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    • 9. 发明申请
    • ANGIOTENSIN II RECEPTOR ANTAGONISTS
    • ANGIOTENSIN II受体拮抗剂
    • WO2008076245A2
    • 2008-06-26
    • PCT/US2007/025231
    • 2007-12-11
    • MERCK & CO., INC.SEBHAT, Iyassu, K.LO, Michael, Man-ChuNARGUND, Ravi, P.ALI, Amjad
    • SEBHAT, Iyassu, K.LO, Michael, Man-ChuNARGUND, Ravi, P.ALI, Amjad
    • C07D403/10A61K31/41A61P9/12
    • C07D403/10
    • A compound having the structure (Formula I), wherein Y is -Y 1 -Y 2 -Y 3 -Y 4 -Y 5 -; Y 1 is C(O) or C(R 1 R 2 ); Y 2 is O, C(O), P(O)(OH) or CH 2 , provided that when Y 1 is C(O), Y 2 is not C(O); R 1 is selected from the group consisting of hydrogen and C 1-4 alkyl; R 2 is selected from the group consisting of hydrogen, C 1-4 alkyl, and -OC(O)C 1-4 alkyl; Y 3 is O, C(O) or CH 2 , provided that when Y 2 is C(O), then Y 3 is not C(O), and further provided that when Y 2 is O, then Y 3 is not O; Y 4 is O or CH 2 or is absent, provided that when Y 3 is O, then Y 4 is not O; Y5 is -(CH 2 ) 1-2 -(X) 0- l -(CH 2 ) 0-l - or is absent; X is -O- or -CR 3 R 4 -; and R 3 and R 4 are independently selected from the group consisting of hydrogen and C 1 -C 4 alkyl; or a pharmaceutically acceptable salt thereof, which is useful for treating hypertension.
    • 具有结构(式I)的化合物,其中Y为-Y 1 -Y 2 -Y 3 -Y 4 - / SUP> -Y 5 - ; Y 1是C(O)或C(R 1 R 2)2)。 Y 2是O,C(O),P(O)(OH)或CH 2,条件是当Y 1是C( O),Y 2不是C(O); R 1选自氢和C 1-4烷基; R 2选自氢,C 1-4烷基和-OC(O)C 1-4烷基; Y 3是O,C(O)或CH 2,条件是当Y 2是C(O)时,则Y 3不是C(O),并且进一步地,当Y 2为O时,Y 3不为O; Y 4是O或CH 2或不存在,条件是当Y 3为O时,则Y 4为O, 不是O Y 5是 - (CH 2)2 - (X)0-1 - (CH 2)2 - 0-1 - 或不存在; X是-O-或-CR 3 R 4 - 。 和R 3和R 4独立地选自氢和C 1 -C 4烷基 ; 或其药学上可接受的盐,其可用于治疗高血压。