DERIVATIVES OF 6-AMINO QUINAZOLINE OR 3-CYANOQUINOLINE, METHODS OF THEIR PRODUCTION AND THEIR APPLICATION AS INHIBITORS OF RECEPTOR TYROZINE KINASES EGFR OR HER-2 Russian patent published in 2014 - IPC C07D401/12 C07D401/14 C07D403/12 C07D403/14 C07F9/6558 A61K31/4709 A61K31/517 A61P35/00 

Abstract RU 2536102 C2

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to heterocyclic compound of formula (I) or its racemate, enantiomer, diastereoisomer and their mixture, as well as to their pharmaceutically acceptable salt, where A is selected from the group, consisting of carbon atom or nitrogen atom; when A represents carbon atom, R1 represents C1-C6-alkoxyl; R2 represents cyano; when A represents nitrogen atom, R1 hydrogen atom or C1-C6-alkoxyl; where said C1-C6-alkoxyl is optionally additionally substituted with one C1-C6-alkoxyl group; R2 is absent; R3 represents radical, which has the formula given below: or , where D represents phenyl, where phenyl is optionally additionally substituted with one or two halogen atoms; T represents -O(CH2)r-; L represents pyridyl; R4 and R5 each represents hydrogen atom; R6 and R7 each is independently selected from hydrogen atom or hydroxyl; R8 represents hydrogen atom; R9 represents hydrogen atom or C1-C6-alkyl; r equals 1 and n equals 2 or 3. Invention also relates to intermediate compound of formula (IA), method of obtaining compound of formulae (I) and (IA), pharmaceutical composition based on formula (I) compound and method of its obtaining and to application of formula (I) compound.

EFFECT: novel heterocyclic compounds, inhibiting activity with respect to receptor tyrosine kinases EGFR or receptor tyrosine kinases HER-2 are obtained.

18 cl, 12 ex, 4 tbl

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RU 2 536 102 C2

Authors

Tan Pehn Cho

Li Sin'

Van Bin'

Van Tszjun'

Chehn' Litszjun'

Dates

2014-12-20Published

2010-08-26Filed