Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Seiji Yoshikawa

Nobuyuki Yasuda

Hironori Ikuta

Seiichi Kobayashi

Richard S Clark

Osamu Asano

Manabu Murakami

Hitoshi Harada

Takashi Inoue

Kazuto Yamazaki

Tadashi Nagakura

Junsaku Nagaoka

Tatsuo Horizoe

Yorihisa Hoshino

Nobuhisa Watanabe

Fumiyoshi Matsuura

Kazunobu Kira

Toshimi Okada

Eita Emori

Kaya Ohashi

Shigeto Negi

Keigo Tanaka

Naoyuki Shimomura

Kenji Hayashi

Tsutomu Kawata

Masashi Ito

Toshihiko Naito

Toshikazu Shimizu

Takao Saeki

Isao Tanaka

Daisuke Shinmyo

Hironobu Hiyoshi

Naoki Ozeki

Nobuyuki Kurusu

Hiroe Minami

Toyokazu Haga

Mamoru Yanagimachi

Hiroshi Akamatsu

Kaya Nagata

Taisuke Uehara

Mika Koyanagi

Mika Aoki

Methods of the present invention for producing dibromofluorobenzene derivatives (compounds II) comprise Step 1, in which compounds (I) having the following general formula (I):  (wherein, Rand Reach independently represent a Calkyl group) are reacted in a solvent with a brominating reagent.

Methods for producing dibromofluorobenzene derivatives

The present invention is related to compounds represented by the following formula, or salts or hydrates thereof  These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.

Condensed imidazole derivatives

The objective of this invention is to provide novel compounds that show excellent DPPIV-inhibiting activity. The present invention provides compounds represented by the general formula (I), salts thereof, or hydrates thereof, [wherein, represents a double bond or a single bond; Xdenotes an oxygen atom or a sulfur atom; Xdenotes a Calkyl group which may have substituents; Zdenotes a nitrogen atom or the formula &#x2014;CR=; Zand Zeach independently denote a nitrogen atom, the formula &#x2014;CR=, a carbonyl group, or the formula &#x2014;NR&#x2014;; R, R, R, and Xeach independently denote a Calkyl group which may have substituents, and such].

Fused 1,3-dihydro-imidazole ring compounds

The present invention relates to use of 1-carbamoylazole derivatives as medicaments and pharmaceutical compositions containing 1-carbamoylazole derivatives as the active ingredient, based on their DPPIV inhibiting effects. The present invention provides a dipeptidyl peptidase IV inhibiting agent comprising a compound represented by the general formula (I): 

Pharmaceutical use of N-carbamoylazole derivatives

An excellent squalene synthase inhibitor is provided. Specifically, what is provided is a compound (I) represented by the following formula, a salt thereof or a hydrate of them. In formula (I), Rrepresents an optionally substituted vinyl group or an aromatic ring which may be substituted. Also, n is an integer of 0 to 2. Further, X, Y and Z are the same as or different from each other and each represents an optionally substituted carbon atom, or an optionally substituted nitrogen atom, sulfur atom or oxygen atom, and Y optionally represents a single bond, and when Y represents the single bond, the ring to which X, Y and Z belong is a 5-membered ring. Also in the formula, CyA represents a 5- to 14 membered non-aromatic cyclic amino group or non-aromatic cyclic amido group which may be substituted, and the non-aromatic cyclic amino group or the non-aromatic cyclic amido group optionally having an oxygen atom or a sulfur atom. Finally, W represents a chain 

N-aryl-substituted cyclic amine derivative and medicine containing the same as active ingredient

The present invention provides novel compounds exhibiting an excellent DPPIV inhibition effect. The compounds are represented by the formula: wherein, m is 0 or 1;

Xanthine derivative and DPPIV inhibitor

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

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Kashima-gun, Japan

Seiji Yoshikawa