- Preparation method of cabozantinib or salt thereof
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The invention relates to a preparation method of cabozantinib or a salt thereof, which comprises the following steps: taking a compound shown as a formula I and 1-((4-fluorophenyl)carbamoyl)cyclopropanecarboxylic acid as raw materials, conducting reacting
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Paragraph 0042-0044; 0049-0050
(2021/06/22)
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- POLYMORPHS OF N-(4-(6,7-DIMETHOXYQUINOLIN-4-YLOXY) PHENYL)-N'-(4-FLUOROPHENYL)CYCLOPROPANE-1, 1-DICARBOXAMIDE, (S)- MALATE, METHODS OF PRODUCTION AND PHARMACEUTICAL USES THEREOF
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A novel crystalline forms of (N-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-N'-(4-fluorophenyl) cyclopropane-1, 1-dicarboxamide, (S)-malate, pharmaceutical compositions containing said crystalline forms and the use of said crystalline forms in the treatment of progressive, unresectable locally advanced or metastatic medullary thyroid carcinoma and advanced renal cell carcinoma (RCC) in people who have received prior anti-angiogenic therapy, are disclosed. The present invention is further directed to a process for the preparation of the novel crystalline forms.
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Page/Page column 19-21
(2020/05/19)
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- Method of Treating Cancer and Bone Cancer Pain
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This invention is directed to the treatment of cancer, particularly lung cancer, breast cancer, melanoma, renal cell carcinoma, thyroid cancer that has metastasized to the bone. The invention is also directed to a method for treating bone cancer pain in a
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Paragraph 0111; 0118; 0119; 0131-0134
(2020/08/25)
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- Method of Treating Cancer
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This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.
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Paragraph 0110; 0123-0124; 0126; 0146-0150
(2020/11/30)
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- Preparation method of cabozantinib (S)-malate and intermediate thereof
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The invention relates to a preparation method of cabozantinib (S)-malate and an intermediate thereof. The method includes: taking 4-chloro-6, 7-dimethoxyquinoline (I) as the starting raw material, andconducting substitution, condensation and salt formatio
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Paragraph 0088-0091
(2019/07/04)
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- A pharmaceutical salt for the nepali kind and its preparation method
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The invention relates to novel crystal forms of L-malate and hydrobromide of an anti-cancer drug N-(4-{[6,7-bis(methoxy)quinoline-4-yl] oxo} phenyl)-N'-(4-fluorophenyl) cyclopropane-1,1-dicarboamide and a preparation method of the novel crystal forms. Pea
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Paragraph 0091-0098
(2019/02/26)
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- LIQUID DOSAGE FORMS TO TREAT CANCER
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This invention relates to a liquid pharmaceutical composition comprising cabozantinib to treat locally advanced or metastatic solid tumors, particularly advanced urothelial cancer or renal cell carcinoma in patients in need thereof.
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Paragraph 00163; 00164; 00182-00183; 00184-00185
(2019/01/06)
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- PROCESS FOR THE PREPARATION OF N-(4-(6,7-DIMETHOXYQUINOLIN-4-YLOXY) PHENYL)-N'-(4-FLUOROPHENYL)CYCLOPROPANE-1, 1-DICARBOXAMIDE, (2S)-HYDROXYBUTANEDIOATE AND ITS POLYMORPHS THEREOF
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The present invention also relates to process for the preparation of N-(4-(6,7-dimethoxy quinolin-4-yloxy)phenyl)-N' -( 4-fluorophenyl)cyclopropane-1, 1-dicarboxamide (S)-malate compound of formula-1a and its polymorphs thereof, represented by the followi
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Page/Page column 28; 29; 32; 33
(2018/06/30)
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- Cabozantinib malate compound and medicine composition therewith
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The invention provides a cabozantinib malate compound in a new crystal form and a preparation method thereof. The cabozantinib malate compound in the new crystal form has excellent stability and is free of significant changes on maximum single impurity content and maximum total impurity content at a high temperature (40 DEG C) under high humidity with light irradiation.
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Paragraph 0050
(2016/10/10)
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- DRUG COMBINATIONS TO TREAT MULTIPLE MYELOMA
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This invention relates to the combination of a C-Met inhibitor and a proteasome inhibitor to treat cancer, particularly multiple myeloma.
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Paragraph 00111; 00123
(2016/03/19)
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- Methods of Using C-Met Modulators
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Methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R1 is halo; R2 is halo; and Q is CH or
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Paragraph 0095; 0101
(2016/03/05)
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- C-met modulator pharmaceutical compositions
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Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
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Page/Page column 31; 35; 36
(2016/10/10)
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- METHOD OF TREATING LUNG ADENOCARCINOMA
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This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with SLC34A2-ROS1, CD74-ROS1, or FIG-ROSl fusion-positive non-small cell lung cancer, with an inhibitor of
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Paragraph 00263; 00275
(2015/11/16)
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- NOVEL POLYMORPHS OF CABOZANTINIB (S)-MALATE AND CABOZANTINIB FREE BASE
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The present disclosure provides novel crystalline forms of cabozantinib (S)-malate, designated as form-M1, M2, M3 and M4 and novel crystalline forms of cabozantinib free base, form-M1, M2 a
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Page/Page column 18; 19
(2015/12/08)
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- CABOZANTINIB DOSAGE FORM AND USE IN THE TREATMENT OF CANCER
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This invention relates to a dosage form of cabozantinib and a method of employing the dosage form to treat cancer.
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Paragraph 00206
(2014/10/18)
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- PROCESS FOR PREPARING QUINOLINE DERIVATIVES
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A process for preparing a compound of Formula I is disclosed, comprising the steps: wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl or (C1-C6)alkyl optionally substituted wit
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Paragraph 0070; 0071; 0072
(2013/05/09)
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- METHOD FOR TREATING OSTEOPOROSIS
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This invention is directed to the treatment of osteoporosis using Ν-(4-{ [6,7- bis(methyloxy)quinolin-4-yI]oxy}ρhenyl)-N'-(4-fluorophenyl)cycIopropane-l,l-dicarboxamide.
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Paragraph 00119; 00131
(2013/04/10)
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- A DUAL MET - VEGF MODULATOR FOR TREATING OSTEOLYTIC BONE METASTASES
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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.
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Paragraph 00125
(2013/11/19)
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- PROCESSES FOR PREPARING QUINOLINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH COMPOUNDS
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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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Page/Page column 31
(2012/08/28)
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- MALATE SALT OF N- (4- { [ 6, 7-BIS (METHYLOXY) QUIN0LIN-4-YL] OXY}PHENYL-N' - (4 -FLUOROPHENYL) CYCLOPROPANE-1-DICARBOXAMIDE, AND CRYSTALLINE FORMS THEROF FOR THE TREATMENT OF CANCER
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Disclosed are malate salts of N-(4-{ [6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)- N'-(4-fluorophenyl)cyclopropane-l,l-dicarboxamide, including a (L)-malate salt, a (D)- malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous
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Page/Page column 26 - 27
(2010/08/08)
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