Eisai Company, Limited

Junsaku Nagaoka

Naoyuki Shimomura

Tsutomu Kawata

Shigeru Souda

Shuhei Miyazawa

Osamu Asano

Shinya Abe

Isao Yamatsu

Hiroyuki Yoshimura

Yoshimasa Machida

Tetsuya Kawahara

Mitsuaki Miyamoto

Koukichi Harada

Kazuo Okano

Kouichi Katayama

Tsutomu Yoshimura

Hiromasa Suzuki

Norihiro Ueda

Seiichi Kobayashi

Takashi Yamanaka

Manabu Murakami

Ieharu Hishinuma

Junichi Nagakawa

Hitoshi Harada

Takashi Inoue

Tsuneo Wakabayashi

Nobuyuki Yasuda

Kaname Miyamoto

Tatsuo Horizoe

Seiji Yoshikawa

Hidetoshi Kawashima

Naoko Nagaoka

Yorihisa Hoshino

Kaya Ohashi

Shigeto Negi

Kenji Hayashi

Nobuhisa Watanabe

Toshihiko Naito

Toshikazu Shimizu

Isao Tanaka

Hiroe Minami

Naoki Ozeki

Toyokazu Haga

Hiroshi Akamatsu

Kaya Nagata

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

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 glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor. ##STR1##

Glycerin derivative and its pharmacological use

A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:

Guanidinobenzoic ester derivative

A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m--, m being an integer of 2 or 3, ##STR3## or a group of the formula:

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Ibaraki, Japan

Junsaku Nagaoka