Kyorin Pharmaceutical Co., Ltd.

Kyorin Pharameuticals Co., Ltd.

Koji Murakami

Masaki Tsunoda

Masahiro Nomura

Katsuya Awano

Tomohiro Ide

Hiroya Satoh

Yasumichi Fukuda

Yoshikazu Asahina

Susumu Kinoshita

Toshio Maeda

Hiroyuki Miyachi

Takahiro Tanase

Michiro Ohnota

Yoshihiro Hirata

Kazuya Yokota

Kohei Ohata

Kyuya Okamura

Shizuyoshi Fujimori

Mitsuo Ohashi

Yukie Takahashi

Toshiyuki Matsui

Yasuo Takano

Kazuhiro Yumoto

Shigeki Isogai

Yunike Akasaka

Mashiro Nomura

Taku Shibue

Takashi Kadowaki

Toshiro Mochizuki

Satoru Katayama

Masakatsu Komuro

Takehiro Shinozaki

Takashi Komine

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

Summary Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. Solving Means The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[(N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).

Bicycloester derivative

The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPAR&#x3b1; isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds. A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C-Calkylene, C-Calkenylene, C-Calkynylene, or the like; Z represents an oxygen atom, sulfur atom or &#x2014;(CH)&#x2014; (n represents 0, 1 or 2); X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and &#x2014;COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.

Cyclic amino benzoic acid derivative

Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).

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

Substituted benzylthiazolidine-2,4-dione derivatives

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 benzylthiazolidine-2, 4-dione derivatives

O-anisamide derivatives

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

The present invention provides novel N-benzyldioxothiazolidylbenzamide derivatives that improve the insulin resistance and have potent hypoglycemic and lipid-lowering effects and processes for preparing the same, and relates to N-benzyldioxothiazolidylbenzamide derivatives characterized by being represented by a general formula (1) ##STR1## [wherein R.sup.1 and R.sup.2 denote identically or differently hydrogen atoms, lower alkyl groups with carbon atoms of 1 to 4, lower alkoxy groups with carbon atoms of 1 to 3, lower haloalkyl groups with carbon atoms of 1 to 3, lower haloalkoxy groups with carbon atoms of 1 to 3, halogen atoms, hydroxyl groups, nitro groups, amino groups which may be substituted with lower alkyl group(s) with carbon atoms of 1 to 3 or hetero rings, or R.sup.1 and R.sup.2 link to form a methylenedioxy group, R.sup.3 denotes a lower alkoxy group with carbon atoms of 1 to 3, hydroxyl group or halogen atom, and dotted line indicates double bond or single bond in combination with solid line], and processes for preparing the same.

N-benzyldioxothiazolidylbenzamide derivatives and process for producing

Growing community of inventors

Tochigi, Japan

Koji Murakami