申请人:Kureha Chemical Industry Co., Ltd.
公开号:EP0696583A1
公开(公告)日:1996-02-14
A benzimidazolesulfonamide derivative of the formula (I):
wherein R¹ is an alkyl group of 1 to 6 carbon atoms or a haloalkyl group of 1 to 6 carbon atoms; R² is a hydrogen atom, an alkyl group of 1 to 6 carbon atoms, a haloalkyl group of 1 to 6 carbon atoms, -OR⁴, -O(CH₂)mC₆H₅, -(CH₂)nC₆H₅, -NH₂, -NHR⁵, -NHC(=O)R⁶, -N(R⁷)₂, -NHC(=O)(CH₂)pC₆H₅, or -NHC(=O)CH(C₆H₅)₂; R³ is an azole group, -COOH, -COOR⁸ ,or -SO₃H; A is -O-, -NH-, or -S(O)q-; R⁴, R⁵, R⁶, R⁷, and R⁸ are independently an alkyl group of 1 to 6 carbon atoms; m, n, and p are independently 0 or an integer of 1 to 6; and q is 0, 1, or 2, or a salt thereof; and a pharmaceutical composition comprising the above compound are disclosed. The compound exhibits a stable and strong antagonism to angiotensin II.
式 (I) 的
苯并咪唑磺酰胺衍
生物:
其中 R¹ 是 1 至 6 个碳原子的烷基或 1 至 6 个碳原子的卤代烷基;R² 是氢原子、1-6 个碳原子的烷基、1-6 个碳原子的卤代烷基、-OR⁴、-O(CH₂)mC₆H₅、-(CH↪No_2000)nC₆H₅、-NH₂、-NHR⁵、-NHC(=O)R⁶、-N(R⁷)₂、-NHC(=O)(CH₂)pC₆H₅或-NHC(=O)CH(C₆H₅)₂;R³是唑基、-COOH、-COOR⁸或-SO₃H;A 是-O-、-NH-或-S(O)q-;R⁴、R⁵、R⁶、R⁷和 R⁸ 独立地是 1 至 6 个碳原子的烷基;m、n 和 p 独立地为 0 或 1 至 6 的整数;q 为 0、1 或 2,或其盐,以及包含上述化合物的药物组合物。该化合物对
血管紧张素 II 具有稳定而强烈的拮抗作用。