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乙炔基衍生物
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
JAESCHKE, GEORG,杰许柯 乔治,傑許柯 喬治,JOLIDON, SYNESE,裘里敦 西尼斯,LINDEMANN, LOTHAR,林德曼 洛撒,STADLER, HEINZ,史丹勒 韩兹,史丹勒 韓茲,VIEIRA, ERIC,维拉 艾瑞克,維拉 艾瑞克,杰许柯 乔治,傑許柯 喬治,裘里敦 西尼斯,林德曼 洛撒,史丹勒 韩兹,史丹勒 韓茲,维拉 艾瑞克,維拉 艾瑞克
申请号:
TW101114577
公开号:
TW201311657A
申请日:
2012.04.24
申请国别(地区):
TW
年份:
2013
代理人:
摘要:
The present invention relates to ethynyl derivatives of formula I wherein X is N or C-R, wherein R is hydrogen or halogen; G is N or CH; with the proviso that maximum one of G or X can be nitrogen; R1 is phenyl or pyridinyl, which are optionally substituted by halogen; R2 is hydrogen, lower alkyl, hydroxy, lower alkoxy or C(O)O-benzyl; R3, R3’, R4, R4’, R6, R6’ are independently from each other hydrogen or lower alkyl; or R6 and R4 may form together with the carbon atom to which they are attached a C4-6-cycloalkyl ring, if m is 0 and n is 1 or 2; R5 is hydrogen or lower alkyl; n is 0, 1 or 2; m is 0 or 1; with the proviso that n and m are not simultaneously 0; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They may be used for the treatment of schizophrenia or cognitive disorders.本發明係關於式I之乙炔基衍生物:其中X 係N或C-R,其中R係氫或鹵素;G 係N或CH;限制條件為G或X中至多一個可為氮;R1 係苯基或吡啶基,其視需要經鹵素取代;R2 係氫、低碳數烷基、羥基、低碳數烷氧基或C(O)O-苄基;R3、R3'、R4、R4'、R6、R6' 相互獨立地為氫或低碳數烷基;或若m係0且n係1或2,則R6及R4可與其等所連接之碳原子一起形成C4-6-環烷基環;R5 係氫或低碳數烷基;n 係0、1或2;m 係0或1;限制條件為n及m不同時為0;或其醫藥上可接受的酸加成鹽、外消旋混合物、或其相應的對映異構體及/或光學異構體及/或立體異構體。現已驚訝地發現該等通式I化合物係代謝型麩胺酸受體亞型5(mGluR5)之正向異位調節劑(PAM)。其可用於治療精神分裂症或認知障礙。
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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