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31.发明授权公开(公告)号：US11298349B2
公开(公告)日：2022-04-12
申请号：US17170275
申请日：2021-02-08
Applicant: Exelixis, Inc.
Inventor： Jo Ann Wilson , Khalid Shah
IPC: A61K31/47 , C07D215/233
Abstract: The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.
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公开(公告)号：US20210379050A1
公开(公告)日：2021-12-09
申请号：US17409098
申请日：2021-08-23
Applicant: Exelixis, Inc.
Inventor： Jo Ann Wilson , Khalid Shah
Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.
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![CRYSTALLINE SOLID FORMS OF SALTS 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/2021/08/26/US20210261509A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210261509A1
公开(公告)日：2021-08-26
申请号：US16617352
申请日：2018-05-26
Applicant: Exelixis, Inc.
Inventor： Khalid Shah
IPC: C07D215/22
Abstract: The invention relates to novel crystalline solid forms of salts of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, 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 renal cell carcinoma (RCC) and medullary thyroid cancer (MTC).
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公开(公告)号：US10548888B2
公开(公告)日：2020-02-04
申请号：US16026708
申请日：2018-07-03
Applicant: Exelixis, Inc.
Inventor： Jo Ann Wilson , Khalid Shah
Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.
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公开(公告)号：US10039757B2
公开(公告)日：2018-08-07
申请号：US15426804
申请日：2017-02-07
Applicant: Exelixis, Inc.
Inventor： Jo Ann Wilson , Khalid Shah
Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
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Patent Agency Ranking
公开(公告)号：US10034873B2
公开(公告)日：2018-07-31
申请号：US15612703
申请日：2017-06-02
Applicant: Exelixis, Inc.
Inventor： Jo Ann Wilson , Khalid Shah
CPC classification number: A61K31/47 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/2095 , A61K9/28 , A61K9/2833 , A61K9/2866 , A61K9/2893 , A61K45/06
Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
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公开(公告)号：US20240156804A1
公开(公告)日：2024-05-16
申请号：US18491407
申请日：2023-10-20
Applicant: Exelixis, Inc.
Inventor： Jo Ann Wilson , Khalid Shah
CPC classification number: A61K31/47 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/2095 , A61K9/28 , A61K9/2833 , A61K9/2893 , A61K45/06 , A61K9/2866
Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.
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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/2023/09/19/US11760726B2/abs.jpg.150x150.jpg)
公开(公告)号：US11760726B2
公开(公告)日：2023-09-19
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
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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![Crystalline solid forms of salts 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/2023/08/22/US11731941B2/abs.jpg.150x150.jpg)
公开(公告)号：US11731941B2
公开(公告)日：2023-08-22
申请号：US17668098
申请日：2022-02-09
Applicant: Exelixis, Inc.
Inventor： Khalid Shah
IPC: C07D215/22
CPC classification number: C07D215/22 , C07B2200/13
Abstract: The invention relates to novel crystalline solid forms of salts of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, 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 renal cell carcinoma (RCC) and medullary thyroid cancer (MTC).
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公开(公告)号：US20230052703A1
公开(公告)日：2023-02-16
申请号：US17616124
申请日：2019-12-12
Applicant: Exelixis, Inc.
Inventor： Frenel DeMorin , Khalid Shah , Sagar Shakya , Peter Wong , Courtney S. Johnson , Melanie Janelle Bevill , Stephan D. Parent
IPC: C07D215/48
Abstract: The present invention relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid crystalline salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.
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