QUINAZOLINYLMETHYLENETRIAZOLINONES AS CDK-1 INHIBITORS Russian patent published in 2010 - IPC C07D417/06 C07D417/14 A61K31/517 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a compound of formula I and to its pharmaceutically acceptable salts. In formula I , R₁ means hydrogen or ; is specified from phenyl, and a 5-member heteroaromatic ring containing 1 to 2 heteroatoms specified inhe group consisting of sulphur and nitrogen; X is specified from lower alkylene, cyclisated lower alkylene containing 3 to 6 carbon atoms, and hydroxy(lower alkylene); R₅ and R₆ are independently specified in the group including hydrogen, lower alkyl, halogen and lower alkoxygroup; R₃ is specified from hydrogen and -NH-R₇; R₄ is specified from hydrogen and -O(CH₂CH₂O)_y-R₁₀; R₇ means lower alkyl; R₁₀ means lower alkyl; n means an integer within 0 to 1; and y is equal to 0; provided when n is equal to 0, and R₁ means hydrogen, then R₃/R₄ both cannot mean hydrogen. The invention also concerns a pharmaceutical composition containing a therapeutically effective amount of the compound under the invention.

EFFECT: preparation of the new compounds which show CDK1 kinase inhibiting activity and can be effective in cancer treatment, particularly breast cancer, lung cancer, colon cancer and prostate cancer treatment.

45 cl, 21 ex