Glucopyranosyloxypyrazole derivative medicinal composition...

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

Reexamination Certificate

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C514S027000, C536S004100, C536S017200, C536S017300, C536S017400, C536S018100

Reexamination Certificate

active

10479083

ABSTRACT:
The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:wherein R1is a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group represented by the general formula;the other is an optionally substituted alkyl group or a cycloalkyl group; and R2is a halogen atom, a hydroxy group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an alkylthio group, a group of the general formula: -A-R3wherein A is a single bond, an oxygen atom, a methylene group, an ethylene group, —OCH2— or —CH2O—; and R3is a cycloalkyl group, a heterocycloalkyl group, an optionally substituted aryl group, an optionally substituted tiazolyl group or an optionally substituted pyridyl group, pharmaceutically acceptable salts thereof or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT1, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, pharmaceutical uses thereof and production intermediates thereof.

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Banker (Modern Pharmaceutics) Banker, G.S. et al, “Modern Pharmaceutics, 3ed.”, Marcel Dekker, New York, 1996.
Kenji Tsujihara, et al.; Na+-Glucose Cotransporter (SGLT) Inhibitors as Antidiabetic Agents. 4. Synthesis and Pharmacological Properties of 4′-Dehydroxyphlorizin Derivatives Substituted on the B Ring; J. Med. Chem 1999, 42, 5311-5324.
Bryan Mackensie, et al.; Biophysical Characteristics of the Pig Kidney Na+/Glucose Cotransporter SGLT2 Reveal a Common Mechanism for SGLT1 and SGLT2; The Journal of Biological Chemistry; vol. 271, No. 51, Issue of Dec. 20, pp. 32678-32683, 1996.

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