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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.

    Acyl dihydro pyrrole derivatives as hcv inhibitors
    9.
    发明申请
    Acyl dihydro pyrrole derivatives as hcv inhibitors 审中-公开
    酰基二氢吡咯衍生物作为hcv抑制剂

    公开(公告)号：US20050009873A1

    公开(公告)日：2005-01-13

    申请号：US10494121

    申请日：2002-10-30

    申请人： Gianpaolo Bravi ,  Peter Howes ,  Victoria Lovegrove ,  Pritom Shah ,  Martin Slater

    发明人： Gianpaolo Bravi ,  Peter Howes ,  Victoria Lovegrove ,  Pritom Shah ,  Martin Slater

    IPC分类号： A61K31/4025 ,  A61P31/12 ,  A61P31/14 ,  A61P31/20 ,  C07D417/04 ,  C07 ,  A61K31/401 ,  A61K31/454

    CPC分类号： C07D417/04

    摘要： Novel anti-viral agents of Formula (I) wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; D represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; E represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts and solvates thereof, processes for their preparation and methods of using them in HCV treatment are provided.

    摘要翻译： 式（I）的新型抗病毒剂，其中：A表示OR 1，NR 1 R 2或R 1，其中R 1和R 2为氢，C 1-6烷基， 芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 1和R 2与它们所连接的氮原子一起形成5或6元饱和环状基团; B表示C（O）R 3，其中R 3是C 1-6烷基，芳基，杂芳基，芳烷基或杂芳基烷基; D表示C 1-6烷基，芳基，杂芳基或杂环基; E表示OR 1，NR 1 R 2或R 1，其中R 1和R 2是氢，C 1-6烷基，芳基，杂芳基，芳烷基或杂芳基烷基; 或R 1和R 2与它们所连接的氮原子一起形成5或6元饱和环状基团; F表示氢，C 1-6烷基，芳基或杂芳基; 和G表示氢，C 1-6烷基，杂环基烷基，芳基烷基或杂芳基烷基; 并提供其盐和溶剂化物，其制备方法及其在HCV治疗中的使用方法。