NOVEL DERIVATIVES OF 1,2,3,4-TETRAHYDROPYRIMIDO{1,2-a}PYRIMIDIN-6-ONE, OBTAINING THEREOF AND PHARMACEUTICAL APPLICATION

摘要

FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to novel compounds of formula (I) or their additive salts with inorganic and organic acids, a method of obtaining thereof and application. The compounds can be used in the treatment of primary tumours and/or metastases, in particular, in case of cancer tumours of the stomach, liver, kidneys, ovaries, large intestine, prostate, endometrium, lungs (NSCLC and SCLC), glioblastomas, cancer tumours of the thyroid gland, urinary bladder, mammary gland, in case of melanomas, in case of lymphoid or myeloid tumours of the haematopoietic system, in case of sarcomas, in case of cancer tumours of the brain, larynx, lymphatic system, cancer tumours of bones and pancreas, in case of hamartomas, as well as in the treatment of malaria. In formula (I),R1 represents -L-aryl or branched -L-heteroaryl, where L represents a simple bond, or a lineaer or branched alkyl, containing from 1 to 6 carbon atoms and having in case of necessity a hydroxygroup, or groups CO or -CO-Alk-; with aryls and hetaroaryls in case of necessity having one or several substituents, which are similar or different and selected from atoms of halogens, alkoxy- and alkyls; with the latter said alkoxy- and alkyls, in turn, having one or several substituents, which are similar or different and selected from atoms of halogens; R2 represents a hydrogen atom or alkyl; R3 represents an alkyl, which has in case of necessity one or several atoms of halogens as substituents; R4 represents a hydrogen atom or a halogen atom; with the term "aryl" standing for phenyl, and the term "heteroaryl" standing for pyridyl or benzothienyl; all the alkyls (alk) and alkoxy, mentioned above, are linear or branched and contain from 1 to 6 carbon atoms.EFFECT: compounds possess properties of the phosphorilation inhibitor AKT(PKB).20 cl, 2 tbl, 56 ex