发明名称 1,7-萘啶衍生物;1,7-NAPHTHYRIDINE DERIVATIVES
摘要 本发明系关于如下通式之化合物,;其中:R 1 系苯基或吡啶基,其可视情况经一个、两个或三个选自卤素、经卤素取代之低碳数烷基、低碳数烷氧基、经卤素取代之低碳数烷氧基、氰基或S(O)2-低碳数烷基之取代基取代,或系:吗啉基、二氢吡喃基或哌啶基,其中哌啶基可视情况经卤素取代,或系:C(O)O-低碳数烷基;R 2 系氢;R 3 系氢、经卤素取代之低碳数烷基、-(CH2)n-S(O)2-低碳数烷基、-(CH2)n-环烷基或-(CH2)n-低碳数烷氧基;R 4 系氢或低碳数烷基;n 系0、1或2;或其医药上可接受之酸加成盐、外消旋混合物或其相应的对映异构体及/或其光学异构体。;该等化合物可用于治疗精神分裂症、强迫型人格障碍、重性抑郁症、躁郁症、焦虑症、正常老化、癫痫症、视网膜变性、脑外伤、脊椎损伤、创伤后压力症、恐慌症、帕金森氏(Parkinson's)病、痴呆、阿兹海默氏(Alzheimer's)病、认知障碍、化疗引起之认知功能障碍(「化疗脑(chemobrain)」)、唐氏(Down)症侯群、自闭症谱系障碍、听力损失、耳鸣、脊髓小脑性共济失调、肌萎缩性脊髓侧索硬化症、多发性硬化、亨廷顿氏(Huntington's)病、中风、及归因于放射治疗、慢性压力、视神经病变或黄斑变性或选自酒精、鸦片剂、甲基苯丙胺、苯环己哌啶及可卡因之神经活性药物滥用之紊乱。; R 2 is hydrogen; R 3 is hydrogen, lower alkyl substituted by halogen, -(CH2)n-S(O)2-lower alkyl, -(CH2)n- cycloalkyl or -(CH2)n-lower alkoxy; R 4 is hydrogen or lower alkyl; n is 0, 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. ;The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson’s disease, dementia, Alzheimer’s disease, cognitive impairment, chemotherapy-induced cognitive dysfunction ("chemobrain"), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington’s disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs, selected from alcohol, opiates, methamphetamine, phencyclidine and cocaine.
申请公布号 TW201516044 申请公布日期 2015.05.01
申请号 TW103125591 申请日期 2014.07.25
申请人 赫孚孟拉罗股份公司 F. HOFFMANN-LA ROCHE AG 发明人 希卡雷利 西蒙纳M CECCARELLI, SIMONA M.;贾葛西亚 雷维 JAGASIA, RAVI;杰考伯 罗尼 罗兰 JAKOB-ROETNE, ROLAND;彼得斯 詹士 乌伊 PETERS, JENS-UWE;威奇曼 吉尔金 WICHMANN, JUERGEN
分类号 C07D471/04(2006.01);A61K31/4375(2006.01);A61K31/444(2006.01);A61K31/4545(2006.01);A61K31/5377(2006.01);A61P25/00(2006.01) 主分类号 C07D471/04(2006.01)
代理机构 代理人 陈长文
主权项
地址 瑞士 CH