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    Processes for the Preparation of Morphinane and Morphinone Compounds
    71.
    发明申请
    Processes for the Preparation of Morphinane and Morphinone Compounds 有权
    吗啡和吗啡酮化合物的制备方法

    公开(公告)号：US20120046465A1

    公开(公告)日：2012-02-23

    申请号：US13264182

    申请日：2010-04-22

    Applicant: Tomas Hudlicky ,  Robert Carroll ,  Hannes Leisch ,  Ales Machara ,  Lukas Werner ,  David R. Adams

    Inventor： Tomas Hudlicky ,  Robert Carroll ,  Hannes Leisch ,  Ales Machara ,  Lukas Werner ,  David R. Adams

    IPC: C07D489/12 ,  C07D489/02 ,  C07D489/04

    CPC classification number: C07D489/02 ,  C07D489/04

    Abstract: The present application describes processes for the synthesis of morphinane and morphinone compounds, useful as pharmaceutical agents. Also included are novel intermediates useful in the preparation of these compounds. The process comprises quaternization of oripavine to provide a mixture of the R- and S-isomeric (at the nitrogen) quaternary salts. The R-isomer is readily isolated and converted to various N-(R)-morphinane and N-(S)-morphinone compounds. The R-isomer, S-isomer or a mixture of R- and S-isomers may be demethylated and converted to various morphinane and morphinone compounds.

    Abstract translation: 本申请描述了可用作药剂的吗啡烷和吗啡酮化合物的合成方法。 还包括可用于制备这些化合物的新型中间体。 该方法包括二磷酸的季铵化以提供R-和S-异构体（在氮）季盐的混合物。 R-异构体容易分离并转化成各种N-（R） - 吗啡烷和N-（S） - 吗啡酮化合物。 R-异构体，S-异构体或R-和S-异构体的混合物可以去甲基化并转化成各种吗啡烷和吗啡酮化合物。

    DELIVERY OF DRUG AMINES THROUGH AN INHALATION ROUTE
    74.
    发明申请
    DELIVERY OF DRUG AMINES THROUGH AN INHALATION ROUTE 审中-公开
    通过吸入路线输送药物

    公开(公告)号：US20110245493A1

    公开(公告)日：2011-10-06

    申请号：US13078525

    申请日：2011-04-01

    Applicant: Joshua D. RABINOWITZ ,  Alejandro C. Zaffaroni

    Inventor： Joshua D. RABINOWITZ ,  Alejandro C. Zaffaroni

    IPC: C07D223/28 ,  C07D215/00 ,  C07D213/38 ,  C07D489/12 ,  C07C225/12 ,  C07D401/14 ,  C07D417/06 ,  C07D241/04 ,  C07D401/04 ,  G01N30/06

    CPC classification number: A61K9/007 ,  A61K9/0073 ,  A61M11/001 ,  A61M11/041 ,  A61M15/00 ,  Y10S514/958

    Abstract: The present invention relates to the delivery of drug amines through an inhalation route. Specifically, it relates to aerosols containing drug amines that are used in inhalation therapy. In one aspect of the present invention, a method of delivering an amine drug in an aerosol form is provided. The method comprises: a) heating a coating, which includes an amine drug salt on a substrate contained in a device to a temperature sufficient to volatilize the amine drug from the coating, h) by said heating, forming an amine drug vapor, and c) during said heating, drawing air through said device, condensing said vapor to form aerosol particles containing less than 10% degradation products of the compound.

    Abstract translation: 本发明涉及通过吸入途径递送药物胺。 具体地说，它涉及用于吸入治疗的含有药物胺的气溶胶。 在本发明的一个方面，提供了以气雾剂形式递送胺药物的方法。 该方法包括：a）将包含在装置中的基质上的胺药物盐的涂层加热到足以使胺药物从涂层挥发的温度，h）通过加热形成胺药物蒸气，和c ），通过所述装置吸入空气，冷凝所述蒸气以形成含有少于10％化合物降解产物的气溶胶颗粒。

    Processes for synthesis of opiate alkaloid derivatives
    76.
    发明申请
    Processes for synthesis of opiate alkaloid derivatives 有权
    合成阿片碱生物碱衍生物的方法

    公开(公告)号：US20100081816A1

    公开(公告)日：2010-04-01

    申请号：US12586874

    申请日：2009-09-29

    Applicant: Anthony Mannino ,  James Zdrodowski

    Inventor： Anthony Mannino ,  James Zdrodowski

    IPC: C07D489/12

    CPC classification number: C07D489/12

    Abstract: The present invention provides processes for the synthesis of opiate alkaloids. In particular, the opiate alkaloids produced by the process of the invention are typically intermediate compounds that may be utilized to produce a variety of biologically active alkaloids including buprenorphine and diprenorphine.

    Abstract translation: 本发明提供了合成阿片碱生物碱的方法。 特别地，通过本发明的方法生产的阿片碱生物碱通常是可用于生产各种生物活性生物碱（包括丁丙诺非和二肾上腺素）的中间体化合物。

    Novel ester derivatives of buprenorphine and their preparation processes, and long acting analgestic pharmaceutical compositions
    77.
    发明申请
    Novel ester derivatives of buprenorphine and their preparation processes, and long acting analgestic pharmaceutical compositions 审中-公开
    丁丙诺啡的新型酯衍生物及其制备方法，以及长效止吐药物组合物

    公开(公告)号：US20050075361A1

    公开(公告)日：2005-04-07

    申请号：US10645557

    申请日：2003-08-22

    Applicant: Jhi-Joung Wang

    Inventor： Jhi-Joung Wang

    IPC: A61K31/485 ,  C07D489/12 ,  C07D519/00

    CPC classification number: A61K31/485 ,  C07D489/12

    Abstract: Disclosed herein are novel buprenorphine monocarboxylic ester derivatives and dibuprenorphine dicarboxylic ester derivatives which exert a longer analgesic effect as compared to buprenorphine hydrochloride. Also disclosed are the processes for synthesizing the novel ester derivatives of buprenorphine, and long-acting analgesic pharmaceutical compositions containing a compound selected from buprenorphine base and the novel ester derivatives of buprenorphine.

    Abstract translation: 本文公开了与丁丙诺非盐酸盐相比施加更长镇痛作用的新型丁丙诺啡单羧酸酯衍生物和二丙诺啡二羧酸酯衍生物。 还公开了合成丁丙诺啡的新型酯衍生物的方法，以及含有选自丁丙诺啡碱和丁丙诺啡的新型酯衍生物的化合物的长效镇痛药物组合物。

    N-but-3-enyl norbuprenorphine and methods of use
    78.
    发明申请
    N-but-3-enyl norbuprenorphine and methods of use 有权
    N-丁基-3-烯基去丁非诺非诺和使用方法

    公开(公告)号：US20040087605A1

    公开(公告)日：2004-05-06

    申请号：US10469553

    申请日：2003-08-29

    Inventor： Bruce E. Reidenberg ,  Donna-Donigi Gale ,  Vinayak J. Srinivasan

    IPC: C07D489/12 ,  A61K031/485

    CPC classification number: C07D489/12

    Abstract: The present invention provides compound having the structure: and pharmaceutically acceptable salts or derivatives thereof, as well as compositions including such compounds. The invention also provides methods of (1) preventing pain, (2) treating pain, (3) inducing sedation, (4) treating opiate addiction, (5) treating opiate withdrawal (abstinence syndrome) and/or (6) treating cough in a patient in need thereof by administering a compound or composition of the invention. 1

    Abstract translation: 本发明提供具有以下结构的化合物及其药学上可接受的盐或衍生物，以及包括这些化合物的组合物。 本发明还提供了（1）预防疼痛，（2）治疗疼痛，（3）诱导镇静，（4）治疗阿片成瘾，（5）治疗阿片戒断（禁欲综合征）和/或（6）治疗咳嗽 通过施用本发明的化合物或组合物来治疗需要的患者。

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