申请人:Pfizer Inc.
公开号:US05889010A1
公开(公告)日:1999-03-30
Pharmaceutically active benzimidazole derivatives are disclosed comprising compounds of the formula: ##STR1## particularly wherein X is nitrogen, R.sup.1 is phenyl or heteroaryl, and one of R.sup.2 or R.sup.3 is hydroxy. Said compounds have D4 dopaminergic receptor binding activity and consequently are useful as active ingredients in pharmaceutical compositions and methods of treatment for sleep disorders, sexual disorders, gastrointestinal disorders, psychosis, affective psychosis, nonorganic psychosis, personality disorders, psychiatric mood disorders, conduct and impulse disorders, schizophrenic and schizoaffective disorders, polydipsia, bipolar disorders, dysphoric mania, anxiety and related disorders, obesity, emesis, bacterial infections of the CNS, learning disorders, memory disorders, Parkinson's disease, depression, extrapyramidal side effects from neuroleptic agents, neuroleptic malignant syndrome, hypothalamic pituitary disorders, ocular disorders, congestive heart failure, chemical dependencies, vascular and cardiovascular disorders, dystonia, tardive dyskinesia, Gilles De La Tourette's syndrome and other hyperkinesias, dementia, ischemia, Parkinson's disease, akathesia and other movement disorders, hypertension and diseases caused by a hyperactive immune system such as allergies and inflammation in a mammal.
公开了一种含有苯并咪唑衍生物的药物,其中包括式子:##STR1## 特别是其中X为氮,R1为苯基或杂环基,R2或R3中的一个为羟基。这些化合物具有D4多巴胺受体结合活性,因此可用作制药组合物和治疗失眠症、性功能障碍、胃肠功能障碍、精神病、情感性精神病、非器质性精神病、人格障碍、精神情绪障碍、行为和冲动障碍、精神分裂症和分裂情感障碍、多饮症、双相障碍、烦躁躁狂、焦虑和相关障碍、肥胖、呕吐、中枢神经系统细菌感染、学习障碍、记忆障碍、帕金森病、抑郁症、神经阻滞剂引起的锥体外副作用、神经阻滞剂恶性综合征、下丘脑垂体障碍、眼部疾病、充血性心力衰竭、化学依赖症、血管和心血管疾病、肌张力障碍、迟发性运动障碍、吉尔·德·拉图雷综合征和其他过度运动症、痴呆、缺血、帕金森病、不安躁动和其他运动障碍、高血压和由哺乳动物的免疫系统过度活跃引起的过敏和炎症等疾病的治疗方法中的有效成分。