Kissei Pharmaceutical Co., Ltd.

Hiroaki Shiohara

Norihiko Kikuchi

Kenji Yokoyama

Harunobu Mukaiyama

Hideki Takeuchi

Kosuke Okazaki

Hiroaki Kobayashi

Yuichiro Kai

Masahiko Uchida

Yoshihiro Terao

Yuji Hoyano

Masayuki Isaji

Nobuhiko Fushimi

Fumiaki Ito

Hideki Fujikura

Kazuo Shimizu

Nobuyuki Tanaka

Hideyuki Muranaka

Takehiro Ishikawa

Shigeru Yonekubo

Makio Kitazawa

Hirotaka Teranishi

Tetsuya Nakamura

Yasunori Ueno

Masako Yoshida

Hitoshi Inoue

Tomonaga Ozawa

Satoko Kobayashi

The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein Rand Rare each hydrogen, lower acyl, lower alkoxycarbonyl or the like; Ris halo-lower alkyl, lower acyl, halo-lower alkylcarbonyl, cycloalkylcarbonyl, optionally substituted arylcarbonyl, lower alkoxycarbonyl or the like; Ris lower alkyl, halo-lower alkyl, cycloalkyl, lower alkoxy-lower alkyl or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Catechol derivative, pharmaceutical composition containing the same, use of the catechol derivative, and use of the pharmaceutical composition

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 fused heterocyclic derivatives represented by the general formula: wherein Rrepresents H, halogen, OH, etc.; Rrepresents H, halogen or an alkyl group; Rand Rrepresent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.

Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use 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;

The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein Ris a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group represented by the general formula; the other is an optionally substituted alkyl group or a cycloalkyl group; and Ris a halogen atom, a hydroxy group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an alkylthio group, a group of the general formula: -A-Rwherein A is a single bond, an oxygen atom, a methylene group, an ethylene group, &#x2014;OCH&#x2014; or &#x2014;CHO&#x2014;; and Ris a cycloalkyl group, a heterocycloalkyl group, an optionally substituted aryl group, an optionally substituted tiazolyl group or an optionally substituted pyridyl group, pharmaceutically acceptable salts thereof or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT1, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, pharmaceutical uses thereof and production intermediates thereof.

Glucopyranosyloxypyrazole derivative medicinal composition containing the same medicinal use thereof and intermediate therefor

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Nagano, Japan

Hiroaki Shiohara