Ajinomoto Co., Ltd.

Sanofi-A Ventis Deutschland Gmbh

Ea Pharma Co., Ltd.

Naoyuki Fukuchi

Morikazu Kito

Naoyuki Yamada

Toshihiko Yoshimura

Fumie Futaki

Satoru Okamoto

Hideyuki Tanaka

Koichi Ishii

Katsumi Maezono

Takao Ikenoue

Takashi Kayahara

Masaru Takayanagi

Wataru Miyanaga

Sen Takeshita

Akiko Tanaka

Yumiko Fukuda

Nozomu Ishida

Yayoi Kawato

Akiko Oonuki

Naoko Arashida

Hiroshi Yamamoto

Hideki Matsumoto

Melitta Just

Otmar Klingler

Munetaka Tokumasu

Sayaka Asari

Eiichiro Suzuki

Kohki Ishikawa

Itsuya Tanabe

Kuniya Sakurai

Nobuhisa Shimba

Keiko Gondoh

Tsuyoshi Kobayashi

Takashi Yamamoto

Seiichi Sato

Koji Ohsumi

Manabu Kitazawa

Masayuki Sugiki

Toshihiro Hatanaka

Ryota Yoshimoto

Akira Chiba

Mitsuo Takahashi

Shingo Makino

Yasuko Jojima

Satoshi Iwayama

Yukitsugu Ono

Shinichi Fujita

Koichi Fujita

Tetsuo Yano

Masataka Shoji

Yoichiro Shima

Misato Noguchi

Shunsuke Kageyama

Youji Yamada

Osamu Ikehara

Mitsuyo Nagano

Masaki Hashimoto

Haruko Hirashima

Junko Shinozaki

Chiori Ijichi

Yasuko Nogi

Takayuki Kajiura

Yuka Kataba

Naoko Oomuta

Yuko Iida

A method of screening a compound having a hypoglycemic effect (hereinafter referred to as 'hypoglycemic compound'), a remedy for diabetes which contains a compound having a novel function mechanism, etc. More specifically speaking, a method of screening a hypoglycemic compound capable of binding to the &#x3b2; subunit of a trimeric GTP-binding protein, a remedy for diabetes comprising a hypoglycemic compound, which is characterized by being capable of binding to the &#x3b2; subunit of a trimeric GTP-binding protein, as the active ingredient, etc.

Remedy for diabetes

It is intended to provide an assay method whereby the activity of a lipid-modifying enzyme can be conveniently measured over a wide range and a drug capable of controlling a lipid-modifying enzyme with the use of this assay method. The above problem can be solved by, for example, a method of measuring the activity of a lipid-modifying enzyme which comprises the steps of (I) preparing a lipid micelle containing a biotinylated lipid and a substrate for the lipid-modifying enzyme; (II) bringing the lipid micelle prepared in the above step (I) into contact with the lipid-modifying enzyme; and (III) evaluating the activity of the lipid-modifying enzyme by applying an evaluation method using the proximity effect to the product obtained in the above step (II).

Method of measuring the activity of lipid-modified enzyme

The present invention provides PPAR (peroxisome proliferator-activated receptor) activity regulators, which can be widely used for improving insulin resistance and preventing/treating various diseases such as diabetes, metabolic syndromes, hyperlipemia, high-blood pressure, vascular disorders, inflammation, hepatitis, fatty liver, liver fibrosis, NASH (non-alcoholic steatohepatitis) and obesity.

PPAR activity regulators

The present invention provides a novel compound having a kininogenase-inhibitory action and its pharmaceutical use. The compounds are represented by the formulas (A), (B), (C), (E) and (H): wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.

Aniline derivatives

The present invention relates to compounds of the formula I, in which R1, R2, A, B, D, E, n, m or o have the meanings indicated below. The compounds of the formula I are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb). They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of atherothrombotic diseases.

Inhibitors of the GPIb-vWF interaction, their preparation and use

The present invention provides an acylamide compound of the following formula (1), prodrugs thereof, or pharmaceutically acceptable salts thereof; and an adiponectin inducer or secretagogue, therapeutic agent of metabolic syndromes, therapeutic agent of hypoadiponectinemia, therapeutic agent of hyperlipemia, preventive/therapeutic agent of diabetes, improving agent of impaired glucose tolerance, improving agent of insulin resistance, enhancing agent of insulin sensitivity, therapeutic agent of hypertension, preventive/therapeutic agent of vascular disorders, an anti-inflammatory agent, therapeutic agent of hepatic inflammation, therapeutic agent of fatty liver, therapeutic agent of hepatic fibrosis, therapeutic agent of liver cirrhosis, preventive/therapeutic agent of non-alcoholic/nonviral steatohepatitis (NASH) or non-alcoholic/nonviral fatty liver disease (NAFLD), or therapeutic agent of obesity, each of which has the above compounds as an active ingredient. 

Acylamide compounds having secretagogue or inducer activity of adiponectin

The object of the present invention is to provide PPAR (peroxisome proliferator-activated receptor) activity regulators, which can be widely used for improving insulin resistance and preventing/treating various diseases such as diabetes, metabolic syndromes, hyperlipemia, high-blood pressure, vascular disorders, inflammation, hepatitis, fatty liver, liver fibrosis, NASH (non-alcoholic steatohepatitis) and obesity. The present invention provides PPAR activity regulators which comprise an acylamide compound having the specific structure, prodrugs thereof, or pharmaceutically acceptable salts thereof.

The present invention provides a piperidine derivative represented by the following formula or analogs thereto, which are used for agents for treating or preventing various diseases related to 5-HT7. 

Piperidine derivative

A method for conveniently detecting binding between the von Willebrand factor and glycoprotein Ib and a means to be used therein. The von Willebrand factor fixed in a reactor immobilized in a reaction vessel in the presence of bottrocetin is bound to a chimeric protein constructed by fusing the carboxyl terminal of a partial protein containing the von Willebrand factor-binding site of glycoprotein Ib with the amino terminal of the Fc region of an immunoglobulin molecule. Then the Fc region of the above immunoglobulin molecule is detected to thereby detect the binding between the von Willebrand factor and the glycoprotein Ib or inhibition of this binding.

Substance with antithrombotic activity and method for detecting glycokallidin

Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.

Azole compound

It is provided a method for producing a subunit peptide originating from an oligomeric protein having disulfide bonds within a subunit and between subunits. The method comprises producing a subunit originating from an oligomeric protein having disulfide bonds within a subunit and between subunits by the following steps:

Process for producing subunit peptide originating in polymer protein

The present invention relates to compounds of the formula I, in which R1, R2, A, B, D, F, n, m and o have the meanings indicated herein. The compounds of the formula I are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb). They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of atherothrombotic diseases 

Inhibitors of the GPIb&#x2014;vWF interaction, their preparation and use

A method for producing a protein having an antithrombotic activity, which comprises replacing, in a protein that has an amino acid sequence having a homology of not less than 30% to the amino acid sequence of SEQ ID NO: 1 and forms a higher order structure composed of a first &#x3b2; strand (&#x3b2;1), a first a helix (&#x3b1;1), a second &#x3b1; helix (&#x3b1;2), a second &#x3b2; strand (&#x3b2;2), a loop, a third &#x3b2; strand (&#x3b2;3), a fourth &#x3b2; strand (&#x3b2;4) and a fifth &#x3b2; strand (&#x3b2;5) in this order from the amino terminus, at least one amino acid residue in a region from &#x3b1;2 to &#x3b2;2 and/or a region from &#x3b2;3 to &#x3b2;4 so that electric charge of the amino acid residue is changed towards positive direction.

Protein having antithrombotic activity and method for producing the same

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Kawasaki, Japan

Naoyuki Fukuchi