SULFONYLPYRAZOLE AND SULFONYLPYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS
申请人:ABBVIE BHAMAS LTD.
公开号:US20140303372A1
公开(公告)日:2014-10-09
This invention concerns compounds of the general formula (1):
and derivatives thereof, which are antagonists of 5-HT
6
receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes.
本发明涉及一般式(1)的化合物及其衍生物,其为5-HT6受体拮抗剂,其中符号在说明中给出了含义。本发明还涉及制备这些化合物的方法,对于其合成有用的新型中间体,以及这些化合物和组合物的用途,特别是在将其用于患者治疗至少一种疾病或病况中,包括帕金森病、亨廷顿舞蹈症、精神分裂症、焦虑症、抑郁症、躁郁症、精神病、癫痫、强迫症、情绪障碍、偏头痛、阿尔茨海默病、年龄相关的认知退化、轻度认知障碍、睡眠障碍、饮食障碍、厌食症、贪食症、暴食症、惊恐发作、不安静脚症、注意力不足过动症、注意力不足障碍、戒除可卡因、乙醇、尼古丁或苯二氮平滥用引起的疾病、疼痛、与脊髓损伤或头部损伤相关的疾病、脑积水、功能性肠道疾病、肠易激综合征、肥胖症和2型糖尿病。