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![Crystalline Solid Forms of N-{4-[(6,7-Dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, Processes for Making, and Methods of Use](/abs-image/US/2021/07/08/US20210206722A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210206722A1
公开(公告)日：2021-07-08
申请号：US17212851
申请日：2021-03-25
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Nathan Guz , Stephen Lau , Noel Hamill , Tracy Walker , Jana Galbraith , Simon Yau , Khalid Shah
IPC: C07D215/233 , C07D215/22
Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.
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![Crystalline Solid Forms of N-{4-[(6,7-Dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, Processes for Making, and Methods of Use](/abs-image/US/2021/07/01/US20210198205A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210198205A1
公开(公告)日：2021-07-01
申请号：US17084312
申请日：2020-10-29
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Nathan Guz , Stephen Lau , Noel Hamill , Tracy Walker , Jana Galbraith , Simon Yau , Khalid Shah
IPC: C07D215/233 , C07D215/22
Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.
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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/2019/04/30/US10273211B2/abs.jpg.150x150.jpg)
公开(公告)号：US10273211B2
公开(公告)日：2019-04-30
申请号：US14776337
申请日：2014-03-17
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Sriram Naganathan , Wei Xu , Steven Lacy , Linh Nguyen
IPC: C07D215/22 , C07C305/24 , C07C233/60 , C07D215/60 , G01N33/487
Abstract: The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
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公开(公告)号：US20190076420A1
公开(公告)日：2019-03-14
申请号：US16190869
申请日：2018-11-14
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Sriram Naganathan , Wei Xu , Steven Lacy
Abstract: The invention relates to administration of various pharmaceutical formulations of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (cabozantinib) a c-Met inhibitor, and its metabolites, to achieve desirable pharmacokinetic and pharmacodynamic effects.
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公开(公告)号：US20150133494A1
公开(公告)日：2015-05-14
申请号：US14398188
申请日：2013-05-02
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab
IPC: A61K31/47
CPC classification number: A61K31/47
Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteolytic bone metastases, with a dual inhibitor of MET and VEGF.
Abstract translation: 本发明涉及用MET和VEGF的双重抑制剂治疗癌症，特别是去势抗性前列腺癌和溶骨性骨转移瘤。
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Patent Agency Ranking
公开(公告)号：US20140228401A1
公开(公告)日：2014-08-14
申请号：US14346570
申请日：2012-09-20
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Douglas Clary
IPC: A61K31/47
CPC classification number: A61K31/47 , A61K9/2018 , A61K9/2054 , G01N33/6887 , G01N2333/78 , G01N2333/916 , G01N2800/108 , G01N2800/52
Abstract: This invention is directed to the treatment of osteoporosis using N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.
Abstract translation: 本发明涉及使用N-（4 - {[6,7-双（甲氧基）喹啉-4-基]氧基}苯基）-N' - （4-氟苯基）环丙烷-1,1-二氧化物 二甲酰胺。
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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/2024/08/29/US20240287002A1/abs.jpg.150x150.jpg)
37.发明公开公开(公告)号：US20240287002A1
公开(公告)日：2024-08-29
申请号：US18641587
申请日：2024-04-22
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Sriram Naganathan , Wei Xu , Steven Lacy , Linh Nguyen
IPC: C07D215/22 , C07C233/60 , C07C305/24 , C07D215/60 , G01N33/487
CPC classification number: C07D215/22 , C07C233/60 , C07C305/24 , C07D215/60 , G01N33/487 , C07C2601/02 , G01N2570/00
Abstract: The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
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![CRYSTALLINE SOLID FORMS OF N-{4-[(6,7-DIMETHOXYQUINOLIN-4-YL)OXY]PHENYL}-N'-(4-FLUOROPHENYL) CYCLOPROPANE-1,1-DICARBOXAMIDE, PROCESSES FOR MAKING, AND METHODS OF USE](/abs-image/US/2023/11/30/US20230382867A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230382867A1
公开(公告)日：2023-11-30
申请号：US18363994
申请日：2023-08-02
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Nathan Guz , Stephen Lau , Noel Hamill , Tracy Walker , Jana Galbraith , Simon Yau , Khalid Shah
IPC: C07D215/233 , C07D215/22
CPC classification number: C07D215/233 , C07D215/22 , C07B2200/13
Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.
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公开(公告)号：US20220401433A1
公开(公告)日：2022-12-22
申请号：US17888356
申请日：2022-08-15
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Gisela Schwab , Colin Hessel , Christian Scheffold , Steven Lacy , Dale Miles , Alan Arroyo , Mark Dean
Abstract: The present disclosure relates to a method of treating advanced renal cell carcinoma (RCC) in human patients who have received prior anti-angiogenic therapy using CABOMETYX, a kinase inhibitor.
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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/2021/01/07/US20210002228A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210002228A1
公开(公告)日：2021-01-07
申请号：US17031196
申请日：2020-09-24
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Sriram Naganathan , Wei Xu , Steven Lacy , Linh Nguyen
IPC: C07D215/22 , C07C305/24 , C07C233/60 , C07D215/60 , G01N33/487
Abstract: The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
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