Opioid prodrugs with heterocyclic linkers
    3.
    发明授权
    Opioid prodrugs with heterocyclic linkers 有权
    阿片类前体药物与杂环接头

    公开(公告)号:US08685916B2

    公开(公告)日:2014-04-01

    申请号:US13415790

    申请日:2012-03-08

    IPC分类号: A61K38/00 A61K47/00

    摘要: The embodiments provide prodrug compounds of Formulae I-XV. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XV that provides controlled release of an opioid. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

    摘要翻译: 实施方案提供式I-XV的前药化合物。 本公开还提供组合物及其使用方法,其中组合物包含提供阿片样物质的受控释放的式I-XV的前药化合物。 这样的组合物可以任选地提供胰蛋白酶抑制剂,其与介导阿片样物质从前药的受控释放的酶相互作用,以减弱前体药物的酶切。

    Compositions Comprising Enzyme-Cleavable Phenol-Modified Tapentadol Prodrug
    4.
    发明申请
    Compositions Comprising Enzyme-Cleavable Phenol-Modified Tapentadol Prodrug 有权
    组合物包含酶 - 可裂解酚改性的他喷他多前药

    公开(公告)号:US20130090379A1

    公开(公告)日:2013-04-11

    申请号:US13634530

    申请日:2010-10-14

    IPC分类号: A61K31/27 C07C271/52

    摘要: A method of providing a patient with controlled release of tapentadol using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing tapentadol is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of tapentadol from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.

    摘要翻译: 公开了一种使用能够在酶活化和分子内环化作用释放他喷他多的前药的患者给予他喷他多的控制释放的方法。 本公开还提供了这样的前药化合物和包含这些化合物的药物组合物。 这样的药物组合物可以任选地包括与酶相互作用的酶抑制剂,以介导来自该前药的酶促释放的他喷他多,以便修饰前药的酶裂解。 还包括使用这些化合物和药物组合物的方法。

    Anesthetic Compounds
    8.
    发明申请
    Anesthetic Compounds 审中-公开
    麻醉化合物

    公开(公告)号:US20110124685A1

    公开(公告)日:2011-05-26

    申请号:US12812231

    申请日:2009-01-13

    申请人: Thomas E. Jenkins

    发明人: Thomas E. Jenkins

    CPC分类号: C07D295/088 C07C219/14

    摘要: The invention provides novel phenolic ester local anesthetic compounds. The invention also provides pharmaceutical compositions that include such compounds as well as methods for making such compounds and compositions and methods for using such compounds and compositions to induce and/or maintain anesthesia and/or analgesia.

    摘要翻译: 本发明提供新型酚酯局部麻醉剂化合物。 本发明还提供包含这些化合物的药物组合物以及制备这些化合物的方法,以及使用这些化合物和组合物诱导和/或维持麻醉和/或镇痛的组合物和方法。