Kissei Pharmaceutical Co., Ltd.

Masato Iizuka

Kazuo Shimizu

Yasushi Takigawa

Hideki Fujikura

Masahiro Hiratochi

Norihiko Kikuchi

Kazuo Shimatzu

(Aza)indolizine derivatives represented by Formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In Formula (I), 0 to 2 of X, X, Xand Xare a nitrogen atom and the others are CR; one of Tand Trepresents cyano and the other represents a group represented by Formula (A), with the proviso that when Tis cyano, at least one of Xto Xis a nitrogen atom; Rindependently represents a hydrogen atom, a halogen atom, a hydroxy group, Calkyl, Calkoxy or the like; ring U represents a benzene ring or the like; m represents integral number from 0 to 2; Rindependently represents a fluorine atom, a hydroxy group or the like. 

(aza)indolizine derivative and pharmaceutical use thereof

5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH, halogen, haloalkyl and the like; Xand Xindependently represent CRor N; Rrepresents H, alkyl and the like; Rrepresents halogen, cyano, haloalkyl, A-D-E-G-L-M, &#x2014;N(-D-L-M)and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SOand the like. 

5-membered nitrogen containing heterocyclic derivatives and pharmaceutical compositions comprising the same

The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH, halogen, nitro, alkyl, alkoxy and the like; X, Xand Xindependently represent CRor N; Rand Rindependently represent halogen, cyano, haloalkyl, A-D-E-G, &#x2014;N(-D-E-G)and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SOand the like. 

(aza)indole derivative and use thereof for medical purposes

The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; Rrepresents halogen, a hydroxy group or the like; Rrepresents halogen, a hydroxy group, alkyl, alkoxy, alkyl substituted by fluorine, alkoxy substituted by fluorine or the like; m represents a number from 0 to 2; n represents a number from 0 to 3; and Rrepresents hydrogen, fluorine or the like. 

Indolizine derivative and use thereof for medical purposes

The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), Xand Xrepresent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; Rrepresents a hydroxy group, amino or Calkyl; Rrepresents Calkyl, Calkoxy Calkyl or the like. 

Fused-ring derivative and medical application of same

The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to 5-membered heterocyclic derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH, halogen, haloalkyl and the like; Xand Xindependently represent CRor N; Rrepresents H, alkyl and the like; Rrepresents halogen, cyano, haloalkyl, A-D-E-G-L-M, -N(-D-L-M)and the like, in the formula, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SOand the like. 

The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetrazolyl and the like; Y represents H, OH, NH, halogen, nitro, alkyl, alkoxy and the like; X, Xand Xindependently represent CRor N; Rand Rindependently represent halogen, cyano, haloalkyl, A-D-E-G, &#x2014;N(-D-E-G)and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SOand the like. 

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Azumino, Japan

Masato Iizuka