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1. 发明授权

EP2616464B1 IMPROVED PROCESS FOR THE PREPARATION OF A PRECURSOR OF SUFENTANIL BASE 有权
标题翻译：改进的苏芬太尼碱前体制备方法
公开(公告)号：EP2616464B1
公开(公告)日：2018-01-03
申请号：EP11761217.6
申请日：2011-09-15
申请人： Mallinckrodt LLC
发明人： ORR, Brian , HAAR, JR., Joseph , KLEMM, George H. , TOMAZI, Keith G.
IPC分类号： C07D409/06
CPC分类号： C07D409/06
摘要： The present disclosure generally related to an improved process for the preparation of various piperidine derivatives. More particularly, the present disclosure related to an improved process for preparing sufentanil base (1) and related compounds, which advantageously utilizes more cost effective and/or less hazardous reagents, including a dispersion comprising between about 50% and about 70% by weight (based on the total weight of the dispersion) of an alkali metal hydride, such as sodium hydride, as well as eliminates the need for expensive and/or time consuming purification techniques.

2. 发明授权

EP2838536B1 IMMEDIATE RELEASE PHARMACEUTICAL COMPOSITIONS WITH ABUSE DETERRENT PROPERTIES 失效
标题翻译：即刻释放具有不良反应特性的药物组合物
公开(公告)号：EP2838536B1
公开(公告)日：2017-08-09
申请号：EP13719340.5
申请日：2013-04-18
申请人： Mallinckrodt LLC
发明人： DIEZI, Thomas, A. , RAMAN, Siva, N. , PARK, Jae Han
IPC分类号： A61K31/485 , A61K9/20 , A61K45/06
CPC分类号： A61K9/205 , A61K9/0007 , A61K9/2009 , A61K9/2031 , A61K31/485 , A61K45/06 , A61K2300/00

3. 发明公开

EP3063152A4 CONVENIENT PREPARATION OF N-SUBSTITUTED MORPHINAN-6-OLS FROM MORPHINAN-6-ONES 有权转让
标题翻译： VEREINFACHTE HERSTELLUNG VON N-SUBSTITUIERTEN MORPHINAN-6-OLEN AUS MORPHINAN-6-ONEN
公开(公告)号：EP3063152A4
公开(公告)日：2017-06-28
申请号：EP14858224
申请日：2014-10-31
申请人： MALLINCKRODT LLC
发明人： WANG PETER X , JIANG TAO
IPC分类号： C07D489/08
CPC分类号： C07D489/08
摘要： Described herein are methods of preparing 6-hydroxy N-alkyl morphinan-6-ols from morphinan-6-ones, as illustrated below: wherein the variables R1, R2, R3, R10, R11, R14, and are as defined herein and wherein the reactions occur in a one-pot procedure using a boron based reducing agent.
摘要翻译：本文描述的是由吗啡烷-6-酮制备6-羟基N-烷基吗啡喃-6-醇的方法，如下所示：其中变量R 1，R 2，R 3，R 10，R 11，R 14和如本文所定义，并且其中该反应在使用硼基还原剂的一锅法中发生。

4. 发明公开

EP3154528A1 SPRAY DRIED COMPOSITIONS HAVING DIFFERENT DISSOLUTION PROFILES AND PROCESSES FOR THEIR PREPARATION 有权转让
标题翻译：针对不同的解决方案配置文件和方法喷雾干燥的组合物及其
公开(公告)号：EP3154528A1
公开(公告)日：2017-04-19
申请号：EP15807576.2
申请日：2015-05-27
申请人： Mallinckrodt LLC
发明人： DAVIS, Joseph M , CUCA, Robert C. , BEASLEY, Edward J.
IPC分类号： A61K9/20 , A61K9/48 , A61K31/165 , A61L15/48
CPC分类号： A61K9/1617 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/1682 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K31/167
摘要： The present disclosure provides compositions having different dissolution profiles. In particular, the compositions are formulated by adjusting the types and/or amounts of excipients and/or surfactants, and the compositions are prepared by spray drying processes.
摘要翻译：本公开提供了具有不同溶出曲线的组合物。特别地，组合物是通过调整类型和/或赋形剂和/或表面活性剂的量配制，并且在组合物通过喷雾干燥方法制备。

5. 发明公开

EP3071575A4 PREPARATION OF NORMORPHINANS 有权转让
标题翻译： HERSTELLUNG VON NORMORPHINANEN
公开(公告)号：EP3071575A4
公开(公告)日：2017-04-19
申请号：EP14862986
申请日：2014-11-18
申请人： MALLINCKRODT LLC
发明人： BRANDT JOHN , LIAO SUBO , HUDSON EDMUND C , JARVI ESA T , WANG PETER X , SCHAEFER MICHAEL
IPC分类号： C07D489/02
CPC分类号： C07D489/02
摘要： The present invention provides processes for preparing normorphinans from N-substituted morphinans. In particular, the invention provides methods for removing the N-substituent from the N-substituted morphinan to from a normorphinan carbamate, and then removing the carbamate functionality from the normorphinan carbamate to form the normorphinan.
摘要翻译：本发明提供了由N-取代的吗啡喃制备去甲吗啡喃的方法。特别是，本发明提供了从N-取代的吗啡喃除去N-取代基以从去甲吗啡喃氨基甲酸酯中除去N-取代基，然后从去甲吗啡喃氨基甲酸酯除去氨基甲酸酯官能团以形成去甲吗啡喃的方法。

6. 发明公开

EP3065743A4 PRODUCTION OF 6-HYDROXY MORPHINANS WITHOUT THE ISOLATION OF INTERMEDIATES 有权转让
标题翻译： HERSTELLUNG VON六羟基吗啡E E UNG UNG ON ON ON TEN TEN TEN TEN TEN TEN TEN TEN TEN
公开(公告)号：EP3065743A4
公开(公告)日：2017-04-05
申请号：EP14860961
申请日：2014-11-05
申请人： MALLINCKRODT LLC
发明人： WANG PETER X , JIANG TAO
IPC分类号： C07D489/02 , A61K31/485 , C07D489/08
CPC分类号： C07D489/08 , C07D489/02
摘要： The present invention provides a process for preparing a saturated 6,14-dihydroxy morphinan. The process comprises contacting an unsaturated 6-O-hydrocarbyl morphinan with hydrogen peroxide and an organic acid to form an unsaturated 6-keto-14-hydroxy morphinan. The unsaturated 6-keto-14-hydroxy morphinan is contacted with a first reducing agent to form an unsaturated 6,14-dihydroxy morphinan, and the unsaturated 6,14-dihydroxy morphinan is contacted with a second reducing agent to form the saturated 6,14-dihydroxy morphinan.
摘要翻译：本发明提供了制备饱和6,14-二羟基吗啡喃的方法。该方法包括使不饱和6-O-烃基吗啡喃与过氧化氢和有机酸接触以形成不饱和的6-酮基-14-羟基吗啡喃。不饱和6-酮基-14-羟基吗啡喃与第一还原剂接触以形成不饱和6,14-二羟基吗啡喃，不饱和6,14-二羟基吗啡喃与第二还原剂接触形成饱和的6,14-二羟基吗啡喃， 14-二羟基吗啡喃。

7. 发明授权

EP2457563B1 Zero-order modified release solid dosage forms 有权转让
标题翻译：零级修饰释放固体剂型
公开(公告)号：EP2457563B1
公开(公告)日：2017-03-22
申请号：EP12156190.6
申请日：2007-05-09
申请人： Mallinckrodt LLC
发明人： Rastogi, Suneel Kumar , Meadows, Justin Clark , Gupta, Vishal Kumar
IPC分类号： A61K9/24 , A61K9/36 , A61K31/4458
CPC分类号： A61K9/209 , A61K9/2886 , A61K31/4458

8. 发明授权

EP2812336B1 ONE POT PROCESS FOR PRODUCING 6-HYDROXYL NAL-OPIATE 有权转让
标题翻译： EIN-TOPF-VERFAHREN ZUR HERSTELLUNG VON 6-HYDROXYL-NAL-OPIAT
公开(公告)号：EP2812336B1
公开(公告)日：2017-02-01
申请号：EP13706352.5
申请日：2013-02-08
申请人： Mallinckrodt LLC
发明人： WANG, Peter, X. , JIANG, Tao , BERBERICH, David, W.
IPC分类号： C07D489/02 , C07D489/08 , A61K31/485
CPC分类号： C07D489/08 , C07D489/02

9. 发明公开

EP3063152A1 CONVENIENT PREPARATION OF N-SUBSTITUTED MORPHINAN-6-OLS FROM MORPHINAN-6-ONES 有权转让
标题翻译： VEREINFACHTE HERSTELLUNG VON N-SUBSTITUIERTEN MORPHINAN-6-OLEN AUS MORPHANAN-6-ONEN
公开(公告)号：EP3063152A1
公开(公告)日：2016-09-07
申请号：EP14858224.0
申请日：2014-10-31
申请人： Mallinckrodt LLC
发明人： WANG, Peter X. , JIANG, Tao
IPC分类号： C07D489/02
CPC分类号： C07D489/08
摘要： Described herein are one-pot methods for preparing N-alkyl morphinan-6-ols from morphinan-6-ones. In particular, the methods comprise contacting a morphinan-6-one with a boron-based reducing agent and either a carbonyl compound, an acylating agent, or an alkylating agent. Disclosed herein are one-pot methods wherein the NH group is treated with a carbonyl compound, such as an aldehyde or ketone, and a reducing agent, and wherein the 6-keto group is reduced to a 6-hydroxy group; one-pot methods wherein the NH group is treated with an alkylating agent and a base, thereby generating an N-alkyl group, and wherein the 6-keto group is reduced to a 6-hydroxy group by the addition of a reducing agent; and methods wherein the NH group is acylated with an acylating agent and a base, thereby generating an N-acyl group, and wherein the 6-keto group is reduced to a 6-hydroxy group by the addition of a reducing agent.
摘要翻译：本文描述的是从吗啡喃-6-酮制备6-羟基N-烷基吗啡喃-6-ols的方法，如下所示：其中变量R1，R2，R3，R10，R11，R14如本文所定义，其中反应在使用硼基还原剂的一锅法中发生。

10. 发明授权

EP2440562B1 PREPARATION OF 6-ALPHA-AMINO N-SUBSTITUTED MORPHINANS BY CATALYTIC HYDROGEN TRANSFER 有权转让
标题翻译： 6-α-氨基-N-取代吗啡喃通过催化氢转移准备
公开(公告)号：EP2440562B1
公开(公告)日：2016-08-10
申请号：EP10724967.4
申请日：2010-06-10
申请人： Mallinckrodt LLC
发明人： GROTE, Christopher, W. , CANTRELL, Gary, L. , MCCLURG, Joseph, P. , THOMASSON, Catherine, E. , MOSER, Frank, W.
IPC分类号： C07D489/00
CPC分类号： C07D489/00

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