Kissei Pharmaceutical Co., Ltd.

Masahiro Hiratochi

Hideki Fujikura

Kazuo Shimizu

Norihiko Kikuchi

Yasushi Takigawa

Masato Iizuka

Masayuki Isaji

Toshihiro Nishimura

Kenji Katsuno

Akira Iyobe

Minoru Fujioka

Kazuya Tatani

Takashi Miyagi

Nobuhiko Fushimi

Yoshinori Nonaka

Yu Kuramochi

Yoshiki Tokutake

Kazuo Shimatzu

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 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. 

(Aza)indole derivative and use thereof for medical purposes

The present invention provides benzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; Rand Rare H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; Ris H, a halogen atom, optionally substituted alkyl group or the like; Rand Rare H, a halogen atom, OH or the like; and Rand Rare H or OH: Ris F or OH. 

Benzimidazole derivatives and medical uses thereof

The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein Rrepresents a hydrogen atom or a lower alkyl group; one of Qand Trepresents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and Rrepresents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

Glucopyranosyloxypyrazole derivatives, medicinal compositions containing the same and intermediates in the production thereof

The present invention relates to benzylphenol derivatives represented by the general formula: 

Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives

The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula:wherein Rrepresents a hydrogen atom or a lower alkyl group; one of Qand Trepresents a group represented by the general formula:while the other represents a lower alkyl group or a halo(lower alkyl) group; and Rrepresents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

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Azumino, Japan

Masahiro Hiratochi