SUBSTITUTED QUINOLINE DERIVATIVES AS MITOTIC KINESIN INHIBITORS Russian patent published in 2010 - IPC C07D215/12 C07D215/18 A61K31/47 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted quinoline derivatives of general formula (I) in which: m is an integer from 0 to 3; R¹ is selected from a group comprising an acylamino group, ester carboxylic group and an alkyl with 1-5 carbon atoms, an optionally substituted hydroxy and a halogen; R² denotes hydrogen or an alkyl with 1-5 carbon atoms; R³ denotes - C(=X)-A, where A is selected from a group comprising aryl, heteroaryl, heterocyclyl and cycloalkyl, each of which can optionally contain from 1 to 4 substitutes selected from a group comprising an alkyl with 1-4 carbon atoms, an alkoxy with 1-4 carbon atoms, a halogen, hydroxy or nitro, and X denotes oxygen or sulphur; R⁴ denotes alkylene-heterocyclyl or alkylene-NR⁷R⁸, where alkylene is a linear alkylene with 1-4 carbon atoms; R⁷ and R⁸ are independently selected from a group comprising hydrogen, an alkyl with 1-4 carbon atoms, arylalkyl, heteroarylalkyl, cycloalkyl or cyclo-alkylalkyl; R⁵ is selected from a group comprising L-A¹, where A¹ is selected from a group comprising aryl, heteroaryl, heterocyclyl and cycloalkyl, each of which can optionally contain from 1 to 4 substitutes selected from a group comprising an alkyl with 1-4 carbon atoms, an alkoxy with 1-4 carbon atoms, a halogen, hydroxy and nitro, and where L is selected from a group consisting of oxygen, -NR⁹, where R⁹ denotes hydrogen or alkyl; -S(O)_q-, where q equals 0, 1 or 2, and an alkylene with 1-5 carbon atoms, optionally substituted with a hydroxy, halogen or acylamino; and R⁶ is selected from a group comprising an alkyl with 1-5 carbon atoms, an alkenyl with 2-5 carbon atoms, an alkynyl with 2-5 carbon atoms, -CF₃, an alkoxy with 1-5 carbon atoms, a halogen and a hydroxy; or its pharmaceutically acceptable salts or esters, as well as to a pharmaceutical composition having anticancer activity or inhibitory effect on mitotic kinesin based on the said compounds, to a method of treating disorders and use of these compounds for making a medicinal agent.

EFFECT: novel compounds which can be useful in treating cancer are obtained and described.

40 cl, 3 ex, 1 tbl