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    COMPOUNDS FOR TREATMENT OF PAIN
    1.
    发明申请
    COMPOUNDS FOR TREATMENT OF PAIN 审中-公开
    治疗疼痛的化合物

    公开(公告)号：WO2014172478A1

    公开(公告)日：2014-10-23

    申请号：PCT/US2014/034398

    申请日：2014-04-16

    Applicant: VOLKMANN, Robert

    Inventor： VOLKMANN, Robert ,  MARFAT, Anthony ,  CORNELIUS, Peter ,  ZAGOURAS, Panayiotis ,  NELSON, Frederick, Raymond ,  FLIRI, Anton Franz, Joseph

    IPC: A61K31/4748 ,  C07D489/02 ,  A61P25/04

    CPC classification number: C07D489/04

    Abstract: The aspects of the disclosed embodiments are directed to novel compounds, specifically, quaternary ammonium derivatives of tertiary amine containing opioid drug compounds such as hydrocodone, hydromorphone and oxycodone, formulations containing said. compounds or pharmaceutically acceptable salts thereof, which are capable of providing controlled release of the opioid drug upon administration to a patient in order to treat pain.

    Abstract translation: 所公开的实施方案的方面涉及新化合物，具体地，含叔胺的阿片类药物化合物如氢可酮，氢吗啡酮和羟考酮的季铵衍生物，含有所述的化合物。 化合物或其药学上可接受的盐，其能够在给予患者时提供阿片类药物的受控释放以治疗疼痛。

    PROCESS FOR PREPARING OXYMORPHONE, NALTREXONE, AND BUPRENORPHINE
    4.
    发明申请
    PROCESS FOR PREPARING OXYMORPHONE, NALTREXONE, AND BUPRENORPHINE 审中-公开
    制备氧化铁，纳曲酮和布非那定的方法

    公开(公告)号：WO2008048957A1

    公开(公告)日：2008-04-24

    申请号：PCT/US2007/081513

    申请日：2007-10-16

    Applicant: PENICK CORPORATION ,  HUANG, Bao-shan

    Inventor： HUANG, Bao-shan

    IPC: A01N43/42 ,  A61K31/44 ,  A61K9/22

    CPC classification number: C07D489/08 ,  A61K31/44 ,  C07D489/02 ,  C07D489/04

    Abstract: Methods are provided which include converting oripavine to other opiates, including converting oripavine to naltrexone, buprenorphine, 14-hydroxymorphinone and/or converting 14-hydroxymorphinone to oxymorphone. Purification and salt formation are optionally included.

    Abstract translation: 提供的方法包括将oripavine转化成其他鸦片剂，包括将oripavine转化为纳曲酮，丁丙诺啡，14-羟基吗啡酮和/或将14-羟基吗啡酮转化为羟吗啡酮。 任选地包括纯化和盐形成。

    METHODS OF TREATING PAIN
    5.
    发明申请
    METHODS OF TREATING PAIN 审中-公开
    治疗疼痛的方法

    公开(公告)号：WO2006066362A1

    公开(公告)日：2006-06-29

    申请号：PCT/AU2005/001976

    申请日：2005-12-23

    Applicant: THE UNIVERSITY OF QUEENSLAND ,  SMITH, Maree, Therese

    Inventor： SMITH, Maree, Therese

    IPC: C07D489/08 ,  A61K31/4468 ,  A61P25/04 ,  A61K31/135 ,  A61K31/485 ,  C07D489/04

    CPC classification number: C07D489/02 ,  A61K31/137 ,  A61K31/485 ,  A61K45/06 ,  C07D489/04 ,  C07D489/08

    Abstract: The present invention is directed to methods and compositions for inducing, promoting or otherwise facilitating pain relief. More particularly the present invention discloses the combination of a nitric oxide donor and an opioid analgesic in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, particularly moderate to severe pain. In particular, the nitric oxide donor is a slow-release nitric oxide donor or is formulated to provide a sustained release of a low dose of nitric oxide.

    Abstract translation: 本发明涉及用于诱导，促进或以其它方式促进疼痛缓解的方法和组合物。 更具体地，本发明公开了在包括人类的脊椎动物的治疗管理中一氧化氮供体和阿片样物质止痛剂的组合，用于预防或缓解疼痛，特别是中度至重度疼痛。 特别地，一氧化氮供体是缓释一氧化氮供体，或配制成提供低剂量一氧化氮的持续释放。

    TOTAL SYNTHESIS OF NORTHEBAINE, NORMORPHINE, NOROXYMORPHONE ENANTIOMERS AND DERIVATIVES VIA N-NOR INTERMEDIATES
    8.
    发明申请
    TOTAL SYNTHESIS OF NORTHEBAINE, NORMORPHINE, NOROXYMORPHONE ENANTIOMERS AND DERIVATIVES VIA N-NOR INTERMEDIATES 审中-公开
    通过N-NOR中间体对诺贝宁，正诺酮，异烟肼酮和衍生物进行总合成

    公开(公告)号：WO1991005768A1

    公开(公告)日：1991-05-02

    申请号：PCT/US1990005911

    申请日：1990-10-16

    Applicant: THE UNITED STATES OF AMERICA, represented by THE ...

    Inventor： THE UNITED STATES OF AMERICA, represented by THE ... ,  RICE, Kenner, Cralle ,  NEWMAN, Amy, Hauck

    IPC: C07D489/08

    CPC classification number: C07D489/02 ,  C07D489/04

    Abstract: Families of antagonist-agonists and opiate narcotics are produced from norhydrocodeinone. In a preferred embodiment, norhydrocodeinone is refluxed with sulfosalicyclic dimethylketal and delta-6-enol ether derivatives and is then converted entirely to the ether by the addition of dry tetrahydrofuran simultaneously with the removal of the thus produced ether. The ether is then reacted with methanesulfonic acid and N-bromoacetamide to form the hydrobromide salt of the 7-bromodimethylketal derivative. From this derivative, a variety of products can be derived, including the novel further intermediate 14 hydroxynorcodeinone. The present invention enables derivation using a starting material which, unlike the starting materials of prior art processes, is available in the natural (-) or synthetic (+) form. Thus, the method of the present invention provides the only known route for the synthesis of (+) forms of various derivatives and intermediates, such as (+)-7-bromo-dimethylketal nordihydrocodeinone.

    Abstract translation: 拮抗剂 - 激动剂和鸦片类麻醉药物的家族是从氢可待因酮生产的。 在一个优选的实施方案中，将可可醋酸氢醌与磺基脂环族二甲基缩酮和δ-6-烯醇醚衍生物一起回流，然后通过加入无水四氢呋喃将其完全转化为乙醚，同时除去由此产生的醚。 然后将醚与甲磺酸和N-溴乙酰胺反应，形成7-溴二甲基缩酮衍生物的氢溴酸盐。 从这种衍生物中可以得出各种产品，包括新型的中间体14羟基可待因酮。 本发明可以使用起始原料进行衍生，其与现有技术方法的起始原料不同，可以天然（ - ）或合成（+）形式获得。 因此，本发明的方法提供了用于合成（+）形式的各种衍生物和中间体的唯一已知途径，例如（+） - 7-溴 - 二甲基缩酮二氢可待因可酮。

    BENZOIC ACID, BENZOIC ACID DERIVATIVES AND HETEROARYL CARBOXYLIC ACID CONJUGATES OF OXYCODONE
    9.
    发明申请
    BENZOIC ACID, BENZOIC ACID DERIVATIVES AND HETEROARYL CARBOXYLIC ACID CONJUGATES OF OXYCODONE 审中-公开
    苯甲酸，苯甲酸衍生物和羟基琥珀酸的羧酸共聚物

    公开(公告)号：WO2016086113A1

    公开(公告)日：2016-06-02

    申请号：PCT/US2015/062637

    申请日：2015-11-25

    Applicant: KEMPHARM, INC.

    Inventor： MICKLE, Travis ,  GUENTHER, Sven ,  BERA, Sanjib ,  BERA, Bindu ,  KANSKI, Jaroslaw ,  MARTIN, Andrea K.

    IPC: A61K31/485 ,  A61P25/36

    CPC classification number: C07D489/04 ,  A61P25/36 ,  C07D498/08

    Abstract: The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxycodone (4,5-α-epoxy-14-hydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxycodone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxycodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

    Abstract translation: 目前描述的技术提供了包含芳基羧酸和例如与羟考酮（4,5-α-环氧基-14-羟基-17-甲基吗啡喃-6-酮）化学偶联的NSAID的组合物，以形成羟考酮的新型前体药物/组合物， 包括具有降低羟考酮滥用潜力的苯甲酸盐，水杨酸盐，丙酸盐，叶酸盐和乙酸盐。 本技术还提供了治疗患者的方法，药物盒和本技术合成缀合物的方法。

    MORPHINE SULFATE METHANOLIC SOLVATE, PROCESSES FOR MAKING SAME AND RELATED COMPOSITIONS AND METHODS FOR TREATING PAIN
    10.
    发明申请
    MORPHINE SULFATE METHANOLIC SOLVATE, PROCESSES FOR MAKING SAME AND RELATED COMPOSITIONS AND METHODS FOR TREATING PAIN 审中-公开
    硫酸吗啉甲醇溶剂，其制备方法及相关组合物及其治疗方法

    公开(公告)号：WO2014140899A3

    公开(公告)日：2015-01-29

    申请号：PCT/IB2014001138

    申请日：2014-03-14

    Applicant: JOHNSON MATTHEY PLC

    Inventor： MARMOR ROBERT S

    IPC: C07D489/04 ,  A61K31/485 ,  A61P29/00

    CPC classification number: C07D489/04 ,  C07B2200/13 ,  C07D489/02

    Abstract: Processes for reducing the amount of impurities, especially α,&bgr;-unsaturated ketones (ABUK), in materials containing morphine. Novel compounds, namely low ABUK morphine sulfate methanolic solvate, and a novel crystal form are also described. The method for making morphine sulfate methanolic solvate comprises mixing a morphine free base composition with methanol to form a solution and adding a liquid comprising sulfuric acid to the solution to form a morphine sulfate methanolic solvate precipitate. A method of making a morphine sulfate compound comprises drying the morphine sulfate methanolic solvate in the presence of water vapor, such that methanol molecules are removed and replaced with water vapor molecules. A composition for treating pain comprises the morphine sulfate compound and at least one pharmaceutically acceptable excipient. A method for treating pain comprises administering to a patient in need thereof the composition comprising the morphine sulfate compound and at least one pharmaceutically acceptable excipient.

    Abstract translation: 在含有吗啡的物质中减少杂质量，特别是α，α，β-不饱和酮（ABUK）的方法。 还描述了新型化合物，即低ABUK吗啡硫酸盐甲醇溶剂合物，以及新颖的晶体形式。 制备硫酸吗啡甲醇溶剂化物的方法包括将吗啡游离碱组合物与甲醇混合以形成溶液，并向溶液中加入包含硫酸的液体以形成硫酸吗啡甲醇溶剂合物沉淀。 制备吗啡硫酸盐化合物的方法包括在水蒸汽存在下干燥硫酸吗啡硫酸酯，从而除去甲醇分子并用水蒸汽分子代替。 用于治疗疼痛的组合物包含硫酸吗啡化合物和至少一种药学上可接受的赋形剂。 用于治疗疼痛的方法包括向有需要的患者施用包含硫酸吗啡化合物和至少一种药学上可接受的赋形剂的组合物。

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