Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Osamu Asano

Shuhei Miyazawa

Shinya Abe

Isao Yamatsu

Hiroyuki Yoshimura

Shigeru Souda

Yoshimasa Machida

Naoyuki Shimomura

Tetsuya Kawahara

Mitsuaki Miyamoto

Koukichi Harada

Kazuo Okano

Kouichi Katayama

Tsutomu Kawata

Seiichi Kobayashi

Kouji Yamada

Kenzo Muramoto

Richard S Clark

Hiroshi Obaishi

Hitoshi Harada

Lynn D Hawkins

Daniel P Rossignol

William J Christ

Manabu Murakami

Nobuhisa Watanabe

Takashi Inoue

Masato Ueda

Yoshihiko Kotake

Yorihisa Hoshino

Naoto Ishii

Shigeto Negi

Yasushi Okamoto

Hisashi Shibata

Kenji Hayashi

Jun Niijima

Kazuki Miyazaki

Junichi Nagakawa

Satoshi Katayama

Hajime Tsunoda

Junsaku Nagaoka

Yoshimori Sakuma

Nobuyuki Yasuda

Tsutomu Yoshimura

Hiromasa Suzuki

Seiji Yoshikawa

Tatsuo Horizoe

Masahiro Yasuda

Takao Saeki

Tadashi Nagakura

Kaya Ohashi

Takayuki Hida

Yasuhiro Kabasawa

Atsushi Inoue

Toshihiko Naito

Kazumasa Nara

Toshikazu Shimizu

Yasutaka Takase

Isao Tanaka

Kazutomi Kusano

Kimiyo Tabata

Daisuke Iida

Kokichi Harada

Eiichi Yamamoto

Naoki Ozeki

Hiroe Minami

Manabu Shirato

Makoto Nakagawa

Toyokazu Haga

Atsushi Takemura

Masahiro Sakurai

Hisashi Wakita

Kaya Nagata

Hiroshi Akamatsu

Takashi Satoh

Mai Saeki, Legal Representative

Richar S Clark

Naoyuki Kimomura

Tomoko Saeki, Legal Representative

Takao (deceased) Saeki

Kazuo Hirota

Crystals, amorphous substances, salts, and hydrates of a salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid having PDE4 inhibitory action are provided. These compounds are useful for treating allergic diseases such as atopic dermatitis.

Crystals, amorphous substances or salts of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl) phenyl] terephthalamic acid

A compound represented by the following formula (I), salt thereof, or hydrate thereof, can effectively relieve itch caused by atopic disease or the like: wherein R represents hydroxyl, Calkoxy optionally substituted with Calkoxy, or amino optionally substituted with Calkyl.

4-(3-benzoylaminophenyl)-6,7-dimethoxy-2-methylaminoquinazoline derivatives

A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. [wherein Rrepresents hydrogen, Rrepresents optionally substituted phenyl, etc., Rrepresents optionally substituted C6-10 aryl, etc.].

2,3-dihydro-iminoisoindole derivatives

The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine Areceptor antagonism, preferably an adenosine Areceptor antagonism, or a salt thereof.

Medicinal compositions promoting bowel movement

The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A, A, and Areceptors), particularly, compounds represented by the general formula (1), salts thereof, or solvates of both: (1) wherein Rand Rare each independently hydrogen, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, Ccycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a Caromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, Cacyl, or Calkylsulfonyl; Ris hydrogen, Calkyl, Calkenyl, or Calkynyl; Ris a Caromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and Ris a Caromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).

Pyrimidone compounds and pharmaceutical compositions containing the same

The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is &#x2014;CHCH&#x2014;, or &#x2014;CH&#x2550;CH&#x2014; or &#x2014;C&#x2261;C&#x2014;; Ris:(in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and Rand Rare the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; Ris an amino group, etc. which maybe substituted with a lower alkyl group, etc.; Ris a cycloalkyl group, an optionally substituted aryl group, etc.; and Ris a lower alkyl group etc.

Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes

Amidino derivatives represented by the following general formula (I):{where X is a group represented by RSONR&#x2014; (wherein Rrepresents optionally substituted Caryl, etc. and Rrepresents hydrogen atom, etc.), etc., Arrepresents 2,6-naphthylene, etc., Rrepresents hydrogen atom, etc. and Y represents carboxyphenyl, etc.}and their pharmacologically acceptable salts or solvates.

Amidino derivatives and anticoagulants and thrombosis therapeutic agents containing them

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 class of substituted compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), wherein R is selected from hydrido, halo, alkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R and R are one more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R and R is substituted with alkysulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.

2-aminopyridine compounds and use thereof as drugs

Disclosed are lipid A analogs useful for the treatment of septic shock and LPS-mediated activation of viral infection.

Anti-endotoxin compounds

A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are useful in the pharmaceutical field, especially in treating allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

1,4-diazepine derivative and its pharmaceutical use

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Tsukuba, Japan

Osamu Asano