574745-76-9Relevant academic research and scientific papers
Angiogenesis inhibitor as well as preparation method and application thereof
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, (2021/02/13)
The invention belongs to the technical field of medicines, and discloses a compound shown as a formula I or pharmaceutically acceptable salt, prodrug, metabolite, isotope derivative and solvate thereof. The compound provided by the invention is a cyclobutyl-containing compound used as a tyrosine kinase inhibitor, and can be used for treating tyrosine kinase, especially tumor diseases related to VEGFR. Due to the existence of the cyclobutyl group, the rigidity of a branched chain molecule can be improved, the directivity of the molecule is improved, the compound can be better combined with a target easily, the dosage of a drug can be reduced, and the side effect of the drug is reduced. The invention also provides a preparation method of the compound and application of the compound in treatment of tumor diseases caused by abnormal activity of tyrosine kinase such as VEGFR.
Synthesis method of cediranib intermediate
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Paragraph 0034; 0040; 0046; 0048; 0052; 0053; 0058; 0064, (2018/05/03)
The invention relates to the field of drug synthesis and particularly relates to a synthesis method of a cediranib intermediate. The synthesis method comprises the following steps: adding a certain amount of reaction solvent into a flask, filling introducing inert protection gas, adding a certain amount of 4-chlorochlorine-6-methoxy-7-benzyloxy-quinazoline, 4-fluorofluorine-5-hydroxy-2-methylindole and alkali under the light shielding condition, starting stirring, reacting for a period of time under a certain temperature to obtain a reaction mixed solution, reducing the temperature of the reaction mixed solution to room temperature, filtering, collecting filtrate, transferring the filtrate into a 2L high-pressure reaction kettle, adding a catalyst, filling introducing hydrogen, starting stirring, reacting for a period of time under a certain temperature, removing a reaction solution, filtering the reaction solution, carrying out pressure-reduced desolvation of the filtrate, adding water, washing and filtering, drying filter cake in vacuum to obtain the cediranib intermediate. The structure formula of the cediranib intermediate is as follows: a formula is as shown in the description. Through the synthesis method of the cediranib intermediate, the complicated separation process of the synthesized intermediate is avoided; the operation is simple; the yield is further improved; theindustrial amplified production is facilitated.
west Neeb salt and its crystalline form, and its preparation method and pharmaceutical composition (by machine translation)
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Paragraph 0122, (2017/03/21)
The invention relates to west Neeb salt and its crystalline form, compared with the prior art, and its west Neeb salt of the invention the crystalline form has more excellent in water solubility. The present invention also relates to the west states the Neeb salt and its crystal preparation method, the medicament composition and its use in treating and/or preventing the pathological angiogenic diseases use of the medicament. (by machine translation)
THERAPEUTIC COMPOUNDS AND USES THEREOF
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, (2014/09/03)
Described herein are compounds of Formula (I)-(III), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating and/or preventing diseases are also provided.
VEGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY
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Page/Page column 28, (2009/04/24)
The present invention relates to VEGFR inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.
CHEMICAL PROCESS
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Page/Page column 55-56, (2008/12/05)
The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline.
