Diuretics
    2.
    发明授权
    Diuretics 有权
    利尿剂

    公开(公告)号:US08377911B2

    公开(公告)日:2013-02-19

    申请号:US13500509

    申请日:2010-09-20

    IPC分类号: A61K31/655 C07D471/06

    CPC分类号: C07D491/04

    摘要: A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

    摘要翻译: 具有结构式(I)的化合物或其药学上可接受的盐,以及使用该化合物治疗高血压的方法。

    DIAZENIUMDIOLATE CYCLOPENTYL DERIVATIVES
    5.
    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

    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。

    Diazeniumdiolate cyclohexyl derivatives
    7.
    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。