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公开(公告)号:US07855211B2
公开(公告)日:2010-12-21
申请号:US12637789
申请日:2009-12-15
申请人: David A Coates , Lawrence Mark Gelbert , John M. Knobeloch , Alfonso De Dios Magana , Ana De Prado Gonzalez , Miriam Filadelfa Del Prado Catalina , Maria Cristina Garcia Paredes , Eva Maria Martin De La Nava , Maria Dolores Martin Ortega Finger , Jose Antonio Martinez Perez , Ana Isabel Mateo Herranz , Carlos Perez Martinez , Concepcion Sanchez Martinez
发明人: David A Coates , Lawrence Mark Gelbert , John M. Knobeloch , Alfonso De Dios Magana , Ana De Prado Gonzalez , Miriam Filadelfa Del Prado Catalina , Maria Cristina Garcia Paredes , Eva Maria Martin De La Nava , Maria Dolores Martin Ortega Finger , Jose Antonio Martinez Perez , Ana Isabel Mateo Herranz , Carlos Perez Martinez , Concepcion Sanchez Martinez
IPC分类号: C07D401/14 , A61K31/517
CPC分类号: C07D401/14
摘要: The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof which is useful in the treatment of cell proliferative diseases.
摘要翻译: 本发明提供了可用于治疗细胞增殖性疾病的式(I)化合物或其药学上可接受的盐。
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公开(公告)号:US07915424B2
公开(公告)日:2011-03-29
申请号:US10598512
申请日:2005-03-09
申请人: Francisco Javier Agejas-Chicharro , Bruce Anthony Dressman , Jose Antonio Martinez Perez , James Allen Monn , Mohammad Sadegh Zia-Ebrahimi , Sonia Gutierrez Sanfeliciano , Steven Marc Massey , Steven Scott Henry
发明人: Francisco Javier Agejas-Chicharro , Bruce Anthony Dressman , Jose Antonio Martinez Perez , James Allen Monn , Mohammad Sadegh Zia-Ebrahimi , Sonia Gutierrez Sanfeliciano , Steven Marc Massey , Steven Scott Henry
IPC分类号: C07D211/78
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.
摘要翻译: 本发明涉及式(I)的吡啶基衍生物作为mGlu5受体的拮抗剂。 因此,这些化合物可用于治疗或预防通过拮抗mGlu5受体治疗的病症,其中Ar是苯基或萘基,其各自可被一个或多个C 1 -C 4烷基,C 1 -C 4烷氧基,C 1 -C 5 酰基,卤素,氨基,硝基,氰基,羟基,C 1 -C 5酰基氨基,C 1 -C 4烷基磺酰基氨基,单 - ,二 - 或三氟化的C 1 -C 3烷基,可以相同或不同并且可以具有CONH 2,CONHCH 3, CON(CH 3)2,CO 2 H,CO 2 CH 3,OCF 3,CH 2 NHCOCH 3,CH 2 NH 2,CH 2 N(CH 3)2,CH 2 CN,CH 2 OH,CH 2 NHSO 2 CH 3,CH 2 N(CH 3)(CH 2)2 CN,CH 2 N(CH 3)CH(CH 3) CH3)2,CH2NH(CH2)2CH3,CH2NHCO2R4,CH2NHCH2CH3,CH2NHCH3 NHCOC(CH3)2或N(S(O)2CH3)2取代基; R1是氢,卤素,R4,CN,C(NOH)R3,C(NO-R4)R3,(CH)2CO2R4,(CH2)n OR3,COR3,CF3,SR4,S(O)R4,S )NH 2,NHCOR 3,C(NOR 3)NH 2,CH 2 OCOR 3,(CH 2)n NH 2,CON(CH 3)2(CH 2)n NHCO 2 R 4,CO 2 R 3,CONH 2,CSNH 2,C(NH)NHOR 3,(CH 2)n N )2或CONHNHCOR3; R2是1,2-乙烯二基或1,2-亚乙炔基; R3是氢或C1-C4烷基; R4是C1-C4烷基; 且n为0,1,2,3或4; 或其药学上可接受的盐或其N-氧化物。
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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.
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