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1.发明授权公开(公告)号：US09126979B2
公开(公告)日：2015-09-08
申请号：US14366857
申请日：2012-12-12
Applicant: Novartis AG
Inventor： Daniel Ford , John Robert Porter , Michael Scott Visser , Naeem Yusuff
IPC: C07D401/10 , A61K31/4725
CPC classification number: C07D401/10
Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
Abstract translation: 本发明涉及式I化合物：其中R 1，R 2，R 3和R 4如发明概述中所定义。 式I的化合物能够破坏含有BH3结构域的蛋白质的BCL-2相互作用。 破坏这种相互作用可以恢复BCL-2在癌细胞和表达BCL-2的肿瘤组织中的抗凋亡功能。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌性疾病的方法。
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公开(公告)号：US10709712B2
公开(公告)日：2020-07-14
申请号：US16274165
申请日：2019-02-12
Applicant: NOVARTIS AG
Inventor： Robert John Aversa , Paul Andrew Barsanti , Matthew T. Burger , Michael Patrick Dillon , Alan Dipesa , Cheng Hu , Yan Lou , Gisele A. Nishiguchi , Yue Pan , Valery Rostislavovich Polyakov , Savithri Ramurthy , Alice C. Rico , Lina Quattrocchio Setti , Aaron Smith , Sharadha Subramanian , Benjamin R. Taft , Huw Roland Tanner , Lifeng Wan , Naeem Yusuff
IPC: A61K31/5377 , C07D413/04 , A61K31/541 , A61K45/06 , C07D213/74 , C07D237/20 , C07D239/42 , C07D239/47 , C07D239/48 , C07D277/42 , C07D401/12 , C07D403/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D493/10 , C07D403/12 , C07D401/14 , C07D405/14 , C07D213/75 , C07D233/88 , C07D401/04 , C07D405/04 , C07D405/12 , C07D241/20 , C07D471/04 , C07D487/04 , C07D263/58 , C07D491/107 , C07D493/04 , C07D495/04 , C07D498/08 , C07D513/04 , A61K31/5375 , C07D213/81 , C07D213/82 , C07D213/84 , C07D237/22 , C07D409/14 , C07D491/048 , A61K31/444 , A61K31/501 , C07B59/00 , C07D237/24 , C07D491/04 , C07D491/08
Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
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公开(公告)号：US09694016B2
公开(公告)日：2017-07-04
申请号：US14774431
申请日：2014-03-13
Applicant: Novartis AG
Inventor： Robert John Aversa , Paul Andrew Barsanti , Matthew Burger , Michael Patrick Dillon , Alan Dipesa , Cheng Hu , Yan Lou , Gisele Nishiguchi , Yue Pan , Valery Polyakov , Savithri Ramurthy , Alice Rico , Lina Setti , Aaron Smith , Sharadha Subramanian , Benjamin Taft , Huw Tanner , Lifeng Wan , Naeem Yusuff
IPC: C07D413/14 , C07D403/14 , C07D403/12 , C07D401/04 , A61K31/5377 , C07D413/04 , A61K31/541 , A61K45/06 , C07D213/74 , C07D237/20 , C07D239/42 , C07D239/47 , C07D239/48 , C07D277/42 , C07D401/12 , C07D403/04 , C07D413/12 , C07D417/12 , C07D493/10 , C07D401/14 , C07D405/14 , C07D213/75 , C07D233/88 , C07D405/04 , C07D405/12 , C07D241/20 , C07D471/04 , C07D487/04 , C07D263/58 , C07D491/107 , C07D493/04 , C07D495/04 , C07D498/08 , C07D513/04 , A61K31/5375 , C07D213/81 , C07D213/82 , C07D213/84 , C07D237/22 , C07D409/14 , C07D491/048
CPC classification number: A61K31/5377 , A61K31/444 , A61K31/501 , A61K31/5375 , A61K31/541 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/84 , C07D233/88 , C07D237/20 , C07D237/22 , C07D237/24 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D263/58 , C07D277/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D491/08 , C07D491/107 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/08 , C07D513/04
Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
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4.发明申请公开(公告)号：US20150080428A1
公开(公告)日：2015-03-19
申请号：US14366858
申请日：2012-12-12
Applicant: NOVARTIS AG
Inventor： Michael Scott Visser , Naeem Yusuff
IPC: C07D401/10 , C07D405/14 , C07D413/14 , C07D401/14 , A61K31/4725 , C07D409/14
CPC classification number: C07D401/10 , A61K31/4725 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
Abstract: The present invention relates to compounds of formula (I) in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2，R 3和R 4如发明概述中所定义。 式I的化合物能够破坏含有BH3结构域的蛋白质的BCL-2相互作用。 破坏这种相互作用可以恢复BCL-2在癌细胞和表达BCL-2的肿瘤组织中的抗凋亡功能。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌性疾病的方法。
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公开(公告)号：US20140350014A1
公开(公告)日：2014-11-27
申请号：US14366860
申请日：2012-12-12
Applicant: NOVARTIS AG
Inventor： Daniel Ford , John Robert Porter , Michael Scott Visser , Naeem Yusuff
IPC: C07D413/14 , C07D401/14 , A61K31/4725 , C07D401/10 , A61K31/5377 , A61K31/496
CPC classification number: C07D413/14 , A61K31/4725 , A61K31/496 , A61K31/5377 , C07D401/10 , C07D401/14
Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
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Patent Agency Ranking
6.发明授权公开(公告)号：US09126980B2
公开(公告)日：2015-09-08
申请号：US14366858
申请日：2012-12-12
Applicant: Novartis AG
Inventor： Michael Scott Visser , Naeem Yusuff
IPC: C07D401/10 , A61K31/4725 , C07D401/14 , C07D405/14 , C07D413/14 , C07D409/14
CPC classification number: C07D401/10 , A61K31/4725 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
Abstract: The present invention relates to compounds of formula (I) in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2，R 3和R 4如发明概述中所定义。 式I的化合物能够破坏含有BH3结构域的蛋白质的BCL-2相互作用。 破坏这种相互作用可以恢复BCL-2在癌细胞和表达BCL-2的肿瘤组织中的抗凋亡功能。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌性疾病的方法。
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公开(公告)号：US20140357633A1
公开(公告)日：2014-12-04
申请号：US14366855
申请日：2012-12-12
Applicant: NOVARTIS AG
Inventor： Daniel Ford , John Robert Porter , Michael Scott Visser , Naeem Yusuff
IPC: C07D513/04 , A61K31/4725 , C07D401/14 , C07D471/04 , C07D413/14 , A61K31/4745 , A61K31/513 , C07D405/14 , C07D487/04 , A61K31/519 , C07D409/14 , C07D417/14 , A61K31/501 , A61K31/5377 , C07D401/10
CPC classification number: C07D513/04 , A61K31/4725 , A61K31/4745 , A61K31/501 , A61K31/513 , A61K31/519 , A61K31/5377 , C07D401/10 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/02
Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
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公开(公告)号：US10245267B2
公开(公告)日：2019-04-02
申请号：US15601423
申请日：2017-05-22
Applicant: NOVARTIS AG
Inventor： Robert John Aversa , Paul Andrew Barsanti , Matthew T. Burger , Michael Patrick Dillon , Alan Dipesa , Cheng Hu , Yan Lou , Gisele A. Nishiguchi , Yue Pan , Valery Rostislavovich Polyakov , Savithri Ramurthy , Alice C. Rico , Lina Quattrocchio Setti , Aaron Smith , Sharadha Subramanian , Benjamin R. Taft , Huw Roland Tanner , Lifeng Wan , Naeem Yusuff
IPC: C07D295/04 , A61K31/5377 , C07D413/04 , A61K31/541 , A61K45/06 , C07D213/74 , C07D237/20 , C07D239/42 , C07D239/47 , C07D239/48 , C07D277/42 , C07D401/12 , C07D403/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D493/10 , C07D403/12 , C07D401/14 , C07D405/14 , C07D213/75 , C07D233/88 , C07D401/04 , C07D405/04 , C07D405/12 , C07D241/20 , C07D471/04 , C07D487/04 , C07D263/58 , C07D491/107 , C07D493/04 , C07D495/04 , C07D498/08 , C07D513/04 , A61K31/5375 , C07D213/81 , C07D213/82 , C07D213/84 , C07D237/22 , C07D409/14 , C07D491/048 , A61K31/444 , A61K31/501 , C07B59/00 , C07D237/24 , C07D491/04 , C07D491/08
Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
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公开(公告)号：US09409871B2
公开(公告)日：2016-08-09
申请号：US13905686
申请日：2013-05-30
Applicant: NOVARTIS AG
Inventor： Feng He , Stefan Peukert , Karen Marie Miller-Moslin , Naeem Yusuff , Zhuoliang Chen , Bharat Lagu
IPC: C07D401/14 , C07D403/14 , C07D403/04 , C07D413/14 , A61K31/501 , A61K31/4523 , A61K31/4427 , C07D237/20 , C07D401/12 , C07D403/12 , C07D471/04 , C07D237/26 , A61P35/00
CPC classification number: C07D237/20 , A61K31/4427 , A61K31/4523 , A61K31/501 , C07D237/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D471/04
Abstract: The present invention relates to compounds of formula I: in which L, W, X, Y, Z, m, p, R1, R2, R3, R4 and R7 are defined in the Summary of the Invention; capable of inhibiting the Hedgehog and Smo signaling pathway. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the diagnosis and treatment of pathologies relating to the Hedgehog and Smo signaling pathway, for example, tumor formation, cancer, neoplasia and non-malignant hyperproliferative disorders.
Abstract translation: 本发明涉及式I化合物：其中L，W，X，Y，Z，m，p，R 1，R 2，R 3，R 4和R 7在发明概述中定义; 能够抑制Hedgehog和Smo信号通路。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物诊断和治疗与Hedgehog和Smo信号传导途径有关的病理学的方法，例如肿瘤形成， 癌症，瘤形成和非恶性过度增生性疾病。
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公开(公告)号：US09242969B2
公开(公告)日：2016-01-26
申请号：US14204823
申请日：2014-03-11
Applicant: Novartis AG
Inventor： Paul A. Barsanti , Matthew Burger , Yan Lou , Gisele Nishiguchi , Valery Polyakov , Savithri Ramurthy , Alice Rico , Lina Setti , Aaron Smith , Benjamin Taft , Huw Tanner , Alan DiPesa , Naeem Yusuff
IPC: C07D401/04 , C07D403/04 , A61K31/5377 , A61K31/541 , C07D413/04 , A61K45/06 , C07D213/74 , C07D237/20 , C07D239/42 , C07D239/47 , C07D239/48 , C07D277/42 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D493/10 , C07D403/12 , C07D401/14 , C07D405/14 , C07D213/75 , C07D233/88 , C07D405/04 , C07D405/12 , C07D241/20 , C07D471/04 , C07D487/04 , C07D263/58 , C07D491/107 , C07D493/04 , C07D495/04 , C07D498/08 , C07D513/04
CPC classification number: A61K31/5377 , A61K31/444 , A61K31/501 , A61K31/5375 , A61K31/541 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/84 , C07D233/88 , C07D237/20 , C07D237/22 , C07D237/24 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D263/58 , C07D277/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D491/08 , C07D491/107 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/08 , C07D513/04
Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
Abstract translation: 本发明提供了本文所述的式（I）化合物及其盐，以及这些化合物治疗与Raf激酶活性相关的疾病的治疗用途。 本发明还提供包含这些化合物的药物组合物，以及包含这些化合物和治疗性助剂的组合物。
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