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    ANGIOTENSIN II RECEPTOR ANTAGONISTS
    4.
    发明申请
    ANGIOTENSIN II RECEPTOR ANTAGONISTS 有权
    ANGIOTENSIN II受体拮抗剂

    公开(公告)号：US20100292192A1

    公开(公告)日：2010-11-18

    申请号：US12812547

    申请日：2009-01-08

    申请人： Amjad Ali ,  Michael Man-Chu Lo ,  Christopher Franklin ,  Brent R. Whitehead

    发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Christopher Franklin ,  Brent R. Whitehead

    IPC分类号： A61K31/655 ,  C07C245/24 ,  A61P9/12 ,  A61P7/10

    CPC分类号： C07D403/10 ,  C07D235/20 ,  C07D257/04 ,  C07D401/14 ,  C07D409/06

    摘要： A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and 2) —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5;Z is —O— or —(CR14R15)_; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N═N(O)—NR3R4; 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选自和：2）-C（R 1 H）OC（O）X（（CR 12 R 13） - （CHR 10）m - （CH 2）n -Z-（CH 2）q - （CHR 11）r - （CR 16 R 17）） - R 5; Z是-O-或 - （CR14R15）_; m，n，p，q和r独立地选自0和1组成的组; X是-O-或 - （CR 18 R 19） - ; R1选自氢，C1-4烷基，芳基和C1-4烷基芳基; R5是-O-N = N（O）-NR3R4; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

    Diazeniumdiolate cyclohexyl derivatives
    6.
    发明授权
    Diazeniumdiolate cyclohexyl derivatives 有权
    二氮烯二硫代环己基衍生物

    公开(公告)号：US09272987B2

    公开(公告)日：2016-03-01

    申请号：US14115139

    申请日：2012-04-27

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

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

    IPC分类号： C07C245/24 ,  C07C247/06 ,  C07D231/12 ,  C07D249/04 ,  C07D317/72 ,  C07C291/08

    CPC分类号： C07C247/06 ,  C07B2200/07 ,  C07C245/24 ,  C07C291/08 ,  C07C2601/14 ,  C07D231/12 ,  C07D249/04 ,  C07D317/72

    摘要： A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R6 is hydrogen, —OH, —C1-6alkyl, —OC1-6alkyl, aryl, or halogen, or together with R7, forms an oxo group, or together with R7 and the atom to which they are attached, form a 5-7-membered carbocycle ring or a 5-7-membered heterocyclic ring having 1, 2, or 3 heteroatoms, wherein alkyl and aryl are unsubstituted or independently mono-, di-, or tri-substituted with R14; R7 is hydrogen, C1-6alkyl, —CF3, aryl, —O-aryl, —O—C1-6alkyl, —C(O)OC1-6alkyl, —C(R15R16)OH, a 5-7-membered heteroaryl having 1, 2, 3 or 4 nitrogen atoms, or halogen, or together with R6, forms an oxo group, or together with R6 and the atom to which they are attached, form a 5-7-membered carbocycle ring or a 5-7-membered heterocyclic ring having 1, 2, or 3 heteroatoms wherein alkyl, aryl and heteroaryl are unsubstituted or independently mono-, di- or tri-substituted with R14; R12 is hydrogen, C1-6alkyl, or —(CH2)1-2OH, or together with R13 and the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or independently mono-, di- or tri-substituted with halogen or —C1-6alkyl; R13 is —C1-6alkyl or —(CH2)1-2OH, or together with R12 and the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or independently mono-, di- or tri-substituted with halogen or —C1-6alkyl.

    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 6是氢，-OH，-C 1-6烷基，-OC 1-6烷基，芳基或卤素，或与R 7一起形成氧代基，或与R 7和 它们连接的原子形成5-7元碳环或具有1,2或3个杂原子的5-7元杂环，其中烷基和芳基是未取代的或独立地是单 - ，二 - 或 用R14三取代; R 7是氢，C 1-6烷基，-CF 3，芳基，-O-芳基，-O-C 1-6烷基，-C（O）OC 1-6烷基，-C（R 15 R 16）OH，5- ，2,3或4个氮原子，或卤素，或与R6一起形成氧代基团，或与R6及其连接的原子一起形成5-7元碳环或5-7元碳环， 其中烷基，芳基和杂芳基是未取代的或独立地被R 14取代或被二取代或三取代的杂环基; R 12是氢，C 1-6烷基或 - （CH 2）1-2 OH，或者与R 13和它们所连接的氮原子一起形成含有一个氮原子和0或1个氧的4-至7-元杂环 原子，其中所述环是未取代的或独立地被卤素或-C 1-6烷基单，二或三取代; R 13是-C 1-6烷基或 - （CH 2）1-2 OH，或与R 12和它们所连接的氮原子一起形成含有一个氮原子和0或1个氧原子的4-至7-元杂环， 其中所述环是未取代的或独立地被卤素或-C 1-6烷基单，二或三取代。

    DIAZENIUMDIOLATE CYCLOPENTYL DERIVATIVES
    10.
    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。