申请人:BTG International Limited
公开号:EP2382979A2
公开(公告)日:2011-11-02
Treatments for conditions involving detrimental activity of the enzyme core 2 GlcNAc - T are provided using compounds of the formula I
wherein
R1 is H, -OH, C1-6 alkoxy, -NR5R6, or Sac 1;
R2 is H, -OH, C1-6 alkoxy or Sac 2;
R3 is H, -OH, C1-6 alkoxy or Sac 3;
R4 is H, C1-6 alkyl, C1-6 hydroxyalkyl or C1-6-alkoxy-C1-6-alkyl;
R5 is H, C1-6 alkyl or C1-6 acyl;
R6 is H, C1-6 alkyl or C1-6 acyl;
Sac 1 Sac 2 and Sac 3 are independently selected saccharide moieties; and
Z is a steroid moiety;
or a pharmaceutically acceptable salt, ether or ester form thereof, wherein the condition is an autoimmune condition.
使用式 I 的化合物可治疗涉及核心 2 GlcNAc - T 酶有害活性的病症。
其中
R1 是 H、-OH、C1-6 烷氧基、-NR5R6 或 Sac 1;
R2 是 H、-OH、C1-6 烷氧基或 Sac 2;
R3 是 H、-OH、C1-6 烷氧基或 Sac 3;
R4 是 H、C1-6-烷基、C1-6-羟基烷基或 C1-6- 烷氧基-C1-6-烷基;
R5 是 H、C1-6 烷基或 C1-6酰基;
R6 是 H、C1-6 烷基或 C1-6 丙烯酸基;
Sac 1 Sac 2 和 Sac 3 是独立选定的糖分子;以及
Z 是类固醇分子;
或其药学上可接受的盐、醚或酯形式,其中所述病症为自身免疫性病症。