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1. 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。

2. 发明授权

US11142534B2 Process for the preparation of 3-substituted 5-amino-6H-thiazolo[4,5-d]pyrimidine-2,7-dione compounds 有权
公开(公告)号：US11142534B2
公开(公告)日：2021-10-12
申请号：US16476165
申请日：2018-01-04
申请人： Hoffmann-La Roche Inc.
发明人： Junli Chen , Manuel Konrath , Roland Meier , Yan Ren , Xuemei Wang , Jing Xiong , Jianhua Yu
IPC分类号： C07D513/04
摘要： The present invention relates to a process for synthesizing a compound of formula (I), R1 is H or C1-6alkyl; R2 is H or hydroxy; or pharmaceutically acceptable salt or diastereomer thereof, which is useful for prophylaxis and treatment of a viral disease in a patient relating to hepatitis B infection or a disease caused by hepatitis B infection.

3. 发明申请

US20140350257A1 Process for the Preparation of a DPP-IV Inhibitor 审中-公开
标题翻译：制备DPP-IV抑制剂的方法
公开(公告)号：US20140350257A1
公开(公告)日：2014-11-27
申请号：US14323021
申请日：2014-07-03
申请人： Hoffmann-La Roche Inc.
发明人： Ulrike Bromberger , Ralph Diodone , Stefan Hildbrand , Roland Meier
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07B2200/13
摘要： The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I wherein R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2S,3S,11bS)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl)-4(S)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form A and form B and to an amorphous form of said compound.
摘要翻译：本发明涉及制备式I的吡啶并[2,1-a]异喹啉衍生物的改进方法，其中R 1，R 2和R 3各自独立地为氢，卤素，羟基，低级烷基，低级烷氧基或低级烯基，其中低级烷基，低级烷氧基和低级烯基可任选被低级烷氧基羰基，芳基或杂环基取代，及其药学上可接受的盐。本发明还涉及（2S，3S，11bS）-1-（2-氨基-9,10-二甲氧基-1,3,4,6,7,11b-六氢-2H-吡啶并[2,1- 1-a]异喹啉-3-基）-4（S） - 氟甲基 - 吡咯烷-2-酮二盐酸盐，其形式为A和B型，并且为所述化合物的无定形形式。

4. 发明申请

US20140046066A1 PROCESS FOR THE PREPARATION OF DPP-IV INHIBITOR 审中-公开
标题翻译：制备DPP-IV抑制剂的方法
公开(公告)号：US20140046066A1
公开(公告)日：2014-02-13
申请号：US13969817
申请日：2013-09-13
申请人： Hoffmann-La Roche Inc.
发明人： Ulrike Bromberger , Ralph Diodone , Stefan Hildbrand , Roland Meier
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07B2200/13
摘要： The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I wherein R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2S,3S,11bS)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl)-4(S)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form A and form B and to an amorphous form of said compound.
摘要翻译：本发明涉及制备式I的吡啶并[2,1-a]异喹啉衍生物的改进方法，其中R 1，R 2和R 3各自独立地为氢，卤素，羟基，低级烷基，低级烷氧基或低级烯基，其中低级烷基，低级烷氧基和低级烯基可任选被低级烷氧基羰基，芳基或杂环基取代，及其药学上可接受的盐。本发明还涉及（2S，3S，11bS）-1-（2-氨基-9,10-二甲氧基-1,3,4,6,7,11b-六氢-2H-吡啶并[2,1- 1-a]异喹啉-3-基）-4（S） - 氟甲基 - 吡咯烷-2-酮二盐酸盐，其形式为A和B型，并且为所述化合物的无定形形式。

5. 发明授权

US10538536B2 Process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one compounds 有权
公开(公告)号：US10538536B2
公开(公告)日：2020-01-21
申请号：US16171936
申请日：2018-10-26
申请人： Hoffmann-La Roche Inc.
发明人： Pascal Dott , Fabian Feyen , Stefan Hildbrand , Ursula Hoffmann , Fabienne Hoffmann-Emery , Roland Meier , Gerard Moine , Pankaj Rege , Georg Wuitschik
IPC分类号： C07D519/00 , C07D401/04 , C07D487/04
摘要： The present invention relates to a process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.

6. 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。

7. 发明申请

US20150336951A1 Process For The Preparation Of A DPP-IV Inhibitor 审中-公开
标题翻译： DPP-IV抑制剂的制备方法
公开(公告)号：US20150336951A1
公开(公告)日：2015-11-26
申请号：US14702035
申请日：2015-05-01
申请人： HOFFMANN-LA ROCHE INC.
发明人： Ulrike Bromberger , Ralph Diodone , Stefan Hildbrand , Roland Meier
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07B2200/13
摘要： The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I wherein R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2S,3S,11bS)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl)-4(S)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form A and form B and to an amorphous form of said compound.
摘要翻译：本发明涉及制备式I的吡啶并[2,1-a]异喹啉衍生物的改进方法，其中R 1，R 2和R 3各自独立地为氢，卤素，羟基，低级烷基，低级烷氧基或低级烯基，其中低级烷基，低级烷氧基和低级烯基可任选地被低级烷氧基羰基，芳基或杂环基取代，及其药学上可接受的盐。本发明还涉及（2S，3S，11bS）-1-（2-氨基-9,10-二甲氧基-1,3,4,6,7,11b-六氢-2H-吡啶并[2,1- 1-a]异喹啉-3-基）-4（S） - 氟甲基 - 吡咯烷-2-酮二盐酸盐，其形式为A和B型，并且为所述化合物的无定形形式。

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