Kissei Pharmaceutical Co., Ltd.

Shigeki Tazawa

Masayuki Isaji

Hideki Fujikura

Norihiko Kikuchi

Tokuhisa Yamato

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 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.

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Nagano, Japan

Shigeki Tazawa