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    Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods
    1.
    发明授权
    Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods 有权
    官能化的八氢 - 异喹啉-1-酮-8-甲酰胺，八氢异喹啉-1-酮-8-羧酸酯和类似物的合成和治疗方法

    公开(公告)号：US08735391B2

    公开(公告)日：2014-05-27

    申请号：US12567573

    申请日：2009-09-25

    申请人： Jeffrey Aube ,  Bryan L. Roth ,  Partha Ghosh ,  Kevin J. Frankowski

    发明人： Jeffrey Aube ,  Bryan L. Roth ,  Partha Ghosh ,  Kevin J. Frankowski

    IPC分类号： A61K31/535 ,  A61K31/497 ,  A61K31/4965 ,  A61K31/47

    CPC分类号： C07D217/24 ,  A61K31/472 ,  C07D217/22 ,  C07D401/06 ,  C07D413/06 ,  C07D417/12

    摘要： A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.

    摘要翻译： 官能化的多环化合物可以具有式1或其盐，前药，类似物或衍生物的结构，该化合物可以通过提供二烯制备; 使二烯与亲二烯体在足够的条件下进行组合的狄尔斯 - 阿尔德/酰化反应，以提供具有羧酸的多环化合物; 并将羧酸与含胺化合物或含羟基化合物偶联以形成酰胺或酯，并制备具有式1结构的化合物。该化合物可用于调节阿片受体，其可以 通过向阿片样受体施用如本文所述的官能化多环化合物以有效量来调节阿片受体的功能性来进行。 这种阿片样物质调节可以为受试者提供生物学益处。