NOVEL DERIVATIVES OF 2,3-DIHYDRO-1H-IMIDAZO[1,2-a]PYRIMIDIN-5-ONE, METHOD OF OBTAINING THEREOF AND APPLICATION IN PHARMACY Russian patent published in 2015 - IPC C07D487/04 A61K31/5377 A61P35/00 A61P33/02 A61P33/06 A61P35/02 

Abstract RU 2554868 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula (I), possessing properties, making it possible to inhibit phosphorylation of AKT (proteinkinase B; PKB), to versions of method of their obtaining, as well as to intermediate products for their obtaining. In particular compounds can be applied in treatment of different tumours and/or metastases, as well as in case parasitic diseases such a malaria. In formula (I), R1 stands for -L-phenyl or -L-heteroaryl, with term "heteroaryl" standing for bicyclic radical, containing from 9 to 12 units, L stands for either linear or branched alkyl, containing 1-6 carbon atoms, optionally substituted with hydroxyl, or CO group, or group L'-X, where L' stands for linear or branched alkyl, containing 1-6 carbon atoms, and X stands for oxygen or sulphur atom; with phenyl and heteroaryl being optionally substituted with one or several radicals, similar or different, selected from halogen atoms, -NRxRy, alkoxy and alkyl; with said alkyl being optionally substituted with one or several halogen atoms; R2 stands for hydrogen atom or alkyl; R3 stands for alkyl, optionally substituted with one or several halogen atoms; R4 stands for hydrogen atom or halogen atom; with NRxRy being such that Rx and Ry form together with nitrogen atom, which they are bound to, cyclic radical, including 3-10 units, and optionally oxygen atom; and all alkyl or alkoxy radicals, mentioned above, are linear or branched and contain 1-6 carbon atoms.

EFFECT: compounds can be applied as active component for obtaining medications, intended for treatment or prevention of disease, characterised by deregulation of protein- or lipidkinase activity.

25 cl, 3 tbl, 43 ex

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RU 2 554 868 C2

Authors

Brollo Moris

Kloss Anni

Ehl' Amad Jussef

Filosh-Romme Brjuno

Alle Frank

Karlsson Karl Andreas

Marsin'Jak Zhil'Ber

Ronan Batist

Shio Loran

Vive Bertran

Viv'Jani Fabris

Zimmermann Andre

Dates

2015-06-27Published

2010-07-01Filed