QUINAZOLINE DERIVATIVES Russian patent published in 2019 - IPC C07D239/94 C07D403/12 A61K31/517 A61P35/00 

Abstract RU 2704125 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a novel compound of formula (I) and a pharmaceutically acceptable salt thereof. Compounds have the properties of a kinase activity inhibitor and can be used in preparing a drug for treating thyroid cancer, non-small cell carcinoma, epidermoid carcinoma, melanoma, colon cancer, gastric carcinoma, oesophageal cancer, pancreatic cancer, kidney cancer, liver cancer, lung cancer or ovarian cancer. In general formula (I)

,

R1 is -O(CH2)nR3, where n equals 3, 4 or 5; R3 is NReRf, where Re and Rf each is independently selected from a group comprising C1-6 alkyl, or Re and Rf are joined together to form - (CH2)4-; R2 is or Compounds of formula (I) are obtained by reacting a compound of formula (III) or a salt thereof with a compound of formula (IV) or a salt thereof in a solvent in the presence of one or more catalyst, base and surfactant according to the following scheme:

.

In said structural formulas R1, R2, R3 and n are defined above, L is halogen, hydroxyl, mesyloxy or hydrogen and p = 0 or 1 with the proviso that when p = 1, L is hydrogen.

EFFECT: compounds of formula (I) show higher activity as compared to compounds with similar structure.

8 cl, 4 tbl, 37 ex

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RU 2 704 125 C2

Authors

Shi Jing

Gao Kingzkhi

Chen Ksiaozuo

Mi Ji

Zang Jaran

Yang Khanyu

Chen Yudzhi

Liu Chunlej

Mi Guoruj

Ma Yuksiu

Shen Dongmin

Guo Yang

Fan Lindzhing

Dates

2019-10-24Published

2015-08-11Filed