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1. 发明授权

US09562009B2 Process to manufacture N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide 有权
标题翻译：制备N - [（3S）-1- [4 - [（3-氟苯基）甲氧基]苯基] -5-氧代 - 吡咯烷-3-基]乙酰胺
公开(公告)号：US09562009B2
公开(公告)日：2017-02-07
申请号：US15139668
申请日：2016-04-27
申请人： Hoffmann-La Roche Inc.
发明人： Olaf Grassmann , Stefan Hildbrand , Roland Meier , Michelangelo Scalone , Urs Schwitter , Beat Wirz , Ulrich Zutter
IPC分类号： C07D207/273 , C07C237/22
CPC分类号： C07D207/273 , C07B2200/13 , C07C237/22
摘要： The present invention provides processes to manufacture crystalline N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide. Also disclosed are compounds useful as intermediates in the methods of the invention.
摘要翻译：本发明提供了制备N - [（3S）-1- [4 - [（3-氟苯基）甲氧基]苯基] -5-氧代 - 吡咯烷-3-基]乙酰胺结晶的方法。还公开了可用作本发明方法中的中间体的化合物。

2. 发明授权

US08796471B2 Process for the preparation of proline derivatives 有权
标题翻译：脯氨酸衍生物的制备方法
公开(公告)号：US08796471B2
公开(公告)日：2014-08-05
申请号：US13671586
申请日：2012-11-08
申请人： Hoffmann-La Roche Inc.
发明人： Bjoern Bartels , Fritz Bliss , Philipp Cueni , Christophe Pfleger , Ulrich Zutter
IPC分类号： C07D207/09
CPC分类号： C07D207/09 , C07D207/16
摘要： The present invention relates in part to a process for the preparation of a proline derivative of formula I wherein, R1 is C1-7-alkyl or wherein R4 is selected from the group consisting of C1-7-alkyl, halogen-C1-7-alkyl and phenyl optionally substituted by halogen; R2 is halogen or halogen-C1-7-alkyl; and R3 is selected from the group consisting of hydrogen, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, halogen-C1-7-alkoxy and a 5- or 6-membered heterocyclic ring containing one or two nitrogen atoms, said ring being optionally substituted by C1-7-alkyl or halogen. The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.
摘要翻译：本发明部分涉及制备式I的脯氨酸衍生物的方法，其中R 1是C 1-7 - 烷基或其中R 4选自C 1-7 - 烷基，卤素-C 1-7 - 烷基和任选被卤素取代的苯基; R2是卤素或卤素-C1-7-烷基; 并且R 3选自氢，卤素，卤素-C 1-7 - 烷基，C 1-7 - 烷氧基，卤素-C 1-7 - 烷氧基和含有一个或两个氮原子的5-或6-元杂环所述环任选被C 1-7 - 烷基或卤素取代。式I的脯氨酸衍生物是半胱氨酸蛋白酶组织蛋白酶S的优先抑制剂，因此可用于治疗糖尿病，动脉粥样硬化，腹主动脉瘤，外周动脉疾病和糖尿病肾病等代谢疾病。

3. 发明申请

US20160237032A1 PROCESS TO MANUFACTURE N-[(3S)-1-[4-[(3-FLUOROPHENYL)METHOXY]PHENYL]-5-OXO-PYRROLIDIN-3-YL]ACETAMIDE 有权
标题翻译：制备N - [（3S）-1- [4 - [（3-氟苯基）甲氧基]苯基] -5-氧代吡咯烷-3-基]乙酰胺的方法
公开(公告)号：US20160237032A1
公开(公告)日：2016-08-18
申请号：US15139668
申请日：2016-04-27
申请人： Hoffmann-La Roche Inc.
发明人： Olaf Grassmann , Stefan Hildbrand , Roland Meier , Michelangelo Scalone , Urs Schwitter , Beat Wirz , Ulrich Zutter
IPC分类号： C07D207/273 , C07C237/22
CPC分类号： C07D207/273 , C07B2200/13 , C07C237/22
摘要： The present invention provides processes to manufacture crystalline N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide. Also disclosed are compounds useful as intermediates in the methods of the invention.
摘要翻译：本发明提供了制备N - [（3S）-1- [4 - [（3-氟苯基）甲氧基]苯基] -5-氧代 - 吡咯烷-3-基]乙酰胺结晶的方法。还公开了可用作本发明方法中的中间体的化合物。

4. 发明申请

US20130123512A1 PROCESS FOR THE PREPARATION OF PROLINE DERIVATIVES 有权
标题翻译：制备衍生物的方法
公开(公告)号：US20130123512A1
公开(公告)日：2013-05-16
申请号：US13671586
申请日：2012-11-08
申请人： Hoffmann-La Roche Inc.
发明人： Bjoern Bartels , Fritz Bliss , Philipp Cueni , Christophe Pfleger , Ulrich Zutter
IPC分类号： C07D207/09
CPC分类号： C07D207/09 , C07D207/16
摘要： The present invention relates in part to a process for the preparation of a proline derivative of formula I wherein, R1 is C1-7-alkyl or wherein R4 is selected from the group consisting of C1-7-alkyl, halogen-C1-7-alkyl and phenyl optionally substituted by halogen; R2 is halogen or halogen-C1-7-alkyl; and R3 is selected from the group consisting of hydrogen, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, halogen-C1-7-alkoxy and a 5- or 6-membered heterocyclic ring containing one or two nitrogen atoms, said ring being optionally substituted by C1-7-alkyl or halogen. The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.
摘要翻译：本发明部分涉及制备式I的脯氨酸衍生物的方法，其中R 1是C 1-7 - 烷基或其中R 4选自C 1-7 - 烷基，卤素-C 1-7 - 烷基和任选被卤素取代的苯基; R2是卤素或卤素-C1-7-烷基; 并且R 3选自氢，卤素，卤素-C 1-7 - 烷基，C 1-7 - 烷氧基，卤素-C 1-7 - 烷氧基和含有一个或两个氮原子的5-或6-元杂环所述环任选被C 1-7 - 烷基或卤素取代。式I的脯氨酸衍生物是半胱氨酸蛋白酶组织蛋白酶S的优先抑制剂，因此可用于治疗糖尿病，动脉粥样硬化，腹主动脉瘤，外周动脉疾病和糖尿病肾病等代谢疾病。

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