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公开(公告)号：US10017509B2
公开(公告)日：2018-07-10
申请号：US15300956
申请日：2015-04-02
发明人： Gaston Stanislas Marcella Diels , Bruno Schoentjes , Matthias Luc Aime Versele , Didier Jean-Claude Berthelot , Marc Willems , Marcel Viellevoye , Werner Constant Johan Embrechts , Berthold Wroblowski , Lieven Meerpoel
IPC分类号： C07D471/22 , C07D498/22
CPC分类号： C07D471/22 , C07D498/22 , Y02P20/582
摘要： The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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公开(公告)号：US20170022201A1
公开(公告)日：2017-01-26
申请号：US15300907
申请日：2015-04-02
发明人： Gaston Stanislas Marcella Diels , Bruno Schoentjes , Matthias Luc Aime Versele , Didier Jean-Claude Berthelot , Mar Willems , Marcel Viellevoye , Francois Maria Sommen , Berthold Wroblowski , Lieven Meerpoel
IPC分类号： C07D471/22 , C07D491/22 , C07D498/22 , C07D513/22
CPC分类号： C07D471/22 , C07D491/22 , C07D498/22 , C07D513/22 , Y02P20/582
摘要： The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
摘要翻译： 其中变量具有权利要求中限定的含义。 根据本发明的化合物具有EF2K抑制活性和任选的Vps34抑制活性。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。
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公开(公告)号：US09040725B2
公开(公告)日：2015-05-26
申请号：US14202136
申请日：2014-03-10
发明人： Bruno Schoentjes , Alain Philippe Poncelet , Julien Georges Pierre-Olivier Doyon , Joannes Theodorus Maria Linders , Lieven Meerpoel , Luc August Laurentius Ver Donck
IPC分类号： C07D313/00 , C07C211/00 , C07C215/42 , C07C35/52 , C07C43/192 , C07C215/64 , C07C217/08 , C07C217/74 , C07D295/092 , C07D313/08 , C07D405/04 , C07D407/04 , C07D207/06 , C07D213/53 , C07D213/65 , C07D215/14 , C07D239/26 , C07D295/096 , C07D295/16 , C07D317/58
CPC分类号： C07C215/42 , C07C35/52 , C07C43/192 , C07C215/64 , C07C217/08 , C07C217/74 , C07C2602/12 , C07D207/06 , C07D213/53 , C07D213/65 , C07D215/14 , C07D239/26 , C07D295/092 , C07D295/096 , C07D295/16 , C07D313/08 , C07D317/58 , C07D405/04 , C07D407/04
摘要： The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.
摘要翻译： 本发明涉及包括其任何立体化学异构体形式的式（I）化合物，其中取代基如说明书和权利要求中所定义; 其N-氧化物，其药学上可接受的盐或其溶剂合物; 条件是该化合物不是其或其药学上可接受的盐。 要求保护的化合物可用于治疗通过激活GHS1A-r受体而影响，介导或促进的疾病的治疗。 本发明还涉及其药物组合物及其制备方法。
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公开(公告)号：US11583524B2
公开(公告)日：2023-02-21
申请号：US16718955
申请日：2019-12-18
IPC分类号： A61K31/438 , A61K31/55 , A61K9/28 , A61K45/06 , C07D401/12 , C07D487/04 , A61K31/4439 , A61K31/4709 , A61K31/5377
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, R20, X, Y, Q and Z have defined meanings.
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公开(公告)号：US20180263966A1
公开(公告)日：2018-09-20
申请号：US15982043
申请日：2018-05-17
IPC分类号： A61K31/4439 , C07D487/04 , A61K45/06 , A61K31/55 , A61K9/28 , C07D401/12 , A61K31/4709 , A61K31/5377 , A61K31/438
CPC分类号： A61K31/4439 , A61K9/28 , A61K31/438 , A61K31/4709 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D401/12 , C07D487/04
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, R20, X, Y, Q and Z have defined meanings.
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公开(公告)号：US20140187557A1
公开(公告)日：2014-07-03
申请号：US14202136
申请日：2014-03-10
发明人： Bruno Schoentjes , Alain Philippe Poncelet , Julien Georges Pierre-Olivier Doyon , Joannes Theodorus Maria Linders , Lieven Meerpoel , Luc August Laurentius Ver Donck
IPC分类号： C07C215/42 , C07D313/08 , C07D405/04 , C07D213/53 , C07C217/74 , C07D295/16 , C07D213/65 , C07D239/26 , C07D215/14 , C07D317/58 , C07D295/096 , C07D207/06
CPC分类号： C07C215/42 , C07C35/52 , C07C43/192 , C07C215/64 , C07C217/08 , C07C217/74 , C07C2602/12 , C07D207/06 , C07D213/53 , C07D213/65 , C07D215/14 , C07D239/26 , C07D295/092 , C07D295/096 , C07D295/16 , C07D313/08 , C07D317/58 , C07D405/04 , C07D407/04
摘要： The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof.The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.
摘要翻译： 本发明涉及包括其任何立体化学异构体形式的式（I）化合物，其中取代基如说明书和权利要求中所定义; 其N-氧化物，其药学上可接受的盐或其溶剂合物; 条件是该化合物不是其或其药学上可接受的盐。 要求保护的化合物可用于治疗通过激活GHS1A-r受体而影响，介导或促进的疾病的治疗。 本发明还涉及其药物组合物及其制备方法。
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公开(公告)号：US20170112818A1
公开(公告)日：2017-04-27
申请号：US15398291
申请日：2017-01-04
IPC分类号： A61K31/4439 , C07D401/12 , A61K31/438 , A61K9/28 , C07D487/04 , A61K31/55 , A61K31/5377 , A61K45/06 , A61K31/4709
CPC分类号： A61K31/4439 , A61K9/28 , A61K31/438 , A61K31/4709 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D401/12 , C07D487/04
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, R20, X, Y, Q and Z have defined meanings.
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