Kissei Pharmaceutical Co., Ltd.

Fumiaki Ito

Masayuki Isaji

Nobuhiko Fushimi

Kazuo Shimizu

Shigeru Yonekubo

Hirotaka Teranishi

Hiroaki Shiohara

Hideki Fujikura

Hideyuki Muranaka

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 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 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.

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Azumino, Japan

Fumiaki Ito