N-9-SUBSTITUTED PURINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE Russian patent published in 2017 - IPC C07D473/00 C07D473/34 A61K31/52 A61P35/00 

Abstract RU 2607635 C2

FIELD: chemistry.

SUBSTANCE: present invention relates to novel compounds of formula I-A, having properties of inhibitors of kinase of phosphoinositide-3-kinase family mTOR and PI3K, for use in treating cancer, as well as for preparing drugs for treating cancer. In compounds of formula I-A R1 is selected from a group comprising cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, oxetan-2-yl, oxetan-3-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl and tetrahydropyran-4-yl, oxepan-2-yl, oxepan-3-yl, oxepan-4-yl, phenyl pyrrol-2-yl, pyrrol-3-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl, furan-2-yl, furan-3-yl, thien-2-yl, thien-3-yl, thiazol-2-yl, thiazol-3-yl, thiazol-4-yl, imidazol-1-yl, imidazol-4-yl, pyrid-2-yl, pyrid-3-yl, pyrid-4-yl, pyrimidin-1-yl, pyrimidin-2-yl, pyrimidin-3-yl, pyrazin-2-yl, pyridazin-2-yl, pyridazin-3-yl and triazin-2-yl, where R1 substituted by 0-3 substitutes RR1, selected from a group consisting of halogen, F, Cl, Br, I, -ORa, -C(O)Ra, -Rc; where Ra is selected from hydrogen or C1-6alkyl, Rc is C1-6alkyl; R2 is selected from a group comprising hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl; R3 is a morpholine-4-yl, where group R3 is substituted with 0–3 substitutes RR3, selected from a group consisting of -Ri, halogen, where Ri is selected from C1-6alkyl, C1-6haloalkyl; D is -NR4C(O)NR5R6 or -NR5R6, where R4 and R5 each denotes hydrogen and R6 is C1-6alkyl, C1-6haloalkyl oxetan-3-yl and pyridyl-on.

EFFECT: treatment of cancer.

11 cl, 1 tbl, 26 ex

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RU 2 607 635 C2

Authors

Kevin Khonlyun Lau

Vendi Li

Dzhozef P. Lissikatos

Chzhonkhua Pej

Kerk D. Robardzh

Dates

2017-01-10Published

2010-11-10Filed