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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:
CECCARELLI, SIMONA M.,希卡雷利 西蒙纳M,希卡雷利 西蒙納M,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,希卡雷利 西蒙纳M,希卡雷利 西蒙納M,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:
TW102128001
公开号:
TWI506027B
申请日:
2013.08.05
申请国别(地区):
TW
年份:
2015
代理人:
摘要:
The present invention relates to compounds of general formula Iwherein R1is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen or cyano; R2is hydrogen, lower alkyl or lower alkyl substituted by halogen; R3is phenyl, benzo[1,3]dioxolyl, 2,3-dihydro-benzofuran-5-yl or a 5- and 6-membered heteroaryl, wherein phenyl and the 5- and 6-rnembered heteroaryl groups may be substituted by one or more substituents, selected from cyano, nitro, amino and lower di-alkylamino, lower alkyl sulfonyl, lower alkoxy, lower alkoxy substituted by halogen, halogen, lower alkyl, lower alkyl substituted by halogen or lower alkyl substituted by hydroxyl; X is -CH(lower alkyl)-, -CH2-, -CH2CH2- or -CH(lower alkyl)CH2-; R is hydrogen or lower alkyl; n is 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, 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係氫、鹵素、低碳數烷基、低碳數烷氧基、由鹵素取代之低碳數烷氧基或氰基;R2係氫、低碳數烷基或由鹵素取代之低碳數烷基;R3係苯基、苯并[1,3]二氧雜環戊烯基、2,3-二氫-苯并呋喃-5-基或5員及6員雜芳基,其中苯基及5員及6員雜芳基可由一或多個選自以下基團之取代基取代:氰基、硝基、胺基及低碳數二烷基胺基、低碳數烷基磺醯基、低碳數烷氧基、由鹵素取代之低碳數烷氧基、鹵素、低碳數烷基、由鹵素取代之低碳數烷基或由羥基取代之低碳數烷基;X係-CH(低碳數烷基)-、-CH2-、-CH2CH2-或-CH(低碳數烷基)CH2-;R係氫或低碳數烷基;n係1或2;或係關於其醫藥上可接受之酸加成鹽,係關於其外消旋混合物或係
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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