Kissei Pharmaceutical Co., Ltd.

Hirotaka Teranishi

Masayuki Isaji

Shigeru Yonekubo

Nobuhiko Fushimi

Kazuo Shimizu

Fumiaki Ito

Masaki Tomae

Toshihide Shibazaki

Toshihiro Nishimura

Kazuya Tatani

Hideyuki Muranaka

Yasunori Ueno

Kiyoshi Kasai

Hiroaki Shiohara

Masako Yoshida

Akira Iyobe

The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein Ris cyano or the like; Rand Rare hydrogen or the like; Ris Calkyl or the like; Ris Calkyl, halo-Calkyl, cycloalkyl, cycloalkyl-Calkyl, aralkyl or the like; Rand Rare each hydrogen, Calkyl, halo-Calkyl, cycloalkyl, Calkoxy-Calkyl, RRN&#x2014;Calkyl or the like, which exhibit potent dopamine Dreceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof. 

Octahydrothienoquinoline derivative, pharmaceutical composition comprising derivative, and use of these

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 represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted Calkyl group etc.; Rrepresents H, a halogen atom, OH, an optionally substituted Calkyl group etc.; X represents a single bond, O or S; Y represents an optionally substituted Calkylene group etc.; Z represents &#x2014;R, &#x2014;CORetc. in which Rrepresents an optionally substituted Calkyl group etc.; and Rrepresents an optionally substituted Calkyl group etc.; Rrepresents H, an optionally substituted Calkyl group etc.; and R, Rand Rrepresent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, impaired glucose tolerance, impaired fasting glycemia, diabetic complications or obesity, and a disease associated with the increase of blood galactose level such as galactosemia, and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.

Pyrazole derivatives, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof

The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, 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, in the formula Rrepresent H, an optionally substituted alkyl group, an alkenyl group, etc.; Rrepresent H, a halogen atom or an alkyl group; Rand Rrepresent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1) or (G-2) (in which Erepresents H, F or OH; and Erepresents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof. 

Nitrogenous fused-ring derivatives, medicinal compositions containing the derivatives, and use thereof as drugs

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 represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted Calkyl group etc.; Rrepresents H, a halogen atom, OH, an optionally substituted Calkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a Calkylene group etc.; Z represents CO or SO; Rand Rrepresent H, an optionally substituted Calkyl group etc.; and R, Rand Rrepresent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, 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 for production thereof

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 nitrogen-containing fused-ring derivatives represented by the following general formula, 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, in the formula Rrepresent H, an optionally substituted alkyl group, analkenyl group, etc.; Rrepresent H, a halogen atom or an alkyl group; Rand Rrepresent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1) or (G-2) (in which Erepresents H, F or OH; and Erepresents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof 

The present invention provides crystals of 2-(4-methoxybenzyl)phenyl 6-O-ethoxycarbonyl-&#x3b2;-D-glucopyranoside, pharmaceutical compositions containing the same and their uses, which exhibit excellent SGLT2 inhibitory activities, and are useful for treating or preventing diseases associated with hyperglycemia.

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Azumino, Japan

Hirotaka Teranishi