FIELD: chemistry.
SUBSTANCE: present invention relates to organic chemistry and specifically to novel morpholinopurine derivatives of general formula
,
or a pharmaceutically acceptable salt thereof, where R1 and R2, each independent of each other, denote a C1-C6 alkyl group or a hydrogen atom, R3a and R3b, each independent of each other, denote a C1-C6 alkyl group which can contain three substitutes selected from a group A, or a hydrogen atom, R4 denotes a C1-C6 alkyl group or a hydrogen atom, Ra denotes a group of formula -Y-R , where Y denotes a single bond or a C1-C6 alkylene group, R5 is a C1-C6 alkyl group which can contain one, two or three substitutes selected from group A, a tetrahydrofuranyl group, a pyrrolidinyl group which contains one substitute selected from a group D, and Rb and Rc, each independent of each other, denote a C1-C6 alkyl group which contains one substitute selected from a group E, or a hydrogen atom, or Rb and Rc, together with a nitrogen atom to which they are bonded, for a 5-7-member alicyclic nitrogen-containing heterocyclic group, which is pierazine, morpholine, pyrrolidine, piperidine, homopiperazine, which can contain one, two or three substitutes selected from group E; group A: halogen atom, hydroxy group, C3-C8 cycloalkyl group and oxy group; group D: C1-C6 alkylsulphonyl group; and group E: hydroxy group, formyl group, C1-C6 alkyl group, which can contain one substitute selected from said group A, diC1-C6 alkylamino group, C1-C6 alkylsulphonylamino group, C1-C6alkylsulphonyl C1-C6 alkylamino group, C1-C6 alkylsulphonylamino C1-C6alkyl group, C1-C6alkylcarbonyl group, which can contain one substitute selected from said group A, C1-C6 alkylsulphonyl group, C1-C6 alkylamino C1-C6 alkylcarbonyl group, diC1-C6 alkylamino C1-C6alkylcarbonyl group, which can contain one substitute selected from said group A, diC1-C6 alkylaminocarbonyl group, phenylsulphonyl group and hateroaryl C1-C6 alkylcarbonyl group, where the heteroaryl is imidazolyl. The invention also relates to a pharmaceutical composition, an inhibitor of phosphatidylinositol-3-kinase (PI3K), an inhibitor of mammalian target of rapamycin (mTOR) based on the compound of formula (1a), a method of treating cancer and use of the compound of formula (1a).
EFFECT: obtaining novel morpholinopurine derivatives, having useful biological properties.
42 cl, 19 tbl, 138 ex
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