Substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and a medicament comprising them
申请人:——
公开号:US20010023257A1
公开(公告)日:2001-09-20
The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them
Substituted norbornylamino derivatives having exo-configured nitrogen and an endo-fused five-membered ring of the formula I, or having exo-configured nitrogen and an exo-fused five-membered ring of the formula I a
1
in which R1, R2, R3, R4, R5, A, B, S1, and S2 are as defined in the claims, are highly suitable for use as antihypertensive agents, for reducing or preventing ischemically induced damage, for use as medicaments for surgical interventions for the treatment of ischemias of the nervous system, of stroke and cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxatives, as agents against ectoparasites, for the prevention of the formation of biliary calculus, as antiatherosclerotics, as agents against late diabetic complications, carcinomatous disorders, fibrotic disorders, endothelial dysfunction, and organ hypertrophies and hyperplasias.
They are inhibitors of the cellular sodium/proton antiporter. They have an influence on serum lipoproteins and can therefore be used for the prophylaxis and regression of atherosclerotic changes.
该申请公开了取代的诺博烯基氨基衍生物,其制备方法,它们作为药物或诊断工具的用途以及包含它们的药物。具有式I中的外向构型氮和内向融合的五元环,或具有式I a1中的外向构型氮和外向融合的五元环的取代诺博烯基氨基衍生物,其中R1,R2,R3,R4,R5,A,B,S1和S2如权利要求所定义,非常适用于用作降压剂,用于减少或预防缺血性损伤,用作治疗神经系统缺血,中风和脑水肿,休克,呼吸驱动力受损的手术干预药物,用于治疗打鼾,作为泻药,对抗外寄生虫药物,预防胆石形成,作为抗动脉粥样硬化药物,对抗晚期糖尿病并发症,癌症疾病,纤维病性疾病,内皮功能障碍以及器官肥大和增生。它们是细胞钠/质子抗转运体的抑制剂。它们对血清脂蛋白有影响,因此可以用于动脉粥样硬化变化的预防和回归。