Glucopyranosyloxypyrazole derivatives, medicinal...

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

Reexamination Certificate

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C514S025000, C514S409000, C514S407000, C514S866000, C514S909000, C536S004100, C548S373100, C548S548000, C548S376100, C548S366100

Reexamination Certificate

active

07115575

ABSTRACT:
The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula:wherein R1represents a hydrogen atom or a lower alkyl group; one of Q1and T1represents a group represented by the general formula:while the other represents a lower alkyl group or a halo(lower alkyl) group; and 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, 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.

REFERENCES:
patent: 5264451 (1993-11-01), Kees
patent: 5274111 (1993-12-01), Kees
patent: 6815428 (2004-11-01), Ohsumi et al.
patent: 2003/0087843 (2003-05-01), Washburn
patent: 2005/0043249 (2005-02-01), Ohsumi et al.
patent: WO 03/020737 (2003-03-01), None
Kees et al. (Journal of Medicinal Chemistry (1996), 39, 3920-3928).
Brian E. Peerce, Molecular mechanism of two noncompetitive inhibitors of NA+glucose cotransporter; comparison of DCCD and PCMB; Am. J. Physiol., vol. 264, No. 2, Pt. 1, Pt. 1, pp. G300-G305 (1993).
Borries Kubel: Einfache Synthese von 4-(Heteroarylmethyl)phenolen und deren Acylierung: Liebigs Ann. Chem., vol. 9. pp. 1392-1401(1980).
Kees et al., Journal of Medicinal Chemistry (1996), 39 (20), 3920-3928.

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