申请人:Matsoukas John
公开号:US20100216854A1
公开(公告)日:2010-08-26
The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds of formulas (I), (IIa), (IIIb) in hydrophilic or lipophilic form, which are useful as angiotensin II AT1 receptor antagonists with sympathetic suppressant properties. In particular, the invention provides pharmaceutical compositions containing the pharmacophoric groups of Losartan and Clonidine as well compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases through Renin Angiotensin System (RAS) and Sympathetic System (SS). Alkylated histamine based double action Saltans are lipophilic and can act transdermally.
本发明提供了新型1,5和1,3,5-取代咪唑化合物的水溶性或脂溶性形式的结构式(I)、(IIa)、(IIIb),这些化合物可作为具有交感神经抑制作用的血管紧张素II AT1受体拮抗剂。具体而言,本发明提供了含有洛卡特普和可乐定的药理作用基团的药物组合物,以及用于制备化合物的化合物、工艺和中间体,并在通过肾素-血管紧张素系统(RAS)和交感神经系统(SS)治疗高血压和心血管疾病的方法中使用这些化合物。烷基化组织胺双重作用盐类是脂溶性的,并可经皮作用。