Kissei Pharmaceutical Co., Ltd.

Norihiko Kikuchi

Hideki Fujikura

Kazuo Shimizu

Masahiro Hiratochi

Masayuki Isaji

Yasushi Takigawa

Masato Iizuka

Kazuya Tatani

Hiroaki Shiohara

Kenji Yokoyama

Harunobu Mukaiyama

Hideki Takeuchi

Kosuke Okazaki

Hiroaki Kobayashi

Yuichiro Kai

Masahiko Uchida

Yoshihiro Terao

Yuji Hoyano

Tokuhisa Yamato

Shigeki Tazawa

Nobuhiko Fushimi

Toshihiro Nishimura

Kenji Katsuno

Yoshinori Nonaka

Takashi Miyagi

Makio Kitazawa

Tetsuya Nakamura

Tomonaga Ozawa

Yu Kuramochi

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 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

Pyrazole derivatives represented by the general formula: wherein Rrepresents H, an optionally substituted Calkyl group etc.; one of Q and T represents a group selected from the following groups: and the other represents &#x2014;(CH)&#x2014;Ar wherein Ar represents a substituted Caryl group, etc., and n represents 0 to 2, R represents an optionally substituted Ccycloalkyl group, etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates from glucose, fructose and mannose or a disease associated with hyperglycemia and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.

Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same

The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; Ris a hydrogen atom or a hydroxyl group; Ris a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and Rto R, Pand Q represents a halogen atom, a cyano group or the like. 

Purine nucleoside derivative modified in 8-position and medical use thereof

The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: 

5-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation

The present invention provides pyrazole derivatives represented by the general formula: wherein Rrepresents H, an optionally substituted Calkyl, etc.; one of Q and T represents a group selected from the following: and the other represents -Z-Ar wherein Z represents &#x2014;O&#x2014;, &#x2014;S&#x2014;, etc.; Ar represents an optionally substituted Caryl, etc.;R represents an optionally substituted Ccycloalkyl, an optionally substituted Caryl, etc., pharmaceutically acceptable salts thereof, and prodrugs thereof, which exhibit an excellent inhibitory activity in human sodium/glucose cotransporter (SGLT) and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose (diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, etc.), and pharmaceutical compositions containing the same, medicinal uses thereof and intermediates for production therefor.

Pyrazole derivative, drug composition containing the same and production intermediate therefor

The present invention provides pyrazole derivatives represented by the general formula: wherein Rrepresents H, an optionally substituted Calkyl group etc.; one of Q and T represents a group selected from the following groups: and the other represents &#x2014;(CH)&#x2014;Ar wherein Ar represents an optionally substituted Caryl group or an optionally substituted Cheteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted Calkoxyl group, an optionally substituted amino group, an optionally substituted Cheterocycloalkyl group or an optionally substituted heterocycle-fused phenyl group; R represents an optionally substituted Ccycloalkyl group, an optionally substituted Caryl group etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose or a disease associated with hyperglycemia (e.g., diabetic complications, diabetes, etc.), and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.

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 provides a compound represented by general formula (I): or pharmaceutically acceptable salts thereof, wherein W is O, S(O), CHand the like; Ris halogen, lower alkyl, halo-lower alkyl, CN and the like; Ris hydrogen and the like; Ris hydrogen, halogen, alkyl, halo-lower alkyl, substituted alkyl, aryl, aralkyl, alkoxy, substituted alkoxy, alkanoyl, aroyl, &#x2014;CONR(R), &#x2014;S(O)R, &#x2014;SONR(R) and the like; Ris hydrogen, halogen, alkyl, substituted alkyl and the like; A is &#x2014;N(R)CO&#x2014;A&#x2014;CORand the like; pharmaceutical compositions containing them and their uses, which have a high affinity to human thyroid hormone receptors, in particular human thyroid hormone receptor &#x3b2;.

Thyroid hormone receptor ligand, medicinal compositions containing the same and use thereof

The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein Ris a hydrogen atom or an optionally substituted lower alkyl group;

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Nagano, Japan

Norihiko Kikuchi