专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2010033890A1 POLYMORPHS OF 6-BETA-NALTREXOL 审中-公开
标题翻译： 6-BETA-NALTREXOL的聚合物
公开(公告)号：WO2010033890A1
公开(公告)日：2010-03-25
申请号：PCT/US2009/057624
申请日：2009-09-21
申请人： MALLINCKRODT INC. , BAO, Jian , NICHOLS, Gary, A.
发明人： BAO, Jian , NICHOLS, Gary, A.
IPC分类号： C07D489/08 , A61K31/485 , A61P25/30
CPC分类号： C07D489/08 , C07D489/02
摘要： The present invention provides polymorphs of 6-beta-naltrexol and process for their preparation. In particular, the present invention provides crystalline forms of the free base of 6-beta-naltrexol and processes for their preparation. The present invention also provides crystalline and amorphous forms of the hydrochloride salt of 6-beta-naltrexol and processes for their preparation.
摘要翻译：本发明提供6-naltrexol的多晶型物及其制备方法。特别地，本发明提供了6-β-纳曲酮的游离碱的结晶形式及其制备方法。本发明还提供6-naltrexol的盐酸盐的结晶和无定形形式及其制备方法。

2. 发明申请

WO2009155259A1 PROCESSES FOR THE PREPARATION OF 6- BETA-HYDROXY MORPHINAN COMPOUNDS 审中-公开
标题翻译：制备6-β-羟基吗啉化合物的方法
公开(公告)号：WO2009155259A1
公开(公告)日：2009-12-23
申请号：PCT/US2009/047446
申请日：2009-06-16
申请人： MALLINCKRODT INC. , BAO, Jian , JIANG, Tao , CANTRELL, Gary, L.
发明人： BAO, Jian , JIANG, Tao , CANTRELL, Gary, L.
IPC分类号： C07D489/02
CPC分类号： C07D489/02
摘要： The. invention provides processes for the conversion of a 6-keto morphinan to a 6-hydroxy morphinan. In particular, the invention provides a stereoselective process for the conversion of a 6-keto morphinan to a 6-beta-hydroxy morphinan. The reduction is preferably done by formamide sulfinic acid and in the presence of a protein receptor (i.e. a base) which is added in two portions, second portion after one of the reaction components has precipitated in the solution.
摘要翻译：的。本发明提供了将6-酮基吗啡喃转化为6-羟基吗啡喃的方法。特别地，本发明提供了用于将6-酮基吗啡喃转化为6-β-羟基吗啡喃的立体选择性方法。还原反应优选由甲酰胺亚磺酸进行，并且在蛋白质受体（即碱）的存在下，分两部分加入，其中一个反应组分在溶液中沉淀出第二部分。

3. 发明申请

WO2009111162A1 PROCESS FOR THE PREPARATION OF 3-HYDROXYMORPHINAN DERIVATIVES 审中-公开
标题翻译：制备3-羟基吗啡衍生物的方法
公开(公告)号：WO2009111162A1
公开(公告)日：2009-09-11
申请号：PCT/US2009/034343
申请日：2009-02-18
申请人： MALLINCKRODT INC. , WANG, Peter, X. , JIANG, Tao , CANTRELL, Gary, L. , BERBERICH, David, W. , MOSER, Frank, W. , BAO, Jian
发明人： WANG, Peter, X. , JIANG, Tao , CANTRELL, Gary, L. , BERBERICH, David, W. , MOSER, Frank, W. , BAO, Jian
IPC分类号： C07D489/02 , C07F5/04
CPC分类号： C07D489/02 , C07F5/025
摘要： Processes are described for the synthesis of 3-hydroxymorphinan derivatives by hydrolysis of side products from the O-demethylation of 3-methoxymorphinan derivatives.
摘要翻译：描述了通过从3-甲氧基吗啡喃衍生物的O-脱甲基化水解副产物来合成3-羟基吗啡喃衍生物的方法。

4. 发明申请

WO2006098855A3 PROCESSES FOR PREPARING MORPHINANS AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备茉莉酮及其中间体的方法
公开(公告)号：WO2006098855A3
公开(公告)日：2007-01-25
申请号：PCT/US2006006285
申请日：2006-02-23
申请人： MALLINCKRODT INC , WANG PETER XIANQI , MOSER FRANK W , CANTRELL GARY L , BAO JIAN
发明人： WANG PETER XIANQI , MOSER FRANK W , CANTRELL GARY L , BAO JIAN
IPC分类号： C07D221/28 , C07D217/20 , C07D489/02 , C07D491/10
CPC分类号： C07D491/10 , C07D217/20 , C07D221/28 , C07D489/02
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a ß,?-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a ß,?-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting a,ß-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to ß,?-bicyclic ketone compounds, wherein the ß,?-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.
摘要翻译：本发明涉及合成吗啡喃的方法。特别地，通过形成包含β，β-双环酮化合物，环化酸和清除水的环化反应的反应混合物，通过使用Grewe环化反应使β，β-二环酮化合物环化以形成诺二氢贝那酮产物的方法得到改善添加剂。在一个实施方案中，Grewe转化发生在作为环化添加剂的酸酐存在下。此外，本发明涉及将β-双环酮化合物（例如，Grewe环化反应的副产物）转化为β，β-双环酮化合物的方法，其中β，ω-双环酮化合物可以是回收进一步进行Grewe环化并形成去氢二苯酮产物。

5. 发明申请

WO2012100174A1 TEMPERATURE CONTROLLED SOL-GEL CO-CONDENSATION 审中-公开
标题翻译：温度控制溶胶凝固
公开(公告)号：WO2012100174A1
公开(公告)日：2012-07-26
申请号：PCT/US2012/022048
申请日：2012-01-20
申请人： NOVAN, INC. , BAO, Jian , STASKO, Nathan
发明人： BAO, Jian , STASKO, Nathan
IPC分类号： C08G77/26
CPC分类号： C08G77/26 , C08G77/06
摘要： Provided according to some embodiments of the invention are methods of making co-condensed macromolecules that include forming a reaction mixture by combining at least one reactant and at least one reagent at a first temperature at which the at least one reactant is substantially unreactive in the presence of the at least one reagent; raising the temperature of the reaction mixture to a second temperature at which the at least one reactant is reactive in the presence of the at least one reagent, wherein the reaction of the at least one reactant in the presence of the at least one reagent produces co-condensed macromolecules such as co-condensed silica macromolecules.
摘要翻译：根据本发明的一些实施方案提供的是制备共缩合大分子的方法，其包括通过在至少一种反应物在存在下基本上不反应的第一温度下组合至少一种反应物和至少一种试剂来形成反应混合物的所述至少一种试剂; 将所述反应混合物的温度升高至所述至少一种反应物在所述至少一种试剂存在下具有反应性的第二温度，其中所述至少一种反应物在所述至少一种试剂存在下的反应产生共聚物稠化大分子如共缩合二氧化硅大分子。

6. 发明申请

WO2009079013A1 PROCESSES FOR THE PRODUCTION OF (+)-'NAL' MORPHINAN COMPOUNDS 审中-公开
标题翻译：（+） - 'NAL'吗啉化合物的制备方法
公开(公告)号：WO2009079013A1
公开(公告)日：2009-06-25
申请号：PCT/US2008/013897
申请日：2008-12-17
申请人： MALLINCKRODT INC. , WANG, Peter, X. , JIANG, Tao , CANTRELL, Gary, L. , BERBERICH, David, W. , TRAWICK, Bobby, N. , LIAO, Subo , GURUSAMY, Narayanasamy , MCCLURG, Joseph, P. , MOSER, Frank, W. , BRANDT, John , BAO, Jian , HARRING, Scott , JUNG, Catherine, K.
发明人： WANG, Peter, X. , JIANG, Tao , CANTRELL, Gary, L. , BERBERICH, David, W. , TRAWICK, Bobby, N. , LIAO, Subo , GURUSAMY, Narayanasamy , MCCLURG, Joseph, P. , MOSER, Frank, W. , BRANDT, John , BAO, Jian , HARRING, Scott , JUNG, Catherine, K.
IPC分类号： C07D489/08
CPC分类号： C07D489/08
摘要： The invention generally provides processes and intermediate compounds useful for the production of (+) nal morphinan compounds. In particular, the process encompasses synthetic routes for the production of (+) nal morphinan compounds or derivatives of (+) nal morphinan compounds from (+)-morphinan substrates such as (+)-hydrocodone, (+)-norhydrocodone or derivatives of either compound.
摘要翻译：本发明通常提供可用于（+）正吗啡喃化合物生产的方法和中间体化合物。特别地，该方法包括用于（+） - 吗啡喃化合物或（+） - 吗啡喃底物的衍生物（+） - 吗啡喃底物（例如（+） - 氢可酮，（+） - 去氢可酮或其衍生物这两种化合物。

7. 发明申请

WO2008073389A3 PREPARATION OF HEXAHYDROISOQUINOLINES FROM DIHYDROISOQUINOLINES 审中-公开
公开(公告)号：WO2008073389A3
公开(公告)日：2008-06-19
申请号：PCT/US2007/025262
申请日：2007-12-10
申请人： MALLINCKRODT INC. , WANG, Peter, X. , CANTRELL, Gary, L. , MAGPARANGALAN, Dan, P. , MOSER, Frank, W. , BAO, Jian , GROTE, Christopher, W.
发明人： WANG, Peter, X. , CANTRELL, Gary, L. , MAGPARANGALAN, Dan, P. , MOSER, Frank, W. , BAO, Jian , GROTE, Christopher, W.
IPC分类号： C07D217/02
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.

8. 发明申请

WO2006098855A2 PROCESSES FOR PREPARING MORPHINANS AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备茉莉酮及其中间体的方法
公开(公告)号：WO2006098855A2
公开(公告)日：2006-09-21
申请号：PCT/US2006/006285
申请日：2006-02-23
申请人： MALLINCKRODT INC. , WANG, Peter, Xianqi , MOSER, Frank, W. , CANTRELL, Gary, L. , BAO, Jian
发明人： WANG, Peter, Xianqi , MOSER, Frank, W. , CANTRELL, Gary, L. , BAO, Jian
IPC分类号： C07D221/28 , C07D489/02 , C07D217/20 , C07D491/10
CPC分类号： C07D491/10 , C07D217/20 , C07D221/28 , C07D489/02
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a ß,γ-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a ß,γ-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting a,ß-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to ß,γ-bicyclic ketone compounds, wherein the ß,γ-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.
摘要翻译：本发明涉及合成吗啡喃的方法。特别地，通过形成包含β，β-双环酮化合物，环化酸和清除水的环化反应的反应混合物，通过使用Grewe环化反应使β，β-二环酮化合物环化以形成诺二氢贝那酮产物的方法得到改善添加剂。在一个实施方案中，Grewe转化发生在作为环化添加剂的酸酐存在下。此外，本发明涉及将β-双环酮化合物（例如，Grewe环化反应的副产物）转化为β，β-双环酮化合物的方法，其中β，ω-双环酮化合物可以是回收进一步进行Grewe环化并形成去氢二苯酮产物。

9. 发明申请

WO2005087370A1 C1-SYMMETRIC BISPHOSPHINE LIGANDS AND THEIR USE IN THE ASYMMETRIC SYNTHESIS OF PREGABALIN 审中-公开
标题翻译： C1对称双磷酸配体及其在不对称合成中的用途
公开(公告)号：WO2005087370A1
公开(公告)日：2005-09-22
申请号：PCT/IB2005/000642
申请日：2005-03-09
申请人： WARNER-LAMBERT COMPANY LLC , BAO, Jian , BEYLIN, Vladimir, Genukh , GREENE, Derek, Joseph , HOGE, Garrett , KISSEL, William, Scott , MARLATT, Mark, Eugene , PFLUM, Derek, Andrew , WU, He-Ping
发明人： BAO, Jian , BEYLIN, Vladimir, Genukh , GREENE, Derek, Joseph , HOGE, Garrett , KISSEL, William, Scott , MARLATT, Mark, Eugene , PFLUM, Derek, Andrew , WU, He-Ping
IPC分类号： B01J31/24
CPC分类号： B01J31/24 , B01J31/2295 , B01J2231/645 , B01J2531/822 , C07B53/00 , C07C227/32 , C07C231/18 , C07C253/30 , C07F9/5027 , C07F9/5045 , C07F9/5329 , C07F9/5463 , Y02P20/582 , C07C233/47 , C07C233/51 , C07C255/19 , C07C229/08
摘要： Materials and methods for preparing (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid and structurally related compounds via enantioselective hydrogenation of prochiral olefins are disclosed. The methods employ novel chiral catalysts, which include C 1 -symmetric bisphosphine ligands bound to transition metals.
摘要翻译：公开了通过前手性烯烃的对映选择性氢化制备（S） - （+） - 3-（氨基甲基）-5-甲基己酸和结构相关化合物的材料和方法。该方法采用新型手性催化剂，其包括与过渡金属结合的C1对称双膦配体。

10. 发明申请

WO2009078989A1 PROCESSES FOR THE PREPARATION OF NORMORPHINAN SALTS 审中-公开
标题翻译：制备正诺烷盐的方法
公开(公告)号：WO2009078989A1
公开(公告)日：2009-06-25
申请号：PCT/US2008/013778
申请日：2008-12-17
申请人： MALLINCKRODT INC. , WANG, Peter, X. , JIANG, Tao , CANTRELL, Gary, L. , BERBERICH, David, W. , TRAWICK, Bobby, N. , BAO, Jian
发明人： WANG, Peter, X. , JIANG, Tao , CANTRELL, Gary, L. , BERBERICH, David, W. , TRAWICK, Bobby, N. , BAO, Jian
IPC分类号： C07D489/08
CPC分类号： C07D489/08
摘要： The invention provides a process for the conversion of opioid derivatives into normorphinan compounds useful for making 'nal' compound analgesics and antagonists. In particular, the process may be used for the production of pure normorphinan salts from crude opioid substrates.
摘要翻译：本发明提供了一种将阿片样物质衍生物转化为可用于制备“纳”复合镇痛药和拮抗剂的正大脑啡肽化合物的方法。特别地，该方法可用于从粗制阿片样物质底物生产纯的正大脑啡肽。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式