申请人:BANYU PHARMACEUTICAL CO., LTD.
公开号:EP1386920A1
公开(公告)日:2004-02-04
This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I]
[in which R1 and R2 stand for, e.g., hydrogen atoms; R3a, R3b, R4, R5 stand for, e.g., hydrogen atoms and alkyl groups; R6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group].
The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease; drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.
本发明涉及苯并咪唑酮衍生物,以通式[I]的化合物为代表。
[其中 R1 和 R2 代表氢原子;R3a、R3b、R4、R5 代表氢原子和烷基;R6 代表芳基或杂芳基;A 环代表含有一个氮原子的 5 至 8 元脂肪杂环;Z 代表羰基或磺酰基]。
本发明的苯并咪唑酮衍生物对毒蕈碱乙酰胆碱受体具有拮抗作用,可作为帕金森病的治疗药物和/或预防药物;药物诱发的帕金森病、肌张力障碍、运动障碍、胰腺炎、胆石症/胆囊炎、胆汁运动障碍、贲门失弛缓症、疼痛、瘙痒、胆碱能性荨麻疹、肠易激综合征、呕吐、恶心、头晕、美尼尔氏病、晕车和排尿障碍。