4-MONOSUBSTITUTED THIAZOLINE-QUINOLINES Russian patent published in 2010 - IPC C07D417/14 C07D417/06 A61K31/4709 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I and their pharmaceutically acceptable salts. Disclosed compounds have inhibitory effect on CDK1 kinase and can be used to prepare medicinal agents for treating diseases associated with abnormal cell cycle development. In formula I , R₁ is hydrogen, -C(O)OR₉ or R₂-(X)_n-; X is (lower)alkylene, hydroxy(lower)alkylene, cyclised(lower)alkylne or mono- or dihalogen(lower)alkylene; R₂ is a group, where denotes a phenyl or a 5-6-member heteroaromatic ring containing 1-2 heteroatoms selected from a group comprising oxygen, sulphur and nitrogen atoms; R₅, R₆ and R₇ are independently selected from a group comprising hydroxy, hydrogen, (lower)alkyl, halogen and (lower)alkoxy; R₄ is a halogen, , (O)_k(CH₂CH₂O)_y-R₁₀, , -S-R₁₂ or -O-(CH₂)_tR₁₄, where denotes a phenyl, a cycloalkyl ring containing 3-6 carbon atoms, a 4-6-member heterocycloalkyl containing 3-5 carbon atoms and 1-2 heteroatoms selected from a group comprising oxygen, nitrogen and sulphur atoms; R₉, R₁₁, R₁₅ and R₁₆ independently denote (lower)alkyl; R₁₀ and R₁₂ denote (lower)alkyl; R₁₄ denotes perfluoro(lower)alkyl or -NR₁₅R₁₆; R₁₇ and R₁₈ independently denote hydrogen, , F, OCH₃ and -C(=O)CH₃; n and k are equal to 0 or 1; m, w, y and z are equal an integer from 0 to 3; and t equals an integer from 0 to 6.

EFFECT: invention also relates to a pharmaceutical composition having antiproliferative activity, containing one or more of the disclosed compounds.

65 cl, 1 tbl, 49 ex