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公开(公告)号：EP4334311A1
公开(公告)日：2024-03-13
申请号：EP22727275.4
申请日：2022-05-03
发明人： BACHMANN, Stephan , CHYTIL, Lukas , FANTASIA, Serena Maria , FETTES, Alec , HOFFMANN, Ursula , KAPPE, Christian Oliver , LEBL, Rene , PUENTENER, Kurt , TOSATTI, Paolo , WILLIAMS, Jason Douglas
IPC分类号： C07D405/14 , C07D487/04 , C07D519/00
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公开(公告)号：EP4295845A2
公开(公告)日：2023-12-27
申请号：EP23178559.3
申请日：2019-06-17
发明人： CHUNG, Cheol Keun , Xu, Jie , IDING, Hans , CLAGG, Kyle , DALZIEL, Michael , FETTES, Alec , GOSSELIN, Francis , LIM, Ngiap-Kie , MCCLORY, Andrew , ZHANG, Haiming , CHAKRAVARTY, Paroma , NAGAPUDI, Karthik , ROBINSON, Sarah
IPC分类号： A61K31/437
摘要： Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.
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公开(公告)号：EP3810283A1
公开(公告)日：2021-04-28
申请号：EP19745335.0
申请日：2019-06-17
发明人： CHUNG, Cheol Keun , XU, Jie , IDING, Hans , CLAGG, Kyle , DALZIEL, Michael , FETTES, Alec , GOSSELIN, Francis , LIM, Ngiap-Kie , MCCLORY, Andrew , ZHANG, Haiming , CHAKRAVARTY, Paroma , NAGAPUDI, Kartik , ROBINSON, Sarah
IPC分类号： A61P35/00 , C07D471/04 , A61K31/437
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公开(公告)号：EP2234997A1
公开(公告)日：2010-10-06
申请号：EP08863591.7
申请日：2008-12-09
发明人： ABRECHT, Stefan , ADAM, Jean-Michel , FETTES, Alec
IPC分类号： C07D401/06 , C07D471/04 , C07D207/26
CPC分类号： C07D401/06 , C07D207/26 , C07D471/04
摘要： The present invention relates to a novel process for the preparation of pyrido[2,1-a] isoquinoline derivatives of the formula (I) wherein R2, R3 and R4 are each independently selected from the group consisting of hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy and lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by a group consisting of lower alkoxycarbonyl, aryl and heterocyclyl, and the pharmaceutically acceptable salts thereof. The pyrido[2,1-a] isoquinoline derivatives of the formula (I) are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.
摘要翻译： 本发明涉及制备式（I）的吡啶并[2,1-a]异喹啉衍生物的新方法，其中R2，R3和R4各自独立地选自氢，卤素，羟基，低级 烷基，低级烷氧基和低级链烯基，其中低级烷基，低级烷氧基和低级链烯基可以任选地被低级烷氧基羰基，芳基和杂环基所组成的组所取代，及其药学上可接受的盐。 式（I）的吡啶并[2,1-a]异喹啉衍生物可用于治疗和/或预防与DPP IV有关的疾病。
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公开(公告)号：EP1893595B1
公开(公告)日：2008-09-03
申请号：EP06763143.2
申请日：2006-05-15
发明人： ABRECHT, Stefan , ADAM, Jean-Michel , FETTES, Alec , FORICHER, Joseph , LOHRI, Bruno , MATTEI, Patrizio , MOINE, Gérard , SCHMID, Rudolf , ZUTTER, Ulrich
IPC分类号： C07D307/32 , C07D307/38
CPC分类号： C07D307/33 , C07D307/34 , C07D307/38 , C07D307/58 , C07D471/04
摘要： This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula (I) and with its use for the manufacture of pyrido[2,1-a] isoquinoline derivatives of the formula (II) which are useful for the treatment and / or prophylaxis of diseases which are associated with DPP IV.
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公开(公告)号：EP4178968A1
公开(公告)日：2023-05-17
申请号：EP21740049.8
申请日：2021-07-07
发明人： FETTES, Alec , GEISER, Achim , JAITZ, Leonhard
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公开(公告)号：EP3983421A1
公开(公告)日：2022-04-20
申请号：EP20732192.8
申请日：2020-06-09
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8.发明公开PROCESS FOR THE PREPARATION OF PYRIDO[2,1-A]ISOQUINOLINE DERIVATIVES COMPRISING OPTICAL RESOLUTION OF AN ENAMINE 有权用于生产吡啶并[2,1-A]异喹啉，一个烯胺的分辨率INCLUDES
公开(公告)号：EP2066667A1
公开(公告)日：2009-06-10
申请号：EP07803228.1
申请日：2007-09-05
IPC分类号： C07D471/04
CPC分类号： C07D455/06 , C07C59/31 , C07D471/04
摘要： This invention relates to a process for the preparation of pyrido[2,1-a] isoquinoline derivatives of the formula wherein R1, R2, R3 and R4 are defined in the specification, comprising the optical resolution of an enamine of the formula wherein R1 is lower alkyl, in the presence of an optical active resolving agent to form an (S)-enamine salt of the formula wherein RCO2− is the conjugate base of the resolving agent.
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公开(公告)号：EP1893595A1
公开(公告)日：2008-03-05
申请号：EP06763143.2
申请日：2006-05-15
发明人： ABRECHT, Stefan , ADAM, Jean-Michel , FETTES, Alec , FORICHER, Joseph , LOHRI, Bruno , MATTEI, Patrizio , MOINE, Gérard , SCHMID, Rudolf , ZUTTER, Ulrich
IPC分类号： C07D307/32 , C07D307/38
CPC分类号： C07D307/33 , C07D307/34 , C07D307/38 , C07D307/58 , C07D471/04
摘要： This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula (I) and with its use for the manufacture of pyrido[2,1-a] isoquinoline derivatives of the formula (II) which are useful for the treatment and / or prophylaxis of diseases which are associated with DPP IV.
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公开(公告)号：EP4295845A3
公开(公告)日：2024-02-28
申请号：EP23178559.3
申请日：2019-06-17
发明人： CHUNG, Cheol Keun , Xu, Jie , IDING, Hans , CLAGG, Kyle , DALZIEL, Michael , FETTES, Alec , GOSSELIN, Francis , LIM, Ngiap-Kie , MCCLORY, Andrew , ZHANG, Haiming , CHAKRAVARTY, Paroma , NAGAPUDI, Karthik , ROBINSON, Sarah
IPC分类号： C07D471/04
摘要： Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.
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