Glucopyranosyloxypyrazole derivatives and use thereof in...

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

Reexamination Certificate

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C514S025000, C514S035000, C536S004100, C536S017400, C536S018100

Reexamination Certificate

active

07084123

ABSTRACT:
The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug: one of Q and T represents a group represented by the general formula:(wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

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patent: WO 02/36602 (2002-10-01), None
patent: WO 02/053573 (2002-11-01), None
patent: WO 03/020737 (2003-03-01), None
New Potent Antihyperglycemic 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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