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    DIAZENIUMDIOLATE CYCLOPENTYL DERIVATIVES
    4.
    发明申请
    DIAZENIUMDIOLATE CYCLOPENTYL DERIVATIVES 有权
    二氮杂环戊烷衍生物

    公开(公告)号：US20130053352A1

    公开(公告)日：2013-02-28

    申请号：US13577797

    申请日：2011-02-10

    申请人： Amjad Ali ,  Michael Man-Chu Lo ,  Edward Metzger ,  Lin Yan

    发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Edward Metzger ,  Lin Yan

    IPC分类号： A61K31/655 ,  A61P9/12 ,  C07D249/04 ,  C07C245/24

    CPC分类号： C07C291/00 ,  C07C291/08 ,  C07C2601/08 ,  C07D249/04

    摘要： A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen, —OH, —O—C1-6 alkyl, ═O, or halogen; R2 is hydrogen, C(O)OR8, C6H5C(O)OR8, (CH2)1-2OH, CR9R10OH, C(O)O(CH2)0-2 aryl, C(O)NR9R10, C(O)SO2NR9R10, C6H5OR9, W—C(O)OR8, W—OR9, Y, or P(O)(OR9)(ORlO); R3 is hydrogen or —C1-6 alkyl; R4 is hydrogen, —OH or —C(O)OR9; R5 is hydrogen or deuterium; R6 and R7 are independently —C1-6 alkyl, fluoro-substituted —C1-6 alkyl, deutero-substituted —C1-6 alkyl or —(CH2)1-2R11, wherein any carbon atom of the fluoro-substituted —C1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted —C1-6 alkyl is mono- or di-substituted with fluoro; R8, in each instance in which it occurs, is independently hydrogen, —C1-6 alkyl, or —(CH2)2N+(CH3)3; R9 and R10, in each instance in which they occur, are independently —C1-6 alkyl; R11 is —OH, —O—C1-6 alkyl, -0CD3, —OC(O)OC1-6 alkyl, —NH2, —C6H5, —N3, or W; W is an unsubslituted 5- or 6-raembered heteroaryl ring having 1, 2, or 3 nitrogen atoms, or a substituted 5- or 6-membered heteroaryl ring having 1, 2, or 3 nitrogen atoms that is mono- or di-substituted at any carbon atom with R6 or R7; Y is a 5- or 6-membered heterocyclic ring having 1, 2, 3 or 4 heteroatoms which are N, O, or S or stereoisomers thereof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using the compounds for treating hypertension.

    摘要翻译： 具有结构或其药学上可接受的盐的化合物，其中R 1是氢，-OH，-O-C 1-6烷基，= O或卤素; R2是氢，C（O）OR8，C6H5C（O）OR8，（CH2）1-2OH，CR9R10OH，C（O）O（CH2）O2芳基，C（O）NR9R10，C（O）SO2NR9R10， C6H5OR9，W-C（O）OR8，W-OR9，Y或P（O）（OR9）（OR10）。 R3是氢或-C 1-6烷基; R4是氢，-OH或-C（O）OR9; R5是氢或氘; R 6和R 7独立地是C 1-6烷基，氟取代的C 1-6烷基，取代的C 1-6烷基或 - （CH 2）1-2 R 11，其中氟取代的-C 1-6的任何碳原子 烷基被氟单取代或二取代，氘取代的C 1-6烷基的任何碳原子被氟单取代或二取代; 在其每次发生的情况下，R 8独立地为氢，-C 1-6烷基或 - （CH 2）2 N +（CH 3）3; 在其各自出现的情况下，R 9和R 10独立地为-C 1-6烷基; R 11是-OH，-O-C 1-6烷基，-CD 3，-OC（O）OC 1-6烷基，-NH 2，-C 6 H 5，-N 3或W; W是具有1,2或3个氮原子的未取代的5-或6-元杂芳基环，或具有1,2或3个氮原子的取代的5-或6-元杂芳基环，其被单取代或二取代 在任何具有R6或R7的碳原子上; Y是具有1,2,3或4个杂原子的5或6元杂环，其为N，O或S或其立体异构体，或其药学上可接受的盐，或其立体异构体的药学上可接受的盐，以及使用 用于治疗高血压的化合物。

    Angiotensin II receptor antagonists
    8.
    发明授权
    Angiotensin II receptor antagonists 有权
    血管紧张素II受体拮抗剂

    公开(公告)号：US07834042B2

    公开(公告)日：2010-11-16

    申请号：US12312225

    申请日：2007-12-11

    申请人： Iyassu K. Sebhat ,  Michael Man-chu Lo ,  Ravi P. Nargund ,  Amjad Ali

    发明人： Iyassu K. Sebhat ,  Michael Man-chu Lo ,  Ravi P. Nargund ,  Amjad Ali

    IPC分类号： A61K31/41 ,  C07D257/04

    CPC分类号： C07D209/10 ,  C07C65/21 ,  C07C215/82 ,  C07C217/92 ,  C07D209/12 ,  C07D307/80 ,  C07D319/18 ,  C07D401/06 ,  C07D403/10 ,  C07D405/04 ,  C07D409/04

    摘要： A compound having the structure (Formula I), wherein Y is —Y1—Y2—Y3—Y4—Y5—; Y1 is C(O) or C(R1R2); Y2 is O, C(O), P(O)(OH) or CH2, provided that when Y1 is C(O), Y2 is not C(O); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the pup consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y3 is O, C(O) or CH2, provided that when Y2 is C(O), then Y3 is not C(O), and further provided that when Y2 is O, then Y3 is not O; Y4 is O or CH2 or is absent, provided that when Y3 is O, then Y4 is not O; Y5 is —(CH2)1-2—(X)0-1—(CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt thereof, which is useful for treating hypertension.

    摘要翻译： 具有结构（式I）的化合物，其中Y为-Y1-Y2-Y3-Y4-Y5-; Y1是C（O）或C（R1R2）; Y2是O，C（O），P（O）（OH）或CH2，条件是当Y1是C（O）时，Y2不是C（O）; R 1选自氢和C 1-4烷基; R2选自由氢，C 1-4烷基和-OC（O）C 1-4烷基组成的小鼠; Y3为O，C（O）或CH2，条件是当Y2为C（O）时，Y3不为C（O），进一步规定，当Y2为O时，Y3不为O; Y4为O或CH2或不存在，条件是当Y 3为O时，Y 4不为O; Y 5是 - （CH 2）1-2 - （X）0-1 - （CH 2）0-1-或不存在; X是-O-或-CR 3 R 4 - ; 并且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。

    ANGIOTENSIN II RECEPTOR ANTAGONISTS
    9.
    发明申请
    ANGIOTENSIN II RECEPTOR ANTAGONISTS 失效
    ANGIOTENSIN II受体拮抗剂

    公开(公告)号：US20100273845A1

    公开(公告)日：2010-10-28

    申请号：US12743402

    申请日：2008-11-21

    申请人： Amjad Ali ,  Michael Man-Chu Lo ,  Chris Franklin ,  Nicoletta Almirante ,  Silvia Stefanini ,  Laura Storoni ,  Stefano Biondi ,  Ennio Ongini

    发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Chris Franklin ,  Nicoletta Almirante ,  Silvia Stefanini ,  Laura Storoni ,  Stefano Biondi ,  Ennio Ongini

    IPC分类号： A61K31/4184 ,  C07D403/10 ,  A61P9/12 ,  A61K31/4178

    CPC分类号： C07D403/10

    摘要： A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is 1) —(CH2)3R5, 2) —C(O)(CH2)2R5, 3) —C(R1R2)OC(O)O(CH2)nR5, wherein n is 1 or 2, 4) —C(R1R2)OC(O)CH2CH2R5, 5) —C(R1R2)OC(O)OCH2CH2C(R3R4)R5, provided that when Y is —C(O)(CH2)2R5, then R is R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is —CH(ONO2)CH(ONO2)R6; R6 is selected from CH3, CH2CH3 and CH(CH3)2; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.

    摘要翻译： 具有结构的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是1） - （CH 2）3 R 5，2）-C（O）（CH 2）2 R 5，3）-C（R 1 R 2）OC（O）O （CH 2）n R 5，其中n为1或2，4）-C（R 1 R 2）OC（O）CH 2 CH 2 R 5，5）-C（R 1 R 2）OC（O）OCH 2 CH 2 C（R 3 R 4） O）（CH 2）2 R 5，则R 1是R 1，R 2，R 3和R 4独立地选自氢和C 1-4烷基; R5是-CH（ONO2）CH（ONO2）R6; R 6选自CH 3，CH 2 CH 3和CH（CH 3）2; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

    Angiotensin II receptor antagonists
    10.
    发明申请
    Angiotensin II receptor antagonists 有权
    血管紧张素II受体拮抗剂

    公开(公告)号：US20080194660A1

    公开(公告)日：2008-08-14

    申请号：US12000247

    申请日：2007-12-11

    申请人： Iyassu K. Sebhat ,  Michael Man-chu Lo ,  Ravi P. Nargund ,  Amjad Ali ,  Chris Franklin ,  Nicoletta Almirante ,  Laura Storoni ,  Silvia Stefanini

    发明人： Iyassu K. Sebhat ,  Michael Man-chu Lo ,  Ravi P. Nargund ,  Amjad Ali ,  Chris Franklin ,  Nicoletta Almirante ,  Laura Storoni ,  Silvia Stefanini

    IPC分类号： A61K31/41 ,  C07D257/04 ,  A61P9/12

    CPC分类号： C07D403/10

    摘要： A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is -Y1-Y2-Y3-Y4-Y5-; Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is —(CH2)1-2—(X)0-1—(CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.

    摘要翻译： 具有其中R是血管紧张素受体拮抗剂活性基团的结构的化合物，Y是-Y 1 -Y 2 -Y 3 -Y 3， SUP> 4 Y 1是C（R 1 R 2）2）。 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 2是O或CH 2; Y 3是C（O）或CH 2 O 2; Y 4是O或CH 2; （CH 2）2 - （X）0-1 - （CH 3） 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或水合物，其可用于治疗高血压。