Glucopyranosyloxypyrazole derivatives and medicinal use thereof

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

Reexamination Certificate

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Details

C514S035000, C514S866000, C536S004100, C536S018100

Reexamination Certificate

active

10469140

ABSTRACT:
The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:wherein R1, R2and R3represent a hydrogen atom or a halogen atom; R4represents a lower alkyl group or a halo(lower alkyl) group; and R5represents 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.

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Kenneth L. Kees, et al.; New Patent Antihyperglycamic Agents in db/db Mice; Synthesis and Structure-Activity Relationship Studies of (4-Substituted benzyl)(trifluoromethyl)pyrazoles and -pyrazolones; J. Med. Chem. 1996, 39, 3920-3928.

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