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哌并[1,2-a]吲哚-1-酮及[1,4]二氮呯并[1,2-a]吲哚-1-酮
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
JAGASIA, RAVI,贾葛西亚 雷维,賈葛西亞 雷維,JAKOB-ROETNE, ROLAND,杰考伯 罗尼 罗兰,傑考伯 羅尼 羅蘭,WICHMANN, JUERGEN,威奇曼 吉尔金,威奇曼 吉爾金,贾葛西亚 雷维,賈葛西亞 雷維,杰考伯 罗尼 罗兰,傑考伯 羅尼 羅蘭,威奇曼 吉尔金,威奇曼 吉爾金
申请号:
TW103111999
公开号:
TW201443056A
申请日:
2014.03.31
申请国别(地区):
TW
年份:
2014
代理人:
摘要:
The present invention relates to compounds of general formula I wherein R1 is halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or cyano; R2 is hydrogen, CF3 or lower alkyl; R3 is hydrogen, lower alkyl, lower alkenyl, lower alkinyl, heterocyeloalkyl, lower alkyl substitueted by cyano, cyano, benzyl substituted by halogen, 2-oxa-6-aza-spiro[3.3]hept-6-yl or is lower alkoxy substituted by halogen; X is -CH2- or -CH2-CH2-; 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, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington’s disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.本發明係關於通式I之化合物其中:R1 為鹵素、低碳數烷基、低碳數烷氧基、經鹵素取代之低碳數烷基、經鹵素取代之低碳數烷氧基或氰基;R2 為氫、CF3或低碳數烷基;R3 為氫、低碳數烷基、低碳數烯基、低碳數炔基、雜環烷基、經氰基取代之低碳數烷基、氰基、經鹵素取代之苄基、2-氧雜-6-氮雜-螺[3.3]庚-6-基或為經鹵素取代之低碳數烷氧基;X為-CH2-或-CH2-CH2-;或關於其醫藥上可接受之酸加成鹽,關於其外消旋混合物或其對應鏡像異構體及/或光學異構體。該等化合物可用於治療精神分裂症、強迫型人格障礙、嚴重抑鬱症、躁鬱症、焦慮症、正常老化、癲癇症、視網膜退化、創傷性腦損傷、脊髓損傷、創傷後壓力症、恐慌症、帕金森氏症(Parkinson’s disease)、癡呆、阿茲海默氏症(Alzheimer’s disease)、輕度認知受損、化學療法誘發之認知功能障礙、唐氏症候群(Down syndrome)、自閉症系列障礙、聽力損失、耳鳴、脊髓小腦共濟失調、肌萎縮性側索硬化症、多發性硬化症、亨丁頓氏症(Huntington’s disease)、中風、放射治療、慢性壓力、神經活性藥物(諸如酒精、鴉片、甲基安非他命(methamphetamine)、苯環己哌啶(phencyclidine)及古柯鹼)濫用。
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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