A compound represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 denote a halogen atom or hydrogen atom; R.sup.3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic ring, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for --S--, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmaceutical composition suitable for use as an antifungal agent.

Antifungal agents, processes for the preparation thereof, and

A compound represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 denote a halogen atom or hydrogen atom; R.sup.3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic ring, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for --S--, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmacetical composition suitable for use as an antifungal agent.

A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.

Benzenesulfonamide derivatives

Antifungal agents, and compositions

A cephalosporin derivative represented by the formula: ##STR1## wherein R.sub.1 represents a lower alkyl group, and A is selected from: a group of the following formula: ##STR2## where R.sub.2 and R.sub.3 are the same or different lower alkyl group, R.sub.4 represents a substituted lower alkyl or amino group; a group which may be substituted and which is represented by the following formula: ##STR3## where R.sub.5 represents a lower alkyl group; or a group of the following formula: ##STR4## where R.sub.5 is as defined above, R.sub.6 represents a hydroxyl lower alkyl or carboxyl group, or its pharmacologically acceptable salt, and a process for preparing the same, as well as an antibacterial agent containing the same.

7Beta-(thiadiazolyl)-2-iminoacetamido-3cephem compounds

A cephem derivative represented by the following formula: ##STR1## wherein R.sub.1 means a fluorine-substituted lower alkyl and A.sub.1 denotes a cyclic or acyclic ammonio group, or a non-toxic salt thereof, is prepared by reacting a compound represented by the following formula: ##STR2## wherein A.sub.1 has the same meaning as defined above, with another compound represented by the following formula: ##STR3## wherein R.sub.1 has the same meaning as defined above, and if necessary, removing the protecting groups.

Process for the preparation of cephem derivatives and intermediates

A 3-propenylcephem derivative of the following formula: ##STR1## wherein R.sub.1 represents a fluoro-substituted lower alkyl group or a cyano-substituted lower alkyl group, and A represents a cyclic or an acylic ammonio group, or a pharmaceutically acceptable salt thereof, exhibiting excellent anti-bacterial activities against both Gram-positive bacteria and Gram-negative bacteria; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcephem derivative; and Process for the preparation of the intermediate.

3-propenylcephem derivative

Novel thiadiazolylacetamide cephem derivatives of the following formula are described. ##STR1## wherein A represents a quaternary ammonio group; or a pharmaceutically acceptable salt thereof. These novel compounds are useful as antibacterial agents, because they have a broad antibacterial spectrum ranging from gram-negative bacteria to gram-positive bacteria. Processes for the preparation of these novel compounds are also described.

Thiadiazolylacetamide cephem derivatives

Growing community of inventors

Ibaraki, Japan

Toshihiko Naito