Shionogi Company Limited

Eiichi Kojima

Yu Hinata

Koji Masuda

Manabu Katou

Tomoyuki Ogawa

Nobuyuki Tanaka

Masahiko Fujioka

Masafumi Iwatsu

Keisuke Tonogaki

Akira Ino

Toru Yamada

Hiroyuki Kai

Naotake Kobayashi

Yuusuke Tamura

Naoki Ohyabu

Shuichi Sugiyama

Naoki Yoshikawa

Toshihiro Wada

Noriyuki Kurose

Shiro Kida

Terukazu Kato

Hiroki Ozasa

Mado Nakajima

Mitsuhiro Yonehara

Hidaka Ikemoto

Mikayo Hayashi

Provided are a novel compound having an antagonistic activity for the P2Xreceptor, and a pharmaceutical composition having an antagonistic activity for the P2Xreceptor. A compound represented by Formula (I): wherein Zis C(R) or the like; Ris a hydrogen atom or the like; Zis C(R)(R) or the like; the dashed line represents the presence or absence of a bond; when the dashed line represents the presence of a bond, then Ris absent; Rand Rare each independently a hydrogen atom or the like; Ring Q is a substituted or unsubstituted 5-membered non-aromatic heterocycle or the like; Yis O or the like; Ris a group represented by the formula: &#x2014;(C(R)(R))&#x2014;R; Ris a hydrogen atom or the like; Rand Ris each independently a hydrogen atom or the like; Ris substituted or unsubstituted aromatic carbocyclyl or the like; X is N(R) or the like; Ris a hydrogen atom or the like; Ris substituted or unsubstituted aromatic carbocyclyl or the like; n is an integer from 0 to 4; and m is an integer from 0 to 4, or a pharmaceutically acceptable salt thereof.

Bicyclic nitrogen-containing heterocyclic derivatives and pharmaceutical composition comprising the same

Provided are a novel compound having an antagonistic activity for the P2Xreceptor, and a pharmaceutical composition having an antagonistic activity for the P2Xreceptor. The compound represented by Formula (I): wherein the symbols are defined in the specification, or a pharmaceutically acceptable salt thereof.

A compound of formula: or its pharmaceutically acceptable salt. L is NRR, SR, SOR, alkyl, or alkenyl; Ris hydrogen, alkyl, alkenyl, or alkynyl; Ris hydrogen, alkyl, alkenyl, alkynyl; Ris hydrogen, alkyl, alkenyl, or alkynyl; Ris hydrogen, alkyl, alkenyl, or alkynyl, provided that Ris not unsubstituted methyl or trifluoromethyl; Y is alkyl, alkenyl, alkynyl, aryl, provided that Y is not unsubstituted methyl or unsubstituted ethyl; Z is &#x2014;CR&#x2550;, or &#x2014;N&#x2550;; Ris hydrogen, or alkyl; R, Rand Rare each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, alkyl, alkenyl, or alkynyl.

Heterocyclic derivative having AMPK-activating activity

Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or a pharmaceutically acceptable salt thereof,

Azabenzimidazole derivative having AMPK-activating activity

Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or its pharmaceutically acceptable salt,whereinX is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, or substituted or unsubstituted heterocyclyl;Ris hydrogen, halogen, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted acyl, substituted or unsubstituted carbamoyl, substituted or unsubstituted alkylthio, substituted or unsubstituted alkylsulfinyl, substituted or unsubstituted alkylsulfonyl, or substituted or unsubstituted alkyloxycarbonyl;Ris halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl, or the like;Ris halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl, or the like; andRis hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like.

Azaindole derivative having AMPK-activating activity

A compound is represented by formula: or its pharmaceutically acceptable salt, wherein Y is substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, or heterocyclyl; T is &#x2014;CR&#x2550; or &#x2014;N&#x2550;; U is &#x2014;CR8&#x2550; or &#x2014;N&#x2550;; Ris hydrogen, halogen, cyano, nitro, carboxy, substituted or unsubstituted alkyl, alkenyl, acyl, carbamoyl, alkylthio, alkylsulfinyl, alkylsulfonyl, or alkyloxycarbonyl; Ris halogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocyclyl; and R, Rand Rare each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, or heterocyclyl.

Indole and azaindole derivative having AMPK-activating activity

Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: 

Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula:   

Hetero ring-fused imidazole derivative having AMPK activating effect

A compound represented by the formula: or its pharmaceutically acceptable salt. Ring A is aromatic carbocycle or aromatic heterocycle, Z is &#x2014;O&#x2014; or &#x2014;S&#x2014;, Ris hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, Rand Rare each independently hydrogen, halogen, hydroxy or the like, Ris a group represented by the formula: &#x2014;(CRR)&#x2014;R, Rand Rare each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, Ris carboxy, cyano, substituted or unsubstituted alkyl or the like, Ris halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, and m is an integer of 0 to 3.

Oxadiazole derivative having endothelial lipase inhibitory activity

Disclosed is a compound useful as a type I 11&#x3b2;hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: 

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Osaka, Japan

Eiichi Kojima