Kyorin Pharmaceutical Co., Ltd.

Teijin Pharma Limited

Tomohiro Ide

Koji Murakami

Yasumichi Fukuda

Yoshikazu Asahina

Shinji Kobayashi

Masanori Yamamoto

Fumiyoshi Kobayashi

Kanji Komatsu

Kenji Fujita

Masahiro Nomura

Kohei Ohata

Masaki Tsunoda

Hiroyuki Miyachi

Masanori Takadoi

Ayako Nakamura

Takahiro Tanase

Yukie Takahashi

Kazuya Yokota

Yunike Akasaka

Taku Shibue

Satoru Katayama

Takashi Komine

Takashi Kadowaki

Toshiro Mochizuki

Naoki Kobayashi

A method for screening an AMPK activator, wherein inhibition of an interaction between prohibitin and AMPK is used as an index is provided. Besides, an AMPK activator comprising, as an active ingredient, a compound inhibiting an interaction between prohibitin and AMPK, and a prohibitin-AMPK complex are also provided.

AMPK activator screening method, and AMPK activator

A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; Rand Rare each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C-Calkyl group, a C-Calkoxy group, a C-Calkylsulfanyl group, a C-Calkylsulfinyl group or a C-Calkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.

Glucokinase activator

A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, Rrepresents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C-Calkyl group, or a C-Calkoxy group, Rrepresents a C-Ccycloalkylsulfanyl group, a C-Ccycloalkylsulfinyl group, or a C-Ccycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).

Novel bicycloamide derivatives (general formula (1)) and pharmaceutically acceptable salts thereof effectively inhibit DPP-IV. The bicycloamide derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[(4-carbamoylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).

Bicycloamide derivative

A novel bicyclo derivative represented by the following general formula (1), or a pharmaceutically acceptable salt thereof, acts as an effective DPP-IV inhibitor:  One example is (2S,4S)-1-[[N-(4-methylbicyclo[2,2,2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile).

Bicyclo derivative

The invention creates a very high-novelty medicinal drug for the carbohydrate and lipid metabolism-related diseases by finding out an inhibitory substance or antagonist against PPAR &agr; and PPAR &ggr;, and relates to an application of fatty acid CoA thioester that was found out as an active inhibitory substance against peroxisome proliferator-activated receptor &agr; and &ggr; (hereinafter referred to as PPARs) to the assay of medicinal drug, and a use of fatty acid CoA thioester for medicinal drug.

Fatty acid CoA thioester inhibitory substance of PPAR&agr; and PPAR&ggr;

Substituted phenylpropionic acid derivatives as agonists to human peroxisome proliferator-activated receptor (PPAR) &agr;

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Tochigi, Japan

Tomohiro Ide