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    Glucose-responsive insulin conjugates
    3.
    发明授权
    Glucose-responsive insulin conjugates 有权
    葡萄糖反应性胰岛素缀合物

    公开(公告)号：US09427475B2

    公开(公告)日：2016-08-30

    申请号：US14504476

    申请日：2014-10-02

    Applicant: Merck Sharp & Dohme Corp.

    Inventor： Songnian Lin ,  Lin Yan ,  Pei Huo

    IPC: A61K38/28 ,  C07K14/62 ,  A61K47/48

    CPC classification number: A61K47/61 ,  A61K38/28 ,  A61K47/549 ,  A61K47/64 ,  C07K14/62

    Abstract: Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein the saccharide for at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.

    Abstract translation: 胰岛素缀合物包含共价连接到具有两个臂的至少一个双齿连接体的胰岛素分子，每个臂独立地连接到包含糖的配体，并且其中所述连接体的至少一个配体的糖是岩藻糖。 胰岛素缀合物显示药代动力学（PK）和/或药效学（PD）谱，其对糖类如葡萄糖或α-甲基甘露糖的全身浓度有反应，即使在不存在外源多价的情况下施用于有需要的受试者时 糖结合分子如Con A.

    DIAZENIUMDIOLATE CYCLOHEXYL DERIVATIVES
    4.
    发明申请
    DIAZENIUMDIOLATE CYCLOHEXYL DERIVATIVES 有权
    二氮杂环丁烷衍生物

    公开(公告)号：US20140088048A1

    公开(公告)日：2014-03-27

    申请号：US14115139

    申请日：2012-04-27

    Applicant: Merck Sharp & Dohme Corp.

    Inventor： Amjad Ali ,  Michael Man-Chu Lo ,  Lin Yan

    IPC: C07C247/06 ,  C07D231/12 ,  C07D249/04 ,  C07D317/72

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

    Abstract: 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.

    Abstract translation: 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。

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