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发明公开
EP1405859A1 NITROGENOUS HETEROCYCLIC DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE THEREFOR 审中-公开
NITRO GENES杂环衍生物CONTAINING医疗用组合物，及其医药用途和中间体THEREFOR

NITROGENOUS HETEROCYCLIC DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE THEREFOR
摘要：
The present invention is to provide a nitrogen-containing heterocyclic derivative represented by the general formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof, which exerts an excellent inhibitory activity in human SGLT2 and is useful as an agent for the prevention or treatment of a disease associated with hyperglycemia such as diabetes etc., or a pharmaceutical composition comprising the same and a pharmaceutical use thereof and a production intermediate thereof. In the general formula (I), X 1 and X 3 are N or CH; X 2 is N or CR 2 ; X 4 is N or CR 3 ; and with the proviso that one or two of X 1 , X 2 , X 3 and X 4 are N; and R 1 , R 2 and R 3 are a hydrogen atom etc.
摘要（中）：

Glucopyranosylheterocycle衍生物（I）是新的。 式（I）的Glucopyranosylheterocycle衍生物和它们的盐和前体药物是新的。 [图像] X 1>，X 3> N或CH; X 2> N或CR 2>; X 4为> N或CR 3>; 的R 1> H，卤素，A，OA，SA，AOA，OAOA，AOAOA，环烷基，低级卤代烷基或A 1 OH; 甲1lower亚烷基，低级alkenyleneoxy或低级亚烷硫基; R 2> H，卤素，A，环烷基，OA，NH 2，低级酰基氨基，NHA或NAA; ，R 3> H或A，并且A：低级烷基，条件没有一个或两个X 1> X 4> = N.因此独立权利要求中包含对式中间体化合物（II） - （IV）。 [图像] P“：H或前药基团; R 11>基团R 1>与A 1 OH由器10p A“取代; ，R 0>基团R 1 OH通过1W A A器10p 1和P 1个为H或羟基保护基团替代。 活动：降糖; 厌食; 降血脂; Antianteriosclerotic; 低血压; Cardiant; 抗炎; Uropathic。 作用机制：拮抗剂钠; 胆固醇拮抗剂。 在使用COS-7细胞，3-（4-乙基苄基）-2-（测试版-D-吡喃葡糖氧基）测定-4,6-二甲基吡啶有一个IC，用于50value甲基基-α-D-吡喃葡糖苷在41人SGLT2受体的结合 纳摩。

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