Shionogi Company Limited

Baylor College of Medicine

Other

E-Na Biotec Inc.

Kitade, Yukio

Akao, Yukihiro

Akira Kugimiya

Yuki Tachibana

Yasunori Mitsuoka

Motonari Uesugi

Takami Murashi

Salih J Wakil

Lutfi Abu-Elheiga

Masahiko Fujioka

Naohiro Onodera

Mitsuaki Sekiguchi

Qian Mao

Shinji Kamisuki

Tetsuya Tanino

Norikazu Kuroda

Jun Nakamura

Koji Masuda

Manabu Katou

Naoki Yoshikawa

Yoshiharu Hiramatsu

Nobuyuki Tanaka

Shiro Kida

Katsutoshi Aono

Itsuo Makino

Natsuki Ishizuka

Kyohei Hayashi

Mado Nakajima

Yukihiro Akao

Yukio Kitade

Aiko Yamashita

Yasuo Sasaki

Michitaka Shichijo

Teruhisa Ichinashi

Yasuharu Kato

Takeshi Kasuya

Kato Yasuharu

Kouji Masuda

The purpose of the present invention is to provide novel complexes that improve the effect of nucleic acid medicines. Provided is a complex in which a multibranched lipid(s) binds through a linker to a strand of an oligonucleotide comprising a nucleic acid medicine having suppressing activity of the target gene expression.

Complex of nucleic acid medicine and multibranched lipid

The purpose of the present invention is to provide novel miR-143 derivatives described herein that can be used as oligonucleotide therapeutics.

MicroRNA-143 derivative

The purpose of the present invention is to provide double-stranded oligonucleotides comprising the CpG oligonucleotide mentioned below, as a nucleic acid derivative having an immunostimulatory activity. An adjuvant comprising a double-stranded oligonucleotide, wherein

Nucleic acid derivative having immunostimulatory activity

The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): 

Sulfonamide derivative having PGD2 receptor antagonistic activity

The present invention provides compounds shown by the formula: whereinYis CRor N,Yis CRor N,Yis CRor N,R, Rand Rare each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like,Bx is a nucleic acid base moiety,Zand Zare each independently, a hydrogen atom, a hydroxyl protecting group or a reactive phosphorus group,Rto Rare each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, andn is an integer of 0 to 3,or salts thereof, that are novel nucleosides or nucleotides that can be useful as materials for synthesizing nucleic acid pharmaceuticals.

Nucleoside and nucleotide having nitrogen-containing heterocycle structure

Disclosed is a compound which is useful as an endothelial lipase inhibitor. A pharmaceutical composition having inhibitory activity on endothelial lipase comprising a compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof,wherein

Acetic acid amide derivative having inhibitory activity on endothelial lipase

The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.

Compositions and methods for the treatment of metabolic disorders

The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (I): 

Indolecarboxylic acid derivative having PGD2 receptor antagonistic activity

The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (I):  wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of -X=X-X=X- is a formula of &#x2014;C(R)&#x2550;C(R)&#x2014;C(R)&#x2550;C(R)&#x2014; etc.; Xis C(R) or N; R, R, R, Rand Ris independently a hydrogen atom, a halogen atom etc; Ris a formula of -Z-Retc. wherein Z is alkylene etc., and Ris carboxy etc.; Ris optionally substituted alkyloxy etc.; Ris independently a halogen atom etc.; Ris independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or a solvate thereof.

The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the generic formula (I)  wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R, R, R, Rand Rare independently a hydrogen atom or a halogen atom etc.; Ris C2-C4 alkyloxy etc.; Ris independently a halogen atom etc.; Ris independently C1-C4 alkyl etc.; Ris carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L, Land Lare a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.

Indole derivative having PGD2 receptor antagonist activity

The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases. A compound of the general formula (I) 

Azaindole derivative having PGD2 receptor antagonistic activity

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Osaka, Japan

Akira Kugimiya