Kissei Pharmaceutical Co., Ltd.

Kenji Katsuno

Masayuki Isaji

Hideki Fujikura

Toshihiro Nishimura

Nobuhiko Fushimi

Kazuya Tatani

Masahiro Hiratochi

Akira Iyobe

Minoru Fujioka

Norihiko Kikuchi

Yoshimitsu Komatsu

Yoshikazu Fujimori

Yoshiki Tokutake

The present invention provides pharmaceutical compositions useful as agents for the inhibition of progression of diseases associated with abnormal accumulation of liver lipids. In particular, the pharmaceutical compositions of the present invention which comprise as an active ingredient a sodium/glucose co-transporter 2 inhibitor are highly suitable as an agent for the inhibition of progression of not only common fatty liver but also non-alcoholic fatty liver disease (NAFL), non-alcoholic steatohepatitis (NASH), hypernutritive fatty liver, diabetic fatty liver, alcoholic fatty liver disease toxic fatty liver or the like.

Progression inhibitor for disease attributed to abnormal accumulation of liver fat

The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein Xrepresents N or CR; Xrepresents N or CR; Xrepresents N or CR; Xrepresents N or CR; and with the proviso that one or two of Xto Xrepresent N; R represents optionally substituted Ccycloalkyl, optionally substituted Caryl, etc.; Rto Rrepresent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.

Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use thereof

The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R, Rand Rrepresent a hydrogen atom or a halogen atom; Rrepresents a lower alkyl group or a halo(lower alkyl) group; and Rrepresents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, etc., a pharmaceutically acceptable salt thereof or a prodrug thereof., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.

Glucopyranosyloxypyrazole derivatives and medicinal use thereof

The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein Xand Xindependently represent N or CH; Xrepresents N or CR; Xrepresents N or CR; and with the proviso that one or two of X, X, Xand Xrepresent N; Rrepresents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group, a lower alkoxy(lower alkoxy)-substituted (lower alkyl) group, a cyclic lower alkyl group, a halo(lower alkyl) group or a group represented by the general formula: HO-A- wherein A represents a lower alkylene group, a lower alkyleneoxy group or a lower alkylenethio group; Rrepresents a hydrogen atom, a halogen atom, a lower alkyl group, a cyclic lower alkyl group, a lower alkoxy group, an amino group, a (lower acyl)amino group, a mono(lower alkyl)amino group or a di(lower alkyl)amino group; and Rrepresents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, or prodrugs thereof which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses and production intermediates thereof.

Nitrogenous heterocyclic derivatives, medicinal compositions containing the same, medicinal uses thereof, and intermediates therefor

The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; Rrepresents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; Rrepresents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.

The present invention relates to glucopyranosyl-oxybenzylbenzene derivatives represented by the general formula: wherein Rrepresents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group etc.; Rrepresents a hydrogen atom or a lower alkyl group; and Rrepresents a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group, a substituted or unsubstituted(lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.

Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof

The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein Rrepresents a hydrogen atom or a lower alkyl group; one of Qand Trepresents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and Rrepresents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

Glucopyranosyloxypyrazole derivatives, medicinal compositions containing the same and intermediates in the production thereof

The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein Rrepresents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group etc.; Rrepresents a hydrogen atom or a lower alkyl group; and Rrepresents a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group, a substituted or unsubstituted (lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.

The present invention relates to benzylphenol derivatives represented by the general formula: 

Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives

The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula:wherein Rrepresents a hydrogen atom or a lower alkyl group; one of Qand Trepresents a group represented by the general formula:while the other represents a lower alkyl group or a halo(lower alkyl) group; and Rrepresents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

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Nagano, Japan

Kenji Katsuno