cas 849217-68-1, Cabozantinib | Articles data

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Preparation method of cabozantinib or salt thereof
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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(2021/06/22)

Synthesis method of cabozantinib and intermediate thereof
The invention provides a synthesis method of cabozantinib and an intermediate thereof, and belongs to the field of medicinal chemistry. According to the invention, cyclopropane-1,1-dicarboxylic acid amine is used as a key intermediate, and reacts with sub
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Paragraph 0124-0127

(2021/02/24)

Preparation method of cabozantinib
The invention relates to a preparation method of cabozantinib. The preparation method comprises the following steps: mixing 4-(6,7-dimethoxy-quinolin-4-yloxy)-phenylamine with primary alcohol ester of1-[(4-fluorophenyl)carbamoyl]cyclopropanecarboxylic acid, and carrying out an amidation reaction under the action of a catalyst to obtain cabozantinib. The method for preparing the cabozantinib is screened out in a unique path and repeated exploration, the steps of the method are few, operation is easy and convenient, the molar yield can reach 94%, and the purity can reach 99.5%.
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Paragraph 0015-0024

(2020/06/20)

Method of Treating Cancer and Bone Cancer Pain
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; 0117; 0119; 0127-0130

(2020/08/25)

Method of Treating Cancer
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; 0121-0122; 0126; 0140-0145

(2020/11/30)

Preparation method of broad-spectrum anti-cancer drug kimatinib (by machine translation)
The preparation method is simple, the reaction conditions are mild . the reaction conditions are mild, the intermediate stability is good, the side reaction: is less likely to occur, and the preparation method is very suitable for industrial production: a
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(2020/04/02)

Preparation method of Cabozantinib
The invention relates to a preparation method of Cabozantinib, and belongs to the field of pharmaceutical chemistry. The Cabozantinib compound is prepared through two steps. The preparation method comprises following steps: 1, a compound III and a compoun
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(2019/08/12)

Preparation method of cabozantinib (S)-malate and intermediate thereof
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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(2019/07/04)

AN IMPROVED PROCESS FOR THE PREPARATION OF CABOZANTINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The present invention relates to an improved process for the preparation of N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide compound of formula-1 which is represented by the following structural formula:
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(2019/12/28)

A quinoline compounds of the new crystal and its preparation method
The invention relates to a new quinoline compound crystal form and a preparation method thereof, and belongs to the field of pharmaceutical chemistry. The new crystal form X-ray powder diffraction diagram has peaks at the position of 2 theta of about 11.9
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Paragraph 0086-0089

(2019/02/26)

A New Synthesis of Cabozantinib
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Fang, Ran,Wang, Bin,Zhao, Zhiwei,Yin, Lingfeng,Wang, Han,Xu, Jingli
p. 381 - 387
(2019/06/27)

Preparing method of cabozantinib
The invention is aimed at providing a method of more efficiently synthesizing cabozantinib. In the method, 6-nitroveratraldehyde serves as the initiator, the reduction, cyclization and hydrolysis reaction are completed through a one-pot method to obtain 6
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(2019/10/01)

Preparation method of Cabozantinib
The invention belongs to the field of pharmaceutical chemistry, and relates to a preparation method of Cabozantinib. The preparation method comprises following steps: 4-halogenated-6, 7-dimethoxyquinoline is reacted with 4-aminophenol to prepare a compoun
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(2019/08/12)

Preparation method of cabozantinib
The invention relates to a preparation method of cabozantinib, and particularly relates to the synthesis of cabozantinib through four steps of hydroxyl protection reaction, coupling reaction, reduction reaction and condensation reaction, using 5,6-dimetho
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(2019/10/01)

Design, synthesis and biological evaluation of 6-substituted quinolines derived from cabozantinib as c-Met inhibitors
Based on the cabozantinib scaffold, novel c-Met inhibitors were rationalized from the limited knowledge of structure-activity relationships for the quinoline 6-position. Emphasis was given to modifications capable of engaging in additional polar interacti
Lien, Vegard Torp,Pettersen, Solveig,Haugen, Mads Haugland,Olberg, Dag Erlend,M?landsmo, Gunhild M.,Klaveness, Jo
(2019/08/21)

Preparation method of multi-receptor tyrosine kinase inhibitor and intermediate thereof
The invention relates to a preparation method of cabozantinib. The method includes: taking 4-chloro-6, 7-dimethoxyquinoline (I) as the starting raw material, and conducting substitution and condensation to obtain cabozantinib. Compared with other preparat
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Paragraph 0041-0052

(2019/07/04)

KINASE INHIBITOR SALTS AND COMPOSITIONS THEREOF
The present invention relates to kinase inhibitor C8-C16 aliphatic sulfate salts and compositions thereof.
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Page/Page column 110

(2020/01/08)

A synthesis method of card abundantly for nepal (by machine translation)
The present invention provides a card abundantly for nepal synthesis method, the method to 1, 1 - cyclopropyl dicarboxylic acid as the starting material, after the acylation with 4 - [(6, 7 - dimethoxy - 4 - quinolyl) oxy] aniline condensation, with 4 - f
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Paragraph 0017; 0028-0029; 0033; 0035; 0037

(2018/04/01)

COMBINATIONS OF CABOZANTINIB AND ATEZOLIZUMAB TO TREAT CANCER
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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Paragraph 0081; 0082; 0094; 0095; 0096; 0097; 0098; 0099

(2018/08/12)

LIQUID DOSAGE FORMS TO TREAT CANCER
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; 00176-00177; 00178-00181

(2019/01/06)

Preparation method of cabozantinib
The invention relates to a preparation method of cabozantinib. The method comprises the following steps: taking 5,6-dimethoxy-4-hydroxyquinoline, TsCl, fluoronitrobenzene, and 1-(4-fluorophenyl)amino-carbonyl cyclopropane carboxylic acid as raw materials, and performing steps of a hydroxy protection reaction, a coupling reaction, a reduction reaction, and a condensation reaction to obtain the cabozantinib. The preparation method of cabozantinib has the advantages of high yield, low cost, less three wastes, easy operation, and safety, and is suitable for industrialization.
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(2018/07/30)

One-step synthesis of [18F]cabozantinib for use in positron emission tomography imaging of c-Met
Cabozantinib is an FDA-approved kinase inhibitor for the treatment of medullary thyroid cancer and advanced renal cell carcinoma, which exerts its therapeutic effect by inhibiting, among others, the tyrosine kinase c-Met. Noninvasive imaging techniques are becoming increasingly important clinically to ensure drug efficacy, staging, monitoring, and patient stratification. PET isotope labelled tyrosine kinase inhibitors have, for the same reason, potential as PET tracers for imaging of various cancers. On the basis of cabozantinib, we synthesized the novel boronic acid pinacol ester 4 as a labelling precursor, where the boronic ester moiety replaces the fluorine native to this kinase inhibitor. By this, we wanted to explore whether recently developed Cu-mediated fluorination methods are adaptable to more complex substrates and thereby provide easy access to [18F]cabozantinib directly. Hydrolysis was implemented before preparative purification due to challenges with on-column hydrolysis of the precursor 4, and [18F]cabozantinib was obtained in ≥99% radiochemical purity and in 2.8?±?0.05% (n?=?4) isolated decay corrected yield in a synthesis time of 90?minutes. The molar activity of representative batches was determined to be 17?±?8?GBq/μmol.
Lien, Vegard Torp,Klaveness, Jo,Olberg, Dag Erlend
p. 11 - 17
(2018/01/27)

Cabozantinib preparation method
The invention discloses a cabozantinib preparation method. The target product cabozantinib is prepared by performing five-step reaction on diethyl malonate, 4-fluoroaniline, 4-chloro-6,7-dimethoxyquinoline, 4-aminophenol, 1,2-dibromoethane and the like us
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(2017/08/28)

METHOD FOR TREATING OSTEOPOROSIS
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.
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Paragraph 0112

(2017/06/21)

Anti-tumor therapeutic drug card abundantly for Nepal synthetic method
The invention discloses a synthesis method of an antineoplastic drug cabozant inib. 4-(6,7-dimethoxyquinolin-4-oxygroup)-phenyl amine and 1-((4-fluorophenyl) carbamoyl) cyclopropane acyl halide and an acid-binding agent are adopted for reaction in an orga
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Paragraph 0054; 0056; 0067; 0068

(2017/08/24)

ASYMMETRIC BISAMIDATION OF MALONIC ESTER DERIVATIVES
The present invention relates to processes, process steps and intermediates useful in the asymmetric bisamidation of malonic ester derivatives wherein the new processes, process steps and intermediates are, for example, useful in the preparation of asymme
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Page/Page column 88

(2017/03/14)

A tyrosine kinase inhibitor and wherein the intermediate preparation method
The invention relates to a preparation method for a tyrosine kinase inhibitor and a midbody thereof. According to the method, a compound 1,1-cyclopropane dicarboxylic acid diester is taken as a raw material, and 1-((4-((6,7-dimethoxy quinoline-4-yl) oxy)
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Paragraph 0141; 0142; 0143

(2016/10/10)

DRUG COMBINATIONS TO TREAT MULTIPLE MYELOMA
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; 00119

(2016/03/19)

Methods of Using C-Met Modulators
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; 0100

(2016/03/05)

C-met modulator pharmaceutical compositions
Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
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Page/Page column 31; 35

(2016/10/10)

Crystal structures of intermediates in a new synthesis of antitumor drug cabozantinib
The heterocyclic antitumor drug cabozantinib was synthesized by condensation of 4-(6,7-dimethoxyquinolin-4-yloxy)aniline and methyl 1-(4-fluorophenylcarbamoyl)cyclopropanecarboxylate in the presence of two equivalents of sodium methoxide and azeotropic re
Laus, Gerhard,Schreiner, Erwin,Nerdinger, Sven,Kahlenberg, Volker,Wurst, Klaus,Vergeiner, Stefan,Schottenberger, Herwig
p. 323 - 332
(2017/03/11)

METHOD OF PREPARING FLUORINE-18 LABELED CABOZANTINIB AND ITS ANALOGS
The present invention relates to a method of preparing Cabozantinib (Cyclopropane- 1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinolin-4-yloxy)-phenylo]amide (4-fluoro- phenyl)amide) and 18F labeled Cabozantinib.
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Paragraph 00107

(2016/03/29)

METHOD OF TREATING LUNG ADENOCARCINOMA
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 00255; 00261

(2015/11/16)

NOVEL POLYMORPHS OF CABOZANTINIB (S)-MALATE AND CABOZANTINIB FREE BASE
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 21

(2015/12/08)

CABOZANTINIB DOSAGE FORM AND USE IN THE TREATMENT OF CANCER
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 00202

(2014/10/18)

DRUG COMBINATIONS TO TREAT CANCER
This invention relates to the combination of cabozantinib and abiraterone to treat cancer, particularly castration resistant prostate cancer.
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Paragraph 0077; 0078; 0085; 0086; 0087; 0088

(2014/10/18)

PROCESS FOR PREPARING QUINOLINE DERIVATIVES
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 0066; 0067; 0068

(2013/05/09)

METHOD FOR TREATING OSTEOPOROSIS
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 00111; 00117

(2013/04/10)

DUAL INHIBITOR OF MET AND VEGF FOR TREATING CANCER
This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and bone metastases, with a dual inhibitor of MET and VEGF.
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Paragraph 00124-00125

(2013/05/23)

A DUAL MET - VEGF MODULATOR FOR TREATING OSTEOLYTIC BONE METASTASES
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 00121

(2013/11/19)

METHODS OF USING C-MET MODULATORS
Disclosed are methods of treating cancer by administering a compound of Formula 1,or a pharmaceutically acceptable salt thereof, in combination with gemcitabine (GEM), or a pharmaceutically acceptable salt thereof, and optionally one or more additional tr
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(2012/04/04)

PROCESSES FOR PREPARING QUINOLINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH COMPOUNDS
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 30

(2012/08/28)

Method of Treating Cancer
This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1.
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(2012/10/08)

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
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

(2010/08/08)

C-MET MODULATORS AND METHODS OF USE
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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Page/Page column 212

(2008/06/13)