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公开(公告)号：US11124482B2
公开(公告)日：2021-09-21
申请号：US15688310
申请日：2017-08-28
Applicant: Exelixis, Inc.
Inventor： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC: C07D215/22 , C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/517 , C07D295/15 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D239/88 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/5377 , C07D215/46 , C07D239/94 , C07D403/12 , C07D413/12 , C07D417/12 , C12Q1/48 , C07D215/36 , C07D215/38
Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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公开(公告)号：US20210253530A9
公开(公告)日：2021-08-19
申请号：US15688310
申请日：2017-08-28
Applicant: Exelixis, Inc.
Inventor： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC: C07D215/233 , A61K31/496 , C07D239/94 , A61K31/4725 , C07D239/88 , C07D405/14 , A61K31/5377 , A61K31/505 , A61K31/517 , C07D295/15 , C07D413/12 , A61K31/506 , C07D401/12 , A61K31/501 , C07D413/14 , C07D215/46 , A61K31/47 , C12Q1/48 , A61K31/4709 , C07D403/12 , C07D215/22 , C07D215/36 , C07D417/12 , C07D215/38 , C07D401/14
Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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公开(公告)号：US20140155396A1
公开(公告)日：2014-06-05
申请号：US13928977
申请日：2013-06-27
Applicant: Exelixis, Inc.
Inventor： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC: C07D215/22 , C07D401/12 , C07D239/88
CPC classification number: C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
Abstract translation: 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物。 更具体地，本发明提供抑制，调节和/或调节与细胞活性变化相关的激酶受体，特别是c-Met，KDF，c-Kit，flt-3和flt-4信号转导途径的喹唑啉和喹啉 如上所述，含有这些化合物的组合物，及其用于治疗激酶依赖性疾病和病症的方法。 本发明还提供了制备上述化合物的方法和含有这些化合物的组合物。
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公开(公告)号：US20230382917A1
公开(公告)日：2023-11-30
申请号：US18323510
申请日：2023-05-25
Applicant: Exelixis, Inc.
Inventor： Sunghoon Ma , Yong Wang , Wei Xu
IPC: C07D487/04 , C07D513/14 , C07D487/14
CPC classification number: C07D487/04 , C07D513/14 , C07D487/14
Abstract: Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.
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公开(公告)号：US11673897B2
公开(公告)日：2023-06-13
申请号：US16964274
申请日：2019-01-25
Applicant: Exelixis, Inc.
Inventor： Lynne Canne Bannen , Minna Bui , Faming Jiang , Yong Wang , Wei Xu
IPC: C07D401/12 , C07D401/14 , C07D413/14 , C07D491/147 , C07D471/04
CPC classification number: C07D491/147 , C07D401/12 , C07D401/14 , C07D413/14 , C07D471/04
Abstract: Disclosed herein are compounds of Formula I′. Compounds of Formula I′ inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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Patent Agency Ranking
公开(公告)号：US11124481B2
公开(公告)日：2021-09-21
申请号：US15500312
申请日：2015-07-31
Applicant: Exelixis, Inc.
Inventor： Wei Xu , David J. Donnelly , Patrick L. Chow , Benjamin J. Henley
IPC: C07D215/233 , C07D215/22
Abstract: The present invention relates to a method of preparing Cabozantinib (Cyclopropane-1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinolin-4-yloxy)-phenylo]amide(4-fluoro-phenyl)amide) and 18F labeled Cabozantinib.
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公开(公告)号：US20210032263A1
公开(公告)日：2021-02-04
申请号：US16964274
申请日：2019-01-25
Applicant: Exelixis, Inc.
Inventor： Lynne Canne Bannen , Minna Bui , Faming Jiang , Yong Wang , Wei Xu
IPC: C07D491/147 , C07D401/12 , C07D413/14 , C07D401/14 , C07D471/04
Abstract: Disclosed herein are compounds of Formula I′. Compounds of Formula I′ inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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![Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide](/abs-image/US/2019/07/18/US20190218182A1/abs.jpg.150x150.jpg)
18.发明申请公开(公告)号：US20190218182A1
公开(公告)日：2019-07-18
申请号：US16362863
申请日：2019-03-25
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Sriram Naganathan , Wei Xu , Steven Lacy , Linh Nguyen
IPC: C07D215/22 , G01N33/487 , C07C233/60 , C07C305/24 , C07D215/60
CPC classification number: C07D215/22 , C07C233/60 , C07C305/24 , C07C2601/02 , C07D215/60 , G01N33/487 , G01N2570/00
Abstract: The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
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公开(公告)号：US20170355678A1
公开(公告)日：2017-12-14
申请号：US15688310
申请日：2017-08-28
Applicant: Exelixis, Inc.
Inventor： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC: C07D215/233 , C07D239/94 , A61K31/4725 , C07D239/88 , C07D405/14 , A61K31/5377 , A61K31/505 , A61K31/517 , C07D295/15 , C07D413/12 , A61K31/506 , C07D401/12 , A61K31/501 , C07D413/14 , C07D215/46 , A61K31/47 , C12Q1/48 , A61K31/4709 , C07D403/12 , C07D215/22 , C07D215/36 , C07D417/12 , C07D215/38 , C07D401/14 , A61K31/496
CPC classification number: C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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公开(公告)号：US20140155378A9
公开(公告)日：2014-06-05
申请号：US13888592
申请日：2013-05-07
Applicant: Exelixis, Inc.
Inventor： Lynne Canne Bannen , Diva Sze-ming Chan , Jeff Chen , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC: C07D215/233 , C07D413/14 , C07D401/14 , C07D405/14 , C07D295/15 , C07D401/12
CPC classification number: C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
Abstract translation: 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物。 更具体地，本发明提供抑制，调节和/或调节与细胞活性变化相关的激酶受体，特别是c-Met，KDF，c-Kit，flt-3和flt-4信号转导途径的喹唑啉和喹啉 如上所述，含有这些化合物的组合物，及其用于治疗激酶依赖性疾病和病症的方法。 本发明还提供了制备上述化合物的方法和含有这些化合物的组合物。
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