| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: invention relates to novel compounds of formula (I) to its salts, in which X is bivalent radical NR2, O; R1 is cyanogroup; n equals 1; R2 is: i) C1-10alkyl, substituted with aryl, where said aryl is substituted with radical -COOR4; or R2 is ii) C1-10alkyl, substituted with radical selected from -O-NR5a-C(=NR5b)-NR5cR5d, -NR7R8, radical ^ ^ in which each Q1 independently is simple bond, -CH2-; each Q2 independently is O; each R4 independently is hydrogen; each R5a, R5b, R5c, R5d independently is hydrogen; R7 is C1-4alkyl; R8 is arylC1-4alkyl; R11 is aryl, C1-4alkylcarbonyl, C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, "ôé"2; each R12 independently is hydroxy, C1-4alkyl; R13a is C1-4alkyl; each R13b is C1-4alkyl; or R2 is iii) radical of formula: ^ ^ -CpH2p-CH(OR14)-CqH2qR15 (b-3); ^ CH2-CH2-(O-CH2-CH2)m-OR14 (b-4); ^ CH2-CH2-(O-CH2-CH2)m-NRI7eR17b (b-5); where in radical (b-3) one of hydrogen atoms in -CpH2p- and one of hydrogen atoms in - CH(OR14)-CqH2q-, which are not part of R14, can be substituted with simple bond or C1-4alkandiyl group; p equals 1, 2 or 3; q equals 0, 1, 2 or 3; each m independently equals 1-10; each R independently is hydrogen, C1-4alkyl, C1-4alkylcarbonyl; R15 is substituent selected from group consisting of NR16aR16, pyrrolidine, pyperidinyl, homopyperidinyl, piperazinyl, , 4-(C1-4alkyl)-piperazinyl, 4-(C1-4alkylcarbonyl)-piperazinyl, 4-(C1-4alkyloxycarbonyl)-piperazinyl, morpholinyl, thiomorpholinyl, 1,1-dioxo-thiomorpholinyl; R16a and R16b, independently on each other, are hydrogen, C1-6alkyl or C1-6alkyl, substituted with aryl; R17a and R17b, independently on each other, are hydrogen, C1-4alkyl; or R17a and R17b, together with nitrogen atom, to which they are bonded, form pyrrolidine, morpholinyl; each R18 independently is arylC1-4alkyl; R19 is hydrogen; R3 is nitrogroup; aryl is phenyl; "ôé"2 is piridyl. Invention also relates to pharmaceutical composition, to method of obtaining compound on any of ii 1-4, as well as to compounds of formula (IV-a), (IV-b),(V). ^ EFFECT: obtaining novel biologically active compounds possessing ability to inhibit HIV. ^ 11 cl, 18 ex, 3 tbl |
