Aminoglycoside derivatives, process for their preparation and pharmaceutical compositions
申请人:SHIONOGI & CO., LTD.
公开号:EP0009197A1
公开(公告)日:1980-04-02
Aminoglycoside derivatives of the general formula (I)
are discolsed,
wherein R1 is hydroxy or amino;
R2 is hydrogen or hydroxy; and
R3 is hydroxymethyl or carbamoyloxymethyl and their salts with acids, together with a process for their preparation and pharmaceutical compositions having antibiotic activity and containing compounds of the general formula (I).
N-substituted pseudo-aminosugars, their production and use
申请人:Takeda Chemical Industries, Ltd.
公开号:EP0089812A1
公开(公告)日:1983-09-28
A compounds of the general formula:
wherein A is hydrogen or a hydroxyl group; B is (1) a group of the formula:
(2) a group of the formula;
(3) a group of the formula:
where X1 and X2 are each a group represented by
either X1 and X2 is oxygen while the other is a group represented
or X1 and X2 combine to be oxygen; Y is 1 a lower alkyl group of 1 to 4 carbon atoms which may have a hydroxyl substitutent, 2 a hydroxyl group, or 3 an amino group; and Z is hydrogen, a hydroxyl group, a hydroxymethyl group or an amino group; R1 and R2 are each a hydroxyl group or combine to be oxygen; and the chemical bond designates either the R- oriand S-configurations; and the amino group or hydroxyl group may be ptoected, or a pharmaceutically acceptable salt thereof is novel and possesses excellent inhibitory activity against a-glucoside hydrolase and is useful for hyperglycemic symptons and various disorders caused by hyperglycemia.
A 通式如下的化合物
其中 A 是氢或羟基;B 是 (1) 式中的一个基团:
(2) 式中的基团
(3) 式中的一个基团:
其中 X1 和 X2 分别是由以下各项代表的基团
或 X1 和 X2 是氧,而另一个是由以下各项表示的基团
或 X1 和 X2 结合为氧;Y 是 1 个可有羟基取代基的 1 至 4 个碳原子的低级烷基,2 个羟基或 3 个氨基;Z 是氢、羟基、羟甲基或氨基;R1 和 R2 各自是羟基或结合为氧;其化学键指定为 R 或 i 和 S 构型;氨基或羟基可被连接,或其药学上可接受的盐是新颖的,对 a-糖苷水解酶具有极好的抑制活性,可用于高血糖症状和高血糖引起的各种疾病。