| 摘要 |
<p>Glucopyranosylheterocycle derivatives (I) are new. Glucopyranosylheterocycle derivatives of formula (I) and their salts and prodrugs are new. [Image] X 1>, X 3>N or CH; X 2>N or CR 2>; X 4>N or CR 3>; R 1>H, halo, A, OA, SA, AOA, OAOA, AOAOA, cycloalkyl, lower haloalkyl or A 1OH; A 1lower alkylene, lower alkenylenoxy or lower alkylenethio; R 2>H, halo, A, cycloalkyl, OA, NH 2, lower acyl amino, NHA or NAA; R 3>H or A, and A : lower alkyl, provided that 1 or 2 of X 1>-X 4>= N. Independent claims are also included for intermediate compounds of formula (II)-(IV). [Image] P' : H or a prodrug group; R 11>a group R 1>with A 1OH replaced by A 1OP'; R 0>a group R 1with A 1OH replaced by A 1OP 1, and P 1H or hydroxy protecting group. ACTIVITY : Antidiabetic; Anorectic; Antilipemic; Antianteriosclerotic; Hypotensive; Cardiant; Antiinflammatory; Uropathic. MECHANISM OF ACTION : Sodium-Antagonist; Cholesterol-Antagonist. In assays using COS-7 cells, 3-(4-ethylbenzyl)-2-(beta -D-glucopyranosyloxy)-4,6-dimethylpyridine had an IC 50value for methyl-alpha -D-glucopyranoside binding at human SGLT2 receptors of 41 nM.</p> |
