申请人:——
公开号:US20040248941A1
公开(公告)日:2004-12-09
The present invention relates to a compound represented by the following formula
1
wherein each symbol is as defined in the specification, or a salt thereof, which has superior stability to acid and which is a prodrug of 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-
1
H-benzimidazole. This compound (1) shows a superior anti-ulcer activity, a gastric acid secretion-suppressive action, a mucosa-protecting action, an anti-
Helicobacter pylori
action and the like in living organisms, (2) shows low toxicity, (3) shows superior stability to acid (which obviates the need to formulate an enteric-coated preparation, thereby lowering the cost, and reduces the size of preparation to facilitate swallowing for patients having difficulty in swallowing), (4) shows faster absorption than enteric-coated preparations (rapid expression of gastric acid secretion-suppressive action), and (5) is sustainable.
本发明涉及以下式1所表示的化合物或其盐,其中每个符号如规范中所定义,该化合物具有优异的酸稳定性,并且是2-[[[3-甲基-4-(2,2,2-三氟乙氧基)-2-吡啶基]甲基]亚磺酰基]-1H-苯并咪唑的前药。该化合物(1)在生物体内显示出优异的抗溃疡活性、抑制胃酸分泌作用、保护粘膜作用、抗幽门螺杆菌作用等,(2)显示出低毒性,(3)显示出优异的酸稳定性(无需配制肠溶涂层制剂,从而降低成本,并减小制剂的大小,以便于吞咽困难的患者),(4)显示出比肠溶涂层制剂更快的吸收速度(快速表达胃酸分泌抑制作用),并且(5)是可持续的。