| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of formula(1) and/or to their pharmaceutically acceptable salts, where Arepresents CH; Aand Aindependently represent CRor N; Aand Atogether with ring B represent 5-membered heteroaryl or heterocycle, with said 5-membered heteroaryl or heterocycle being selected fromwhere t represents 1 or 2; and Ris independently selected from H, C-Calkyl, C-aryl, C-C-membered cycloalkyl, C(O)NRR, -OR, heteroaryl, representing pyridine, and heterocycle, representing piperidine and tetrahydropyran; and each of said alkyl, aryl, cycloalkyl, heteroaryl and heterocycle can be substituted with one group, independently selected from C-Calkyl, possibly substituted with one substituent, selected from -CONMe, C-membered cycloalkyl, -CN, -OMe, -pyridine, tetrahydropyran, -CO-morpholine, -CO-pyrrolidine, (3-methyl)oxetane; -OH; -C(O)R; -CN; -C(O)NRR; -NRR; -OR; -S(O)R; halogen, and substituted with one group -COMe heterocycle, representing piperidine, on condition that when Arepresents CR, Aand Atogether with ring B are selected from structure (3), (5) or (6);represents single bond or double bond; Rrepresents heteroaryl, representing 6-membered or 9-10-membered aromatic mono- or bicyclic ring, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; possibly substituted with one or two groups, independently selected from Calkyl, Calkinyl, -NRR, -NRS(O)R, -OR, halogen, halogenalkyl; Ris independently selected from H; each R, R, R, R, and Ris independently selected from H; C-Calkyl, possibly substituted with one substituent, selected from -OH, -OMe, -CN, -NH, -NMe, C-cycloalkyl; C-Calkenyl; Calkinyl; Caryl, possibly substituted with one or more substituents, selected from fluorine or methyl group; C-membered cycloalkyl, possibly substituted with one substituent, selected from -OH and -CN; halogenalkyl; heteroaryl, representing pyridine; and substituted with one methyl group heterocycle, representing piperidine, or Rand Rtogether with atom (atoms) which they are bound to form 5-6-membered heterocyclic ring, representing pyrrolidine or morpholine; and in each case n is independently equal 2. Invention also relates to particular compounds, pharmaceutical composition, based on claimed compounds; method of inhibiting PI3K and/or mTOR activity and to application of claimed compounds.EFFECT: novel compounds, useful for inhibiting PI3K and/or mTOR activity have been obtained.15 cl, 16 ex |
