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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/2025/02/18/US12227481B2/abs.jpg.150x150.jpg)
公开(公告)号：US12227481B2
公开(公告)日：2025-02-18
申请号：US18344267
申请日：2023-06-29
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：US12128039B2
公开(公告)日：2024-10-29
申请号：US18436836
申请日：2024-02-08
Applicant: Exelixis, Inc.
Inventor： Jo Ann Wilson , Khalid Shah
IPC: A61K31/47 , C07D215/233
CPC classification number: 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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3.发明公开公开(公告)号：US20240189298A1
公开(公告)日：2024-06-13
申请号：US18436836
申请日：2024-02-08
Applicant: Exelixis, Inc.
Inventor： Jo Ann Wilson , Khalid Shah
IPC: A61K31/47 , C07D215/233
CPC classification number: 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：US20220370436A1
公开(公告)日：2022-11-24
申请号：US17869427
申请日：2022-07-20
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 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/2020/12/01/US10851061B2/abs.jpg.150x150.jpg)
公开(公告)号：US10851061B2
公开(公告)日：2020-12-01
申请号：US16671834
申请日：2019-11-01
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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Patent Agency Ranking
6.发明申请公开(公告)号：US20190030021A1
公开(公告)日：2019-01-31
申请号：US16151653
申请日：2018-10-04
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, Cl, or X2 is H, Br, Cl, or n1 is 1-2; and n2 is 1-2.
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7.发明申请Processes for Preparing Quinoline Compounds and Pharmaceutical Compositions Containing Such Compounds 审中-公开制备喹啉化合物和含有这些化合物的药物组合物的方法公开(公告)号：US20170057921A1
公开(公告)日：2017-03-02
申请号：US15348716
申请日：2016-11-10
Applicant: Exelixis, Inc.
Inventor： Jo Ann Wilson , Khalid Shah
IPC: C07D215/233
CPC classification number: 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, Cl, or X2 is H, Br, Cl, or n1 is 1-2; and n2 is 1-2.
Abstract translation: 本发明涉及制备方法和含有喹啉如式I或其药学上可接受的盐的组合物，其中：X 1是H，Br，Cl或X 2是H，Br，Cl或n 1是1-2; n2为1-2。
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8.发明申请Crystalline Solid Forms of N--N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, Processes for Making, and Methods of Use 审中-公开N-N' - （4-氟苯基）环丙烷-1,1-二甲酰胺的结晶固体形式，制备方法和使用方法公开(公告)号：US20170044106A1
公开(公告)日：2017-02-16
申请号：US15118738
申请日：2015-02-16
Applicant: Exelixis, Inc.
Inventor： Dana T. Aftab , Nathan Guz , Stephen Lau , Noel Hamill , Tracy Walker , Jana Galbraith , Simon Yau , Khalid Shah
IPC: C07D215/233
CPC classification number: C07D215/233 , C07B2200/13 , 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.
Abstract translation: 本发明涉及化合物N- {4 - [（6,7-二甲氧基喹啉-4-基）氧基]苯基} -N' - （4-氟苯基）环丙烷-1,1-二甲酰胺（ 化合物1）及其溶剂化物，包括水合物，其可用于治疗癌症。 还公开了包含结晶固体形式和用于制备结晶固体形式的方法的药物组合物，以及其用于治疗癌症，特别是甲状腺癌，前列腺癌，肝细胞癌，肾癌和非小细胞的方法 肺癌。 结晶固体形式可用于制备卡泊沙坦的L-苹果酸盐。
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公开(公告)号：US20250017916A1
公开(公告)日：2025-01-16
申请号：US18899774
申请日：2024-09-27
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：US20240300897A1
公开(公告)日：2024-09-12
申请号：US18657052
申请日：2024-05-07
Applicant: Exelixis, Inc.
Inventor： Frenel DeMorin , Khalid Shah , Sagar Shakya , Peter Wong , Courtney S. Johnson , Melanie Janelle Bevill , Stephan D. Parent
IPC: C07D215/48
CPC classification number: C07D215/48 , C07B2200/13
Abstract: The present invention relates to crystalline forms of the free base of the c-Met inhibitor, Compound 1. The invention also relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid polymorphs of the free base and 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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