CONFORMATIONALLY RESTRICTED PI3K AND MTOR INHIBITORS Russian patent published in 2018 - IPC C07D498/14 C07D513/14 A61K31/519 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) and (II) and their stereoisomers and pharmaceutically acceptable salts that inhibit phosphoinositide-3-kinase (PI3K) and a mammalian target of rapamycin (mTOR), that are conformationally restricted. In formulae (I) and (II) , R₁ is and the wavy lines indicate bonding site of R₁; X is selected from the group consisting of O and NR₇; R_3x, R_3y, R_3z and R_3P are independently selected from the group consisting of hydrogen, methyl and ethyl; R₅, R₆ and R₇ are independently selected from H and C₁-C₆ alkyl; R₂ is independently selected from the groups consisting of both phenyl and monocyclic heteroaryl with 1 to 2 nitrogen heteroatoms with 1 to 2 substituents selected from C₁-C₄ alkyl, cyclopropyl, F, Cl, Br, I, -OR₅, CN, CF₃, CHF₂, CFH₂, NR₇COR₅ and NR₅R₆. Preferably, R₂ represents

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EFFECT: compounds can be used to treat cancer, modulated with PI3K.

13 cl, 6 tbl, 10 ex