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公开(公告)号：US11180487B2
公开(公告)日：2021-11-23
申请号：US16071192
申请日：2017-01-20
发明人： Ian Stansfield , Olivier Alexis Georges Querolle , Virginie Sophie Poncelet , Gerhard Max Gross , Edgar Jacoby , Lieven Meerpoel , Janusz Jozef Kulagowski , Calum Macleod , Samuel Edward Mann , Simon Richard Green , George Hynd
IPC分类号： C07D405/14 , C07D403/10 , C07D403/14 , C07D413/14 , C07D401/14 , C07F9/535 , A61P35/00
摘要： The present invention relates to pharmaceutical agents of formula (I) useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
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公开(公告)号：US20210032267A1
公开(公告)日：2021-02-04
申请号：US16783810
申请日：2020-02-06
发明人： Ian Stansfield , Olivier Alexis Georges Querolle , Yannick Aime Eddy Ligny , Gerhard Max Gross , Edgar Jacoby , Lieven Meerpoel , Simon Richard Green , George Hynd , Janusz Jozef Kulagowski , Calum Macleod , Samuel Edward Mann
IPC分类号： C07D498/04 , C07D405/14 , C07D471/04 , C07D487/04 , C07D405/04 , C07D491/04 , C07D403/12 , A61P35/00 , C07D401/14 , C07D403/14 , C07D491/052
摘要： The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
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公开(公告)号：US11001569B2
公开(公告)日：2021-05-11
申请号：US16071298
申请日：2017-01-20
发明人： Ian Stansfield , Olivier Alexis Georges Querolle , Gerhard Max Gross , Edgar Jacoby , Lieven Meerpoel , Janusz Jozef Kulagowski , Calum Macleod , Samuel Edward Mann , Simon Richard Green , George Hynd
IPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , A61P35/00
摘要： The present invention relates to pharmaceutical agents of formula (I), useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as a cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
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公开(公告)号：US11236084B2
公开(公告)日：2022-02-01
申请号：US16622016
申请日：2018-07-04
发明人： George Hynd , Calum Macleod , Samuel Edward Mann , Janusz Jozef Kulagowski , Ian Stansfield , Olivier Alexis Georges Querolle , Virginie Sophie Poncelet , Gerhard Max Gross , Edgar Jacoby , Lieven Meerpoel
IPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
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公开(公告)号：US11186589B2
公开(公告)日：2021-11-30
申请号：US16783810
申请日：2020-02-06
发明人： Ian Stansfield , Olivier Alexis Georges Querolle , Yannick Aime Eddy Ligny , Gerhard Max Gross , Edgar Jacoby , Lieven Meerpoel , Simon Richard Green , George Hynd , Janusz Jozef Kulagowski , Calum Macleod , Samuel Edward Mann
IPC分类号： C07D498/04 , C07D405/14 , C07D471/04 , C07D487/04 , C07D405/04 , C07D491/04 , C07D403/12 , A61P35/00 , C07D401/14 , C07D403/14 , C07D491/052
摘要： The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
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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)
7.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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公开(公告)号：US11136311B2
公开(公告)日：2021-10-05
申请号：US16309059
申请日：2017-06-29
发明人： Ian Stansfield , Olivier Alexis Georges Querolle , Yannick Aime Eddy Ligny , Gerhard Max Gross , Edgar Jacoby , Lieven Meerpoel , Simon Richard Green , George Hynd , Janusz Jozef Kulagowski , Calum Macleod , Samuel Edward Mann
IPC分类号： C07D403/14 , C07D405/12 , C07D417/14
摘要： The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
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公开(公告)号：US20190119299A1
公开(公告)日：2019-04-25
申请号：US16309080
申请日：2017-06-29
发明人： Ian Stansfield , Olivier Alexis Georges Querolle , Yannick Aime Eddy Ligny , Gerhard Max Gross , Edgar Jacoby , Lieven Meerpoel , Simon Richard Green , George Hynd , Janusz Jozef Kulagowski , Calum Macleod , Samuel Edward Mann
IPC分类号： C07D498/04 , C07D491/052 , C07D471/04 , C07D405/14 , C07D403/14 , A61P35/00 , C07D401/14 , C07D487/04
摘要： Fused aromatic bicyclic substituted 5-(2-amino-4-pyrimidinyl)-cyanoindoline derivatives (I) useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-KB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
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