FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to novel dihydropteridinone derivatives of formula (I), method of obtaining thereof (versions) and their pharmaceutical application as Plk kinase derivatives. In formula
R1 and R2 each is independently selected from the group, consisting of a hydrogen atom and C1-6alkyl; R3 is selected from the group, consisting of C1-6alkyl and C5-6cycloalkyl; R4 and R5 each is independently selected from the group, consisting of a hydrogen atom, C1-6alkyl, where the alkyl is optionally substituted with one or more groups, selected from the group, consisting of C1-6alkoxyl and -NR9R10; R6 is selected from the group, consisting of C1-3alkyl, C5-6cycloalkyl, heterocyclic alkyl, selected from a 6-membered heterocyclic alkyl with 1 nitrogen atom, hexahydrocyclopenta(c)pyrrol or cyclopenta(c)piperidine, where C1-3alkyl, C5-6cycloalkyl or heterocyclic alkyl each is optionally substituted with one or more groups, selected from the group, consisting of C1-6alkyl, C1-6alkoxyl, hydroxyl, C3-6cycloalkyl, C3-6cycloalkylC1-6alkyl, heterocyclic alkyl, N-methylmorpholine, hexahydropyrrolo[2,1-c][1,4]oxazine, -C(O)R9, -NR9R10 and C1-6alkylcarbonyloxygroup; where R9 and R10 together with a nitrogen atom which they are bound to form a 4-8-membered heterocycle, where the 4-8-membered heterocycle contains one or more N or O heteroatoms and the 4-8-membered heterocycle is optionally substituted with C1-6alkyl, optionally substituted with C3-6cycloalkyl; R7 and R8 each is independently selected from a hydrogen atom or C1-6alkyl; R9 and R10 each is independently selected from a hydrogen atom or C1-6alkyl. The invention also relates to a novel intermediate compound of formula (IA), where R1, R2 R3 R4, R5, R7, R8 R9 and R10 have the said values; R11 is selected from the group, consisting of hydroxyl or C1-6alkoxyl. The method of obtaining the formula I compound consists in the interaction of the formula
compound with R6NH2 compound, or in the interaction of the formula (IB) compound with the formula (IC) compound. Formulae (IB) and (IC) are given in the invention formula.
EFFECT: compounds can be used for obtaining the medication for treating a cell proliferation disorder, in particular, in case of a disorder, which is cancer, which is selected from the group, consisting of non-small lung cancer, squamous cell carcinoma, breast cancer, ovarian cancer, cervical cancer, papillary carcinoma or colorectal carcinoma, preferably cervical cancer or colorectal carcinoma.
11 cl, 2 tbl, 47 ex
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