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公开(公告)号:US20080194647A1
公开(公告)日:2008-08-14
申请号:US10598512
申请日:2005-03-09
申请人: Francisco Javier Agejas-Chicharro , Anthony Bruce Dressman , Sonia Gutierrez Sanfeliciano , Steven Scott Henry , Jose Antonio Martinez Perez , Steven Marc Massey , James Allen Monn , Mohammad Sadegh Zia-Ebrahimi
发明人: Francisco Javier Agejas-Chicharro , Anthony Bruce Dressman , Sonia Gutierrez Sanfeliciano , Steven Scott Henry , Jose Antonio Martinez Perez , Steven Marc Massey , James Allen Monn , Mohammad Sadegh Zia-Ebrahimi
IPC分类号: A61K31/44 , C07D213/16 , A61P29/00
CPC分类号: C07D213/89 , C07D213/16 , C07D213/26 , C07D213/48 , C07D213/55 , C07D213/57 , C07D213/61 , C07D213/65 , C07D213/73 , C07D213/75 , C07D213/78 , C07D213/80 , C07D213/85
摘要: The present invention is directed toward pyridyl derivatives of formula (I) as antagonists of the mGlu5 receptor. As such the compounds may be useful for treatment or prevention of disorders remedied by antagonism of the mGlu5 receptor, wherein Ar is phenyl or napthyl each of which may be substituted by one or more C1-C4 alkyl, C1-C4 alkoxy, C1-C5 acyl, halo, amino, nitro, cyano, hydroxy, C1-C5 acylamino, C1-C4 alkylsulfonylamino, mono-, di- or trifluorinated C1-C3 alkyl, substituents which may be the same or different and may bear a CONH2, CONHCH3, CON(CH3)2, CO2H, CO2CH3, OCF3, CH2NHCOCH3, CH2NH2, CH2N(CH3)2, CH2CN, CH2OH, CH2NHSO2CH3, CH2N(CH3)(CH2)2 CN, CH2N(CH3)CH(CH3)2, CH2NHCH(CH3)2, CH2NH(CH2)2CH3, CH2NHCO2R4, CH2NHCH2CH3, CH2NHCH3 NHCOC(CH3)2, or N(S(O)2CH3)2 substituent; R1 is hydrogen, halo, R4, CN, C(NOH)R3, C(NO—R4)R3, (CH)2CO2R4, (CH2)n OR3, COR3, CF3, SR4, S(O)R4, S(O)2R4, COCH2CO2R3, NHSO2R4, NHCOR3, C(NOR3)NH2, CH2OCOR3, (CH2)nNH2, CON(CH3)2 (CH2)nNHCO2R4, CO2R3, CONH2, CSNH2, C(NH)NHOR3, (CH2)nN(CH3)2, or CONHNHCOR3; R2 is 1,2-ethenediyl or 1,2-ethynediyl; R3 is hydrogen or C1-C4 alkyl; R4 is C1-C4 alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof, or an N-oxide thereof.