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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：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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![N-(2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-quinazolinamine and N-(2,3-dihydro-1H-indol-5-yl)-4-quinazolinamine derivatives as perk inhibitors](/abs-image/US/2017/06/27/US09688662B2/abs.jpg.150x150.jpg)
公开(公告)号：US09688662B2
公开(公告)日：2017-06-27
申请号：US14782091
申请日：2014-03-31
发明人： Ian Stansfield , Yannick Aime Eddy Ligny , Nathalie Claudie Isabelle Amblard , Matthias Luc Aime Versele
IPC分类号： A61K31/4045 , A61K31/407 , A61K31/517 , C07D239/72 , C07D403/12 , C07D405/14 , C07D413/14 , C07D403/14 , C07D409/14 , C07D471/04 , C07D491/056
CPC分类号： C07D403/12 , A61K31/4045 , A61K31/407 , A61K31/517 , C07D239/72 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/056
摘要： The present invention relates to N-(2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-quinazolinamine and N-(2,3-dihydro-1H-indol-5-yl)-4-quinazolinamine derivatives of Formula (I) wherein R1, R2, R3, R4, R5, R6 and A have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors of PERK. The invention further relates to processes for preparing such 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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![NOVEL N-(2,3-DIHYDRO-1H-PYRROLO[2,3-b]PYRIDIN-5-YL)-4-QUINAZOLINAMINE AND N-(2,3-DIHYDRO-1H-INDOL-5-YL)-4-QUINAZOLINAMINE DERIVATIVES AS PERK INHIBITORS](/abs-image/US/2016/02/11/US20160039798A1/abs.jpg.150x150.jpg)
4.发明申请NOVEL N-(2,3-DIHYDRO-1H-PYRROLO[2,3-b]PYRIDIN-5-YL)-4-QUINAZOLINAMINE AND N-(2,3-DIHYDRO-1H-INDOL-5-YL)-4-QUINAZOLINAMINE DERIVATIVES AS PERK INHIBITORS 有权新的N-（2,3-二氢-1H-吡咯并[2,3-b]吡啶-5-YL）-4-喹唑啉胺和N-（2,3-二氢-1H-吲哚-5-基）-4 作为PERK抑制剂的间苯并咪唑衍生物公开(公告)号：US20160039798A1
公开(公告)日：2016-02-11
申请号：US14782091
申请日：2014-03-31
发明人： Ian Stansfield , Yannick Aime Eddy Ligny , Nathalie Claudie Isabelle Amblard , Matthias Luc Aime Versele
IPC分类号： C07D403/12 , C07D471/04 , C07D409/14 , C07D403/14 , C07D491/056
CPC分类号： C07D403/12 , A61K31/4045 , A61K31/407 , A61K31/517 , C07D239/72 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/056
摘要： The present invention relates to N-(2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-quinazolinamine and N-(2,3-dihydro-1H-indol-5-yl)-4-quinazolinamine derivatives of Formula (I) wherein R1, R2, R3, R4, R5, R6 and A have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors of PERK. The invention further relates to processes for preparing such 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： 本发明涉及N-（2,3-二氢-1H-吡咯并[2,3-b]吡啶-5-基）-4-喹唑啉胺和N-（2,3-二氢-1H-吲哚-5-基） （I）的4-喹唑啉胺衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6和A具有权利要求中限定的含义。 根据本发明的化合物可用作PERK的抑制剂。 本发明还涉及制备这些化合物的方法，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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