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六氫吡啶衍生物
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
KOLCZEWSKI, SABINE,考佐斯基 沙宾,考佐斯基 沙賓,PINARD, EMMANUEL,匹纳德 艾曼纽,匹納德 艾曼紐,STALDER, HENRI,史托德 亨利,考佐斯基 沙宾,考佐斯基 沙賓,匹纳德 艾曼纽,匹納德 艾曼紐,史托德 亨利
申请号:
TW099101973
公开号:
TWI403322B
申请日:
2010.01.25
申请国别(地区):
TW
年份:
2013
代理人:
摘要:
The present invention relates to a compound of general formula Iwherein R1 is hydrogen, lower alkyl, CD3, -(CH2)n-CHO, -(CH2)n-O-lower alkyl, -(CH2)n-OH, -(CH2)n-cycloalkyl or is heterocycloalkyl; R2 is hydrogen, halogen, hydroxy, lower alkyl, di-lower alkyl, -OCH2-O-lower alkyl, or lower alkoxy; or the piperidin ring form together with R2a spiro ring, selected from 4-aza-spiro[2.5]oct-6-yl; Ar is aryl or heteroaryl, which are optionally substituted by one, two or three substituents, selected from halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl, lower alkoxy, S-lower alkyl, heteroaryl, heterocycloalkyl, or by phenyl optionally substituted by R', and R' is halogen, lower alkyl, lower alkoxy or lower alkoxy substituted by halogen, or is heteroaryl; R is lower alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, wherein aryl and heteroaryl are optionally substituted by one or two R'; n is 0, 1 2 or 3; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof.Furthermore, the present invention relates to pharmaceutical compositions containing the compounds of formula I and to their use in the treatment of neurological and neuropsychiatric disorders.本發明係關於一種通式I之化合物其中R1 為氫、低碳烷基、CD3、-(CH2)n-CHO、-(CH2)n-O-低碳烷基、-(CH2)n-OH、-(CH2)n-環烷基或雜環烷基;R2 為氫、鹵素、羥基、低碳烷基、二低碳烷基、-OCH2-O-低碳烷基或低碳烷氧基;或六氫吡啶環與R2一起形成螺環,其選自4-氮雜-螺[2.5]辛-6-基;Ar 為芳基或雜芳基,其視情況經1、2或3個選自鹵素、低碳烷基、經鹵素取代之低碳烷基、經鹵素取代之低碳烷氧基、環烷基、低碳烷氧基、S-低碳烷基、雜芳基、雜環烷基之取代基取代,或經視情況經R'取代之苯基取代,及R' 為鹵素、低碳烷基、低碳烷氧基或經鹵素取代之低碳烷氧基,或為雜芳基;R 為低碳烷基、環烷基、雜環烷基、芳基或雜芳基,其中芳基及雜芳基視情況經1或2個R'取代;n 為0、1、2或3;或其醫藥學上可接受之酸加成鹽、外消旋混合物或其相應對映異構體及/或光學異構體。此外,本發明係關於一種含有式I化合物之醫藥組合物及其於治療神經病症及神經精神病症中之用途。
来源网站:
中国工程科技知识中心
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