SALTS OF EPIDERMAL GROWTH FACTOR RECEPTOR KINASE Russian patent published in 2020 - IPC C07D403/12 A61K31/506 A61P35/00 

Abstract RU 2711077 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel salt forms of a compound of formula 2 or a hydrate or solvate thereof. Compounds have selective inhibition properties of at least one epidermal growth factor receptor (EGFR) mutant compared to wild-type EGFR (EGFR WT). Mutant of epidermal growth factor receptor kinase (EGFR) receptors is an activating mutant, a deletion mutant, a mutation with a point mutation or a mutant selected from T790M, deIE746-A750, L858R and G719S. Salts of compound 2 are described by general formula

where n is 1 or 2; and X is hydrobromic acid, benzenesulphonic acid, camphorsulphonic acid, 1,2-ethane disulphonic acid, hydrochloric acid, maleic acid, methanesulphonic acid, naphthalene-2-sulphonic acid, 1,5-naphthalene disulphonic acid, oxalic acid, 4-toluenesulphonic acid or 2,4,6-trihydroxybenzoic acid. Also described are crystal forms of salts characterized by data of X-ray powder diffraction pattern.

EFFECT: compounds can be used in treating tumorous diseases, such as non-small-cell lung cancer.

31 cl, 87 dwg, 21 tbl, 16 ex

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RU 2 711 077 C2

Authors

Laj Mej

Vitovski Stiven Richard

Tester Richland Vejn

Li Kvangkho

Dates

2020-01-15Published

2013-03-13Filed