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Применить Всего найдено 7. Отображено 7.
31-01-2019 дата публикации

DIFLUOROMETHOXY SUBSTITUTED DIPHENYLETHANE AND TRANS-STILBENE DERIVATIVES, AND PREPARATION METHOD THEREFOR AND USE THEREOF

Номер: WO2019020026A1
Принадлежит:

Disclosed are a difluoromethoxy diphenylethane and trans-stilbene derivatives, and a preparation method therefor and the use thereof. The present invention conducts a chemical structure modification with a difluoromethoxy group at the 4' position of the B-aryl ring of diphenylethane/stilbene, and the 3' position thereof is modified into a substituent such as a nitro, amino or hydroxyl. The difluoromethoxy diphenylethane and trans-stilbene derivatives obtained by the present invention have strong anti-tumour activity in vitro, with the introduction of the difluoromethyl changing the physical, chemical and biological properties of the compounds, and have a significant inhibitory effect on tumour cells.

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31-01-2019 дата публикации

GEM-DIFLUOROETHYL SUBSTITUTED STILBENE AND DIPHENYLETHANE DERIVATIVES, AND PREPARATION METHOD THEREFOR AND USE THEREOF

Номер: WO2019020029A1
Принадлежит:

Disclosed are a gem-difluoroethyl substituted stilbene and diphenylethane derivatives, and a preparation method therefor and the use thereof. The present invention conducts a chemical structure modification with a gem-difluoroethyl at the 4' position of the B-aryl ring of diphenylethane/stilbene, and the 2' position thereof is modified into a substituent such as a nitro or amino. The gem-difluoroethyl substituted stilbene and diphenylethane derivatives have strong anti-tumour activity in vitro, with the anti-tumour activity of the trans-structure thereof better than that of the cis-structure thereof, and with the introduction of a fluorine atom not only changing the physical properties of the compounds themselves but also enhancing the anti-tumor activity in vitro, and have a good inhibitory effect on a variety of tumour cells. (I) ...

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22-04-2010 дата публикации

ETHOXY DIPHENYL ETHANE DERIVATES, PREPARATION PROCESSES AND USES THEREOF

Номер: WO2010043180A1
Принадлежит:

Disclosed are ethoxy diphenyl ethane derivates, preparation processes and uses thereof. Diphenyl ethane is chemically modified by ethoxy substituted on the 4'-position of its B aryl ring and is changed into their soluble prodrugs of phosphates or the like by modifying the hydroxyl on the 3'-position of their B aryl ring. Similarly, side chain of amino acid can be introduced to 3'-amino to form soluble prodrug of amino acidamide. The structure of the said compounds is showed as formula (I). Ethoxy diphenyl ethane derivates and prodrugs thereof are characterized by the following: possessing potent tubulin polymerizaion inhibitory activity; possessing obvious target damage of tumour vessel; resulting in dysfunction and structural damage of tumour vessel selectively; evoking die of vessel endothelium cell; making the tumor cell lose nourishment and oxygen; and killing tumor cell or inhibiting tumor metastasis.

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16-05-2019 дата публикации

5-FLUOROURACIL DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF

Номер: WO2019090558A1
Принадлежит:

Disclosed is a 5-fluorouracil derivative having the molecular structure shown in general formula VI, in which Ra and Rb groups are an alkoxy group or a fluorine-substituted alkoxy group having 1, 2, 3, or 4 carbon atoms, and are mono-, bis-, tri-, tetra- or penta-substituted on a phenyl group; a linking group L1 is an alkyl or alkenyl group having 1, 2, 3, or 4 carbon atoms, a linking group L2 is oxygen, or an alkyl or alkoxy group having 1, 2, 3, or 4 carbon atoms, or an amino acid, or an alkyl group having 1, 2, 3, or 4 carbon atoms containing an amino moiety, or a furyl group, and an X group is O or -NH-. Further disclosed is a method for preparing such a derivative and a use of the same in the treatment of cancer, tumor diseases, and diseases caused by abnormal neovascularization in a human or non-human mammal, and a medicament or a composition containing the 5-fluorouracil derivative.

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31-01-2019 дата публикации

CA-4 ANTITUMOUR DRUG, SYNTHESIS METHOD AND USE THEREOF

Номер: WO2019020016A1
Принадлежит:

Disclosed are a CA-4 antitumour drug, a synthesis method and the use thereof. The CA-4 antitumour drug introduces an alkoxy group or a fluorine-containing alkoxy group at the 4' position of a natural product, i.e., combretastatin, and carries out functional chemical modification at the 3' position thereof. The CA-4 antitumour drug of the present invention has an inhibitory ability for the two targets of tubulin and aryl sulfatase and can be used for antitumour therapy.

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08-12-2004 дата публикации

催化法制备叠氮磷酸二苯酯

Номер: CN0001552719A
Принадлежит:

A process for preparing diphenyl azidophosphate by catalytic method features the reaction between its raw materials (diphenyl chlorophosphate and sodium azide) and the phase-transfer catalyst chosen from quaternary ammonium salt, inorganic tetraamine salt, strong-alkaline alamine and crown ether at 15-30 deg.c for 10-15 hr. Its advantages are simple process and high purity of product.

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27-12-2018 дата публикации

TWIN DRUG-TYPE HMG-COA REDUCTASE INHIBITOR AND SYNTHESIS METHOD THEREFOR

Номер: WO2018233595A1
Принадлежит:

Disclosed is a twin drug-type HMG-CoA reductase inhibitor, which is a twin drug formed by chain linking a fibrate compound, selected from any one of gemfibrozil, clofibric acid, fenofibrate acid, bezafibrate or ciprofibrate, or nicotinic acid or acipimox and a statin by a linker Br-(CH2)n-Br, Br-(CH2)n-OH or Br-(CH2)n-NH2, wherein n is an integer from 1 to 30, and the statin is mevastatin, lovastatin, simvastatin, pravastatin, fluvastatin, cerivastatin, atorvastatin, rosuvastatin or pitavastatin.

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