Angiotensin II receptor antagonists
    42.
    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

    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。

    Diazeniumdiolate cyclohexyl derivatives
    44.
    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

    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。

    ANGIOTENSIN II RECEPTOR ANTAGONISTS
    50.
    发明申请
    ANGIOTENSIN II RECEPTOR ANTAGONISTS 有权
    ANGIOTENSIN II受体拮抗剂

    公开(公告)号:US20100298277A1

    公开(公告)日:2010-11-25

    申请号:US12864448

    申请日:2009-01-29

    CPC分类号: C07D403/14 C07D401/14

    摘要: A compound having the structure wherein R is an angiotensin receptor blocking group Y is —(CR1R20)1-7R5, or —C(O)(CR1R20)1-7R5; R1 and R20 are independently selected from the group consisting of hydrogen or C1-4 alkyl; R5 is —O—N═N(O)—NR3R4; and R3 and R4 are independently selected from the group consisting of —CH2CH2OH, —CH2CH2OCH3, —C1-4 alkyl, unsubstituted or substituted C1-6 alkenyl, unsubstituted or substituted morpholino, amino, unsubstituted or substituted benzyl, unsubstituted or substituted phenyl, unsubstituted or substituted arylC1-4 alkyl, or R3 and R4 together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, which is useful for treating hypertension.

    摘要翻译: 具有结构的化合物,其中R是血管紧张素受体阻断基团Y是 - (CR1R20)1-7R5或-C(O)(CR1R20)1-7R5; R 1和R 20独立地选自氢或C 1-4烷基; R5是-O-N = N(O)-NR3R4; 并且R 3和R 4独立地选自-CH 2 CH 2 OH,-CH 2 CH 2 OCH 3,-C 1-4烷基,未取代或取代的C 1-6烯基,未取代或取代的吗啉代,氨基,未取代或取代的苄基,未取代或取代的苯基,未取代的 或取代的芳基C 1-4烷基,或R 3和R 4与它们所连接的氮原子一起形成选自下列的环或其立体异构体或其药学上可接受的盐,或其药学上可接受的盐 其立体异构体,其可用于治疗高血压。