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    PYRIMIDINE DERIVATIVES
    1.
    发明申请
    PYRIMIDINE DERIVATIVES 审中-公开

    公开(公告)号：US20100267755A1

    公开(公告)日：2010-10-21

    申请号：US10477546

    申请日：2002-05-23

    申请人： Gianpaolo Bravi ,  Malcolm Clive Carter ,  Richard Howard Green ,  Jennifer Margaret Doughty ,  Charles David Hartley ,  Alan Naylor ,  Martin Pass ,  Jeremy John Payne ,  Neil Anthony Pegg

    发明人： Gianpaolo Bravi ,  Malcolm Clive Carter ,  Richard Howard Green ,  Jennifer Margaret Doughty ,  Charles David Hartley ,  Alan Naylor ,  Martin Pass ,  Jeremy John Payne ,  Neil Anthony Pegg

    IPC分类号： A61K31/505 ,  A61P29/00 ,  C07D239/42 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/506

    CPC分类号： C07D239/42 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R1 and R2 are independently selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR7R8)n and B(CR7R8)n; R3 is selected from the group consisting of C1-6alkyl, NH2 and R10CONH; R4 is C1-2alkyl substituted by one to five fluorine atoms; R5 is selected from the group consisting of H, C1-4alkyl, C1-2alkyl substituted with one to five fluorine atoms, halogen and C3-10cycloalkylC0-6alkyl, with the proviso that when R6 is H R5 is not H. R6 is selected from the group consisting of H, C1-4alkyl, C1-2alkyl substituted with one to five fluorine atoms, halogen, C1-4alkoxy, CN, NO2, C1-6alkylOCO, NH2CO, C1-6alkylNHCO, NH2, C1-6alkylNH, (C1-6alkyl)2N, (C1-6alkyl)2NCO, C1-6alkylCONH, NH2SO2, C1-6alkylNHSO2, (C1-6alkyl)2NSO2, C1-6alkylSO2NH, ArSO2NH, C1-6alkylSO2, ArSO2, C3-10cycloalkylC0-6alkyl, C3-6alkenyl and C3-6alkynyl, with the proviso that when R5 is H R6 is not H. R7 and R8 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R9; R9 is selected from the group consisting of hydroxy, halogen, C1-6alkyl, C1-6alkyl substituted by one more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; R10 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCOC1-6alkyl, C1-6alkylOCO, H2NC1-6alkyl, C1-6alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl; B is selected from the group consisting of defines the point of attachment of the ring; and n is 0 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of pain, fever and inflammation of a variety of conditions and diseases.

    Pyrimidine derivatives as selective inhibitors of cox-2
    5.
    发明授权
    Pyrimidine derivatives as selective inhibitors of cox-2 失效
    嘧啶衍生物作为cox-2的选择性抑制剂

    公开(公告)号：US07074802B2

    公开(公告)日：2006-07-11

    申请号：US10477819

    申请日：2002-05-23

    申请人： Jennifer Doughty, legal representative ,  Charles David Hartley ,  Alan Naylor ,  Jeremy John Payne ,  Neil Anthony Pegg

    发明人： Richard Howard Doughty, deceased

    IPC分类号： C07D239/42 ,  A61K31/505

    CPC分类号： C07D239/42

    摘要： The invention thus provides the compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R1 and R2 are independently selected from the group consisting of H, C1-6alkyl, C2-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl and C4-12bridged cycloalkyl; R3 is selected from the group consisting of C1-6alkyl, NH2 and R5CONH; R4 is selected from the group consisting of CH2F, CHF2, CF3CH2, CF3CHF and CF3CF2; and R5 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCOC1-6alkyl, C1-6alkylOCO, H2NC1-6alkyl, C1-6alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

    摘要翻译： 因此，本发明提供式（I）化合物及其药学上可接受的盐，其中：R 1和R 2独立地选自H，C C 1-6烷基，C 2-6链烯基，C 3-6亚炔基，C 3-10环烷基C 0-6个烷基和C 4-12-12桥连环烷基; R 3选自C 1-6烷基，NH 2和R 5 CONH; R 4选自CH 2，CH 2，CH 3，CH 3，CH 3，CH 3， 2，CF 3 CHF和CF 3 3 CF 2; 和R 5选自H，C 1-6烷基，C 1-6烷氧基，C 1 C 1-6烷基，C 1-6烷基，苯基，HO 2 C 1-6烷基，C 1-6 C 1-6烷基，C 1-6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 烷基，C 1-6烷基，C 1-6烷基和C 1-6烷基CONHC 1-6烷基。 式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，各种病症和疾病的炎症。