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公开(公告)号:US11597699B2
公开(公告)日:2023-03-07
申请号:US16853043
申请日:2020-04-20
申请人: Exelixis, Inc.
发明人: Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
IPC分类号: C07D205/04 , C07D205/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D401/04 , C07D409/12
摘要: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
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公开(公告)号:US20230045783A9
公开(公告)日:2023-02-09
申请号:US17468103
申请日:2021-09-07
申请人: Exelixis, Inc.
发明人: Dana T. Aftab , Gisela Schwab , Colin Hessel , Christian Scheffold , Steven Lacy , Dale Miles , Alan Arroyo , Mark Dean
摘要: 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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公开(公告)号:US11564915B2
公开(公告)日:2023-01-31
申请号:US14782537
申请日:2014-04-04
申请人: Exelixis, Inc.
发明人: Aaron Weitzman
IPC分类号: A61K31/47 , A61K9/20 , A61K9/00 , A61K9/28 , A61K31/194
摘要: This invention relates to a dosage form of cabozantinib and a method of employing the dosage form to treat cancer.
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公开(公告)号:US20220370436A1
公开(公告)日:2022-11-24
申请号:US17869427
申请日:2022-07-20
申请人: Exelixis, Inc.
发明人: Jo Ann Wilson , Khalid Shah
摘要: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.
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公开(公告)号:US20220315579A1
公开(公告)日:2022-10-06
申请号:US17033475
申请日:2020-09-25
申请人: Exelixis, Inc.
发明人: Lynne Bannen , Minna Bui , Faming Jiang , Jack Maung , Andrew Raub , Justin Salvant , Benjamin Spangler , Kin Tso , Yong Wang , Wei Xu
IPC分类号: C07D471/04
摘要: The present disclosure relates generally to compounds and pharmaceutical compositions suitable as modulators of protein kinases, and methods for their use in treating disorders mediated, at least in part by, protein kinases.
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公开(公告)号:US20220089541A1
公开(公告)日:2022-03-24
申请号:US17425661
申请日:2020-01-24
申请人: Exelixis, Inc.
发明人: Lynne Canne Bannen , Faming Jiang , Kin Tso , Xu Wei
IPC分类号: C07D215/22 , C07D215/48 , C07D401/12 , C07D471/04 , A61P35/00
摘要: The present invention relates to compounds that modulate cellular activities such as proliferation, differentiation, programmed cell death, migration, and chemoinvasion, by modulating protein kinase enzymatic activity, and compositions thereof, and methods of using such compounds.
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公开(公告)号:US20220056138A1
公开(公告)日:2022-02-24
申请号:US17519327
申请日:2021-11-04
申请人: Exelixis, Inc.
发明人: Gisela Schwab , Christian Scheffold , Colin Hessel
IPC分类号: C07K16/28 , A61P35/04 , A61K31/47 , A61K39/395 , A61K45/06
摘要: This invention relates to the combination of cabozantinib and atezolizumab to treat locally advanced or metastatic solid tumors, particularly advanced urothelial cancer or renal cell carcinoma.
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公开(公告)号:US11098015B2
公开(公告)日:2021-08-24
申请号:US17171752
申请日:2021-02-09
申请人: Exelixis, Inc.
IPC分类号: C07D215/22 , C07D215/233
摘要: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide.
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公开(公告)号:US20210139430A1
公开(公告)日:2021-05-13
申请号:US17149365
申请日:2021-01-14
申请人: Exelixis, Inc.
IPC分类号: C07D215/22 , C07D215/233
摘要: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclo-propane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide.
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公开(公告)号:US10851061B2
公开(公告)日:2020-12-01
申请号:US16671834
申请日:2019-11-01
申请人: Exelixis, Inc.
发明人: Dana T. Aftab , Nathan Guz , Stephen Lau , Noel Hamill , Tracy Walker , Jana Galbraith , Simon Yau , Khalid Shah
IPC分类号: C07D215/233 , C07D215/22
摘要: 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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