Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Kazuto Yamazaki

Richard S Clark

Fumiyoshi Matsuura

Eita Emori

Masanobu Shinoda

Hideki Yoshitomi

Sadakazu Miyashita

Shunji Kasai

Takashi Inoue

Taro Hihara

Hironori Ikuta

Hitoshi Harada

Nobuyuki Yasuda

Tadashi Nagakura

Seiji Yoshikawa

Toshihiko Kaneko

Kazunobu Kira

Toshimi Okada

Norihito Ohi

Koji Sagane

Kaya Ohashi

Eiki Takahashi

Turo Oki

Mika Koyanagi

Mika Aoki

Taro Hibara

Takashi Seiki

It is an object of the present invention to provide a non-human gene-disrupted animal with a disrupted ADAM11 gene. According to the present invention, a non-human gene-disrupted animal, wherein either one of or both alleles of an ADAM11 gene are disrupted, is provided.

Non-human gene-disrupted animal with disrupted ADAM11 gene

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 present invention provides novel carboxylic acid derivatives useful as an insulin sensitizer, a salt thereof or a hydrate of them, and a medicament comprising the derivative as the active ingredient. Specifically, it provides a carboxylic acid derivative represented by the following formula (I): (wherein Y, L, X, T, Z, U, M and W are defined in the specification) and a salt thereof, and ester thereof or a hydrate of them.

Carboxylic acid derivative, a salt thereof or an ester of them, and medicament comprising it

Carboxylic acid compound or salt or hydrate thereof useful as insulin sensitizer, represented by the formula wherein Rrepresents hydrogen, hydroxyl, halogen, carboxyl, or Calkyl, L represents single bond or C-alkylene, C-alkenylene, or C-alkynylene, M represents single bond or C-alkylene, C-alkenylene, or C-alkynylene, T represents single bond, or C-alkylene, C-alkenylene, or C-alkynylene, W represents carboxyl, represents single bond, X represents single bond, oxygen, &#x2014;NRCQO&#x2014;, &#x2014;OCQNR&#x2014;, &#x2014;CQNRO&#x2014;, ONRCQ&#x2014;, &#x2014;QSO&#x2014;, or &#x2014;SOQ&#x2014;, Y represents 5- to 14-membered aromatic group, and ring Z represents 5- to 14-membered aromatic group.

Carboxylic acid derivative and salt thereof

The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein a, b and c are the same as or different from one another and each represents 0 to 4; Rto Rare the same as or different from one another and each represents a hydrogen atom, a hydroxyl group, a cyano group, a halogen atom, etc.; represents a single bond or a double bond;

Cyclic compound and PPAR agonist

The present invention provides a novel carboxylic acid derivative, a salt thereof or a hydrate of them which is useful as an insulin sensitizer, and a medicament comprising the derivative as the effective ingredient. More specifically, it provides a carboxylic acid compound represented by the formula (I), a salt thereof or a hydrate of them. In the formula, Ar represents a 6- to 14-membered aromatic ring group which may have at least one substituent; R, R, R, R, R, R, Rand Rare the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a Calkyl group or a Calkoxy group; X represents an oxygen atom or a methylene group; Y represents a group represented by the formula (II) or (III): (wherein Z represents a group represented by the formula (IV): (wherein R, R, Rand Rare the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a Calkyl group or a Calkoxy group)); m is 0 or 1; and n is 0 or 1.

Carboxylic acids

The present invention provides a medicament comprising a benzene compound useful as an insulin sensitizer, a salt thereof or a hydrate of them and a derivative of them as the active ingredient. Specifically, it provides a benzene compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, X represents 1) a Caryl group which may have one or more substituents or 2) a 5- to 10-membered heteroaryl group which may have one or more substituents; Y represents a group represented by the formula: (in the above formulae, R, Rand Rare the same as or different from one another and each represents a hydrogen atom, a halogen atom, a Calkyl group, a Calkoxy group, or a Ccycloalkyl group) etc.; Z represents a group represented by the formula: (in the formula, m represents an integer of 0 to 2; R, Rand Rare the same as or different from one another and each represents a hydrogen atom, a halogen atom, a Calkyl group, a Calkoxy group, a Ccycloalkyl group, a halogenated Calkyl group, a halogenated Calkoxy group etc.); and R, R, Rand Rare the same as or different from one another and each represents a hydrogen atom, a halogen atom, a Calkyl group, a Calkoxy group, a Ccycloalkyl group etc.

Benzene compound and salt thereof

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

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

Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, Ris hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, &#x2014;CON(R)R, or the like;represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.

Growing community of inventors

Ibaraki, Japan

Kazuto Yamazaki