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1. 发明授权

US09102627B2 Processes for preparing 3-benzazepines 有权
标题翻译：制备3-苯并氮杂的方法
公开(公告)号：US09102627B2
公开(公告)日：2015-08-11
申请号：US13619788
申请日：2012-09-14
申请人： Beverly L. Wolgast , Charles A. Gilson, III , Shelley Aytes , Scott A. Estrada , Dipanjan Sengupta , Brian Smith , Max Rey , Ulrich Weigl , Heidedore Jlsabeth Rey-Papina
发明人： Beverly L. Wolgast , Charles A. Gilson, III , Shelley Aytes , Scott A. Estrada , Dipanjan Sengupta , Brian Smith , Max Rey , Ulrich Weigl
IPC分类号： A61K31/55 , C07D223/16 , C07D401/02 , C07D403/02 , C07C209/50 , C07C211/29 , C07C213/02 , C07C215/08 , C07C231/02 , C07C17/16 , C07C25/06 , C07C209/74 , C07C211/27
CPC分类号： C07D223/16 , C07C17/16 , C07C25/06 , C07C59/255 , C07C209/50 , C07C209/74 , C07C211/27 , C07C211/29 , C07C213/02 , C07C215/08 , C07C231/02 , C07C233/13
摘要： The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
摘要翻译：本发明提供了用于制备3-苯并氮杂及其盐的方法和中间体，其可用作5-羟色胺（5-HT）受体激动剂，用于治疗例如中枢神经系统疾病如肥胖症。

2. 发明申请

US20150038701A1 PROCESSES FOR THE PREPARATION OF 8-CHLORO-1-METHYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINE AND INTERMEDIATES RELATED THERETO 审中-公开
标题翻译：制备8-氯代-1-甲基-2,3,4,5-四氢-1H-苯并嗪的方法及其相关的中间体
公开(公告)号：US20150038701A1
公开(公告)日：2015-02-05
申请号：US14321342
申请日：2014-07-01
申请人： Ulrich Weigl , Frank Porstmann , Christoph Straessler , Lars Ulmer , Ulf Koetz
发明人： Ulrich Weigl , Frank Porstmann , Christoph Straessler , Lars Ulmer , Ulf Koetz
IPC分类号： C07D223/16
CPC分类号： C07D223/16
摘要： The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2, 3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
摘要翻译：本发明提供了可用作5-羟色胺的8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂盐，水合物及其结晶形式的方法，方法和中间体 5-HT）受体激动剂，用于治疗例如中枢神经系统疾病如肥胖症。

3. 发明授权

US08227609B2 Process for purifying noroxymorphone compounds 有权
标题翻译：净化去甲吗啉酮化合物的方法
公开(公告)号：US08227609B2
公开(公告)日：2012-07-24
申请号：US11815784
申请日：2006-02-09
申请人： Ulrich Weigl , Ulf Kötz , Ilia Freifeld
发明人： Ulrich Weigl , Ulf Kötz , Ilia Freifeld
IPC分类号： C07D221/22
CPC分类号： C07D489/08
摘要： A process for purifying plant extracts which consist essentially of noroxymorphone compounds and which comprise, as impurities, α,β-unsaturated noroxymorphone compounds, by (a) converting the plant extract or the product of a subsequent stage in the synthesis of a selected noroxymorphone compound in a reaction which converts the hydroxyl groups present in the mixture to leaving groups of the formula —OR2 in which R2 is the introduced radical of the leaving group, (b) these leaving groups are optionally detached again, then (c) the resulting mixture is subjected to a selective hydrogenation, so that a saturated bond is formed in the α,β-position of the unsaturated noroxymorphone compounds and any remaining leaving groups are each converted to a hydroxyl group and then optionally (d) the pure noroxymorphone compound is isolated; processing of the noroxymorphone purified in this way to naltrexone or naloxone or a salt of these compounds or a quaternary derivative of these compounds; pharmaceutical formulations comprising such a compound.
摘要翻译：一种纯化植物提取物的方法，该方法基本上由去甲羟吗啡酮化合物组成，并且通过（a）在选择的去甲吗啡酮合成中转化植物提取物或后续阶段的产物，作为杂质包含α，β-不饱和的去甲吗啉酮化合物在将该混合物中存在的羟基转化为离去基团，其中R 2是离去基团的引入基团的反应基团的反应中，化合物，（b）这些离去基团再次任选地分离，然后（c）使混合物进行选择性氢化，使得在不饱和去甲羟甲基苯氧基化合物的α，bgr-位上形成饱和键，并且任何剩余的离去基团各自转化为羟基，然后任选地（d）纯的去甲吗啉酮化合物孤立以这种方式纯化的诺羟吗啡酮的加工是纳曲酮或纳洛酮或这些化合物的盐或这些化合物的季衍生物; 包含这种化合物的药物制剂。

4. 发明授权

US08168782B2 Processes for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and intermediates related thereto 有权
标题翻译：制备8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并吖庚因的方法及其相关的中间体
公开(公告)号：US08168782B2
公开(公告)日：2012-05-01
申请号：US12225966
申请日：2007-04-02
申请人： Ulrich Weigl , Frank Porstmann , Christoph Straessler , Lars Ulmer , Ulf Koetz
发明人： Ulrich Weigl , Frank Porstmann , Christoph Straessler , Lars Ulmer , Ulf Koetz
IPC分类号： C07D223/16
CPC分类号： C07D223/16
摘要： The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
摘要翻译：本发明提供了可用作5-羟色胺的8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂盐，水合物及其结晶形式的方法，方法和中间体 5-HT）受体激动剂，用于治疗例如中枢神经系统疾病如肥胖症。

5. 发明申请

US20090143576A1 Processes for the Preparation of 8-Chloro-1-Methyl-2,3,4,5-Tetrahydro-1H-3-Benzazepine and Intermediates Related Thereto 有权
标题翻译：制备8-氯-1-甲基-2,3,4,5-四氢-1H-苯并氮杂及其相关中间体的方法
公开(公告)号：US20090143576A1
公开(公告)日：2009-06-04
申请号：US12225966
申请日：2007-04-02
申请人： Ulrich Weigl , Frank Porstmann , Christoph Straessler , Lars Ulmer , Ulf Koetz
发明人： Ulrich Weigl , Frank Porstmann , Christoph Straessler , Lars Ulmer , Ulf Koetz
IPC分类号： C07D223/16
CPC分类号： C07D223/16
摘要： The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
摘要翻译：本发明提供了可用作5-羟色胺的8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂盐，水合物及其结晶形式的方法，方法和中间体 5-HT）受体激动剂，用于治疗例如中枢神经系统疾病如肥胖症。

6. 发明申请

US20080275237A1 Method for Obtaining Pure Tetrahydrocannabinol 有权
标题翻译：获得纯四氢大麻酚的方法
公开(公告)号：US20080275237A1
公开(公告)日：2008-11-06
申请号：US11571864
申请日：2004-07-19
申请人： Enver Arslantas , Ulrich Weigl
发明人： Enver Arslantas , Ulrich Weigl
IPC分类号： C07D405/02 , C07D311/80
CPC分类号： C07D311/80
摘要： The invention relates to a method for obtaining pure tetrahydrocannabinol from reaction mixtures containing tetrahydrocannabinol compounds or from raw products containing tetrahydrocannabinol compounds. According to said method, the tetrahydrocannabinol compounds in the reaction mixture or in the raw product are converted into crystallisable derivatives, preferably using a suitable solvent, said derivatives are then crystallised and isolated, and the pure tetrahydrocannabinol compounds are then obtained from the crystallised derivatives. The invention also related to the use of compounds produced in this way for the production of a medicament for human therapy, and to the medicaments thus produced.
摘要翻译：本发明涉及从含有四氢大麻酚化合物的反应混合物或含有四氢大麻酚化合物的原料中得到纯四氢大麻酚的方法。根据所述方法，将反应混合物或原料中的四氢大麻酚化合物转化为可结晶的衍生物，优选使用合适的溶剂，然后将所述衍生物结晶分离，然后从结晶的衍生物中获得纯的四氢大麻酚化合物。本发明还涉及以这种方式制备的化合物用于生产用于人类治疗的药物以及如此制备的药物的用途。

7. 发明授权

US08802845B2 Processes for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and intermediates related thereto 有权
标题翻译：制备8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并吖庚因的方法及其相关的中间体
公开(公告)号：US08802845B2
公开(公告)日：2014-08-12
申请号：US13618995
申请日：2012-09-14
申请人： Ulrich Weigl , Frank Porstmann , Christoph Straessler , Lars Ulmer , Ulf Koetz
发明人： Ulrich Weigl , Frank Porstmann , Christoph Straessler , Lars Ulmer , Ulf Koetz
IPC分类号： C07D223/16
CPC分类号： C07D223/16
摘要： The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
摘要翻译：本发明提供了可用作5-羟色胺的8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂盐，水合物及其结晶形式的方法，方法和中间体 5-HT）受体激动剂，用于治疗例如中枢神经系统疾病如肥胖症。

8. 发明授权

US08367657B2 Processes for preparing 3-benzazepines 有权
公开(公告)号：US08367657B2
公开(公告)日：2013-02-05
申请号：US10560953
申请日：2004-06-16
申请人： Beverly L. Wolgast , Charles A. Gilson, III , Shelley Aytes , Scott A. Estrada , Dipanjan Sengupta , Brian Smith , Ulrich Weigl , Heidedore Jlsabeth Rey-Papina
发明人： Beverly L. Wolgast , Charles A. Gilson, III , Shelley Aytes , Scott A. Estrada , Dipanjan Sengupta , Brian Smith , Max Rey , Ulrich Weigl
IPC分类号： A61P25/00 , A61K31/55 , C07D223/00
CPC分类号： C07D223/16 , C07C17/16 , C07C25/06 , C07C59/255 , C07C209/50 , C07C209/74 , C07C211/27 , C07C211/29 , C07C213/02 , C07C215/08 , C07C231/02 , C07C233/13
摘要： The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.

9. 发明申请

US20100210675A1 SOLVENT-FREE CRYSTALLINE FORM OF NALTREXONE 审中-公开
标题翻译：无溶剂的NALTREXONE结晶形式
公开(公告)号：US20100210675A1
公开(公告)日：2010-08-19
申请号：US12597818
申请日：2007-04-27
申请人： Ulrich Weigl , Ulf Költz
发明人： Ulrich Weigl , Ulf Költz
IPC分类号： C07D489/08 , A61K31/485 , A61P25/30
CPC分类号： C07D489/08
摘要： Solvent-free crystalline polymorphic form of naltrexone, characterized in that it has the XRD data listed in Table 1, and a method for the preparation of this polymorphic form; and a method for converting this polymorphic form of naltrexone into a known polymorphic form of naltrexone.
摘要翻译：纳曲酮的无溶剂结晶多晶型，其特征在于其具有表1中列出的XRD数据及其制备方法。以及将这种多晶型形式的纳曲酮转化为已知的纳曲酮多态形式的方法。

10. 发明授权

US08946207B2 Processes for preparing 3-benzazepines 有权
公开(公告)号：US08946207B2
公开(公告)日：2015-02-03
申请号：US13619773
申请日：2012-09-14
申请人： Beverly L. Wolgast , Charles A. Gilson, III , Shelley Aytes , Scott A. Estrada , Dipanjan Sengupta , Brian Smith , Ulrich Weigl , Heidedore Jlsabeth Rey-Papina
发明人： Beverly L. Wolgast , Charles A. Gilson, III , Shelley Aytes , Scott A. Estrada , Dipanjan Sengupta , Brian Smith , Max Rey , Ulrich Weigl
IPC分类号： A61K31/55 , C07D223/16 , C07C209/50 , C07C211/29 , C07C213/02 , C07C215/08 , C07C231/02 , C07C17/16 , C07C25/06 , C07C209/74 , C07C211/27
CPC分类号： C07D223/16 , C07C17/16 , C07C25/06 , C07C59/255 , C07C209/50 , C07C209/74 , C07C211/27 , C07C211/29 , C07C213/02 , C07C215/08 , C07C231/02 , C07C233/13
摘要： The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.

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