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公开(公告)号：US20200262814A1
公开(公告)日：2020-08-20
申请号：US16666108
申请日：2019-10-28
申请人： Novartis AG
IPC分类号： C07D401/14 , A61K45/06 , A61P35/00 , A61K31/506 , A61P31/04 , C07D413/14 , A61K31/497
摘要： PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
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公开(公告)号：US10647701B2
公开(公告)日：2020-05-12
申请号：US16532118
申请日：2019-08-05
申请人： Novartis AG
发明人： Rohan Eric John Beckwith , Simone Bonazzi , Artiom Cernijenko , Ritesh Bhanudasji Tichkule , Michael Scott Visser
IPC分类号： C07D401/14 , A61K31/44 , C07D401/04 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D495/04 , C07D513/04 , A61P35/00
摘要： The present disclosure provides a compound of Formula (I′): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein R1, R2, Rx, X1, n, n1, and q are as defined herein, and methods of making and using same.
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公开(公告)号：US20140343093A1
公开(公告)日：2014-11-20
申请号：US14366857
申请日：2012-12-12
申请人： Novartis AG
IPC分类号： C07D401/10
CPC分类号： C07D401/10
摘要： 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：US10508101B2
公开(公告)日：2019-12-17
申请号：US16354416
申请日：2019-03-15
申请人： Novartis AG
IPC分类号： A61K31/497 , C07D401/14 , C07D413/14 , A61P31/04 , A61K31/506 , A61P35/00 , A61K45/06
摘要： PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
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5.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
申请人： Novartis AG
IPC分类号： C07D401/10 , A61K31/4725
CPC分类号： C07D401/10
摘要： 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.
摘要翻译： 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：US11505541B2
公开(公告)日：2022-11-22
申请号：US17200509
申请日：2021-03-12
申请人： Novartis AG
IPC分类号： A61K31/497 , C07D401/14 , C07D413/14 , A61P31/04 , A61K31/506 , A61P35/00 , A61K45/06
摘要： PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
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公开(公告)号：US20220323436A1
公开(公告)日：2022-10-13
申请号：US17808388
申请日：2022-06-23
申请人： NOVARTIS AG
IPC分类号： A61K31/497 , A61P35/00 , A61K9/00 , A61K45/06
摘要： The present disclosure relates to use of a protein kinase C (PKC) inhibitor in the treatment or prevention of proliferative diseases. The disclosure also relates to corresponding pharmaceutical formulations, uses, methods, combinations, and related disclosure embodiments. The disclosure further relates to use of a pharmaceutical combination comprising a PKC inhibitor and another therapeutic agent, such as an MDM2 inhibitor, in the treatment or prevention of a proliferative disease.
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8.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
申请人： Novartis AG
发明人： Michael Scott Visser , Naeem Yusuff
IPC分类号： C07D401/10 , A61K31/4725 , C07D401/14 , C07D405/14 , C07D413/14 , C07D409/14
CPC分类号： C07D401/10 , A61K31/4725 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： 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.
摘要翻译： 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
申请人： NOVARTIS AG
IPC分类号： 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分类号： 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
摘要： 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：US20240308979A1
公开(公告)日：2024-09-19
申请号：US18483436
申请日：2023-10-09
申请人： Novartis AG
IPC分类号： C07D401/14 , A61K31/497 , A61K31/506 , A61K45/06 , A61P31/04 , A61P35/00 , C07D413/14
CPC分类号： C07D401/14 , A61K31/497 , A61K31/506 , A61K45/06 , A61P31/04 , A61P35/00 , C07D413/14
摘要： PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
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