- Discovery of remogliflozin etabonate: A potent and highly selective SGLT2 inhibitor
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We optimized the structure of an active metabolite (1) of WAY-123783, which was obtained from mouse urine after oral administration, to improve selectivity for SGLT2 and oral bioavailability. O-glucoside derivative 24 (remogliflozin etabonate) was subsequently identified as a potent, highly selective, and orally available SGLT2 inhibitor.
- Shimizu, Kazuo,Fujikura, Hideki,Fushimi, Nobuhiko,Nishimura, Toshihiro,Tatani, Kazuya,Katsuno, Kenji,Fujimori, Yoshikazu,Watanabe, Shinjiro,Hiratochi, Masahiro,Nakabayashi, Takeshi,Kamada, Noboru,Arakawa, Koichi,Hikawa, Hidemasa,Azumaya, Isao,Isaji, Masayuki
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- Mild Nitration of Pyrazolin-5-ones by a Combination of Fe(NO3)3 and NaNO2: Discovery of a New Readily Available Class of Fungicides, 4-Nitropyrazolin-5-ones
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4-Nitropyrazolin-5-ones have been synthesized by the nitration of pyrazolin-5-ones at room temperature by employing the Fe(NO3)3/NaNO2 system. The method demonstrated selectivity towards the 4-position of pyrazolin-5-ones
- Krylov, Igor B.,Budnikov, Alexander S.,Lopat'eva, Elena R.,Nikishin, Gennady I.,Terent'ev, Alexander O.
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p. 5922 - 5933
(2019/04/03)
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- Selective reduction exocyclic double bond of isoxazolones and pyrazolones by hantzsch 1,4-dihydropyridine
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Hantzsch 1,4-dihydropyridine (HEH) was used to realize the selective reduction of the exocyclic double bond of 4-arylmethylene- and 4-alkylidene-4H-isoxazol-5-ones and 4-arylraethylene-4H-pyrazol-5-ones. Georg Thieme Verlag Stuttgart.
- Liu, Zhengang,Han, Bing,Liu, Qiang,Zhang, Wei,Yang, Li,Liu, Zhong-Li,Yu, Wei
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p. 1579 - 1580
(2007/10/03)
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- GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND USE THEREOF IN MEDICINES
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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 f
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Page/Page column 20
(2008/06/13)
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- GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES IN THE PRODUCTION THEREOF
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The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents 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 on 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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