The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.
本发明涉及公式I的非肽取代的螺环异杂苯并
环己烯,其可用作血管
加压素受体拮抗剂,用于治疗与血管
加压素受体活性有关的情况,如涉及增加血管阻力和心脏不全的情况,包括充血性心力衰竭、低
钠血症和高血压等。还公开了包含公式I化合物的药物组合物和治疗高血压、充血性心力衰竭、心脏不全、冠状动脉痉挛、心肌缺血、肝硬化、低
钠血症、肾脏痉挛、肾衰竭、糖尿病肾病、脑
水肿、脑缺血、中风、血栓形成或
水肿等情况的方法。