5-SUBSTITUTED 1-PHENYL-1,5-DIHYDROPIRIDO[3,2-b]INDOLE-2-ONES AND ANALOGUES AS ANTI-VIRUS PREPARATIONS Russian patent published in 2009 - IPC C07D471/04 A61K31/437 A61P31/12 A61P31/18 

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) C_1-10alkyl, substituted with aryl, where said aryl is substituted with radical -COOR⁴; or R² is ii) C_1-10alkyl, substituted with radical selected from -O-NR^5a-C(=NR^5b)-NR^5cR^5d, -NR⁷R⁸, radical

in which each Q¹ independently is simple bond, -CH₂-; each Q² independently is O; each R⁴ independently is hydrogen; each R^5a, R^5b, R^5c, R^5d independently is hydrogen; R⁷ is C_1-4alkyl; R⁸ is arylC_1-4alkyl; R¹¹ is aryl, C_1-4alkylcarbonyl, C_1-4alkyloxycarbonyl, hydroxyC_1-4alkyl, "Гет"₂; each R¹² independently is hydroxy, C_1-4alkyl; R^13a is C_1-4alkyl; each R^13b is C_1-4alkyl; or R² is iii) radical of formula:

-C_pH_2p-CH(OR¹⁴)-C_qH_2qR¹⁵ (b-3);

CH₂-CH₂-(O-CH₂-CH₂)_m-OR¹⁴ (b-4);

CH₂-CH₂-(O-CH₂-CH₂)_m-NR^I7eR^17b (b-5); where in radical (b-3) one of hydrogen atoms in -C_pH_2p- and one of hydrogen atoms in - CH(OR¹⁴)-C_qH_2q-, which are not part of R¹⁴, can be substituted with simple bond or C_1-4alkandiyl 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, C_1-4alkyl, C_1-4alkylcarbonyl; R¹⁵ is substituent selected from group consisting of NR^16aR¹⁶, pyrrolidine, pyperidinyl, homopyperidinyl, piperazinyl, , 4-(C_1-4alkyl)-piperazinyl, 4-(C_1-4alkylcarbonyl)-piperazinyl, 4-(C_1-4alkyloxycarbonyl)-piperazinyl, morpholinyl, thiomorpholinyl, 1,1-dioxo-thiomorpholinyl; R^16a and R^16b, independently on each other, are hydrogen, C_1-6alkyl or C_1-6alkyl, substituted with aryl; R^17a and R^17b, independently on each other, are hydrogen, C_1-4alkyl; or R^17a and R^17b, together with nitrogen atom, to which they are bonded, form pyrrolidine, morpholinyl; each R¹⁸ independently is arylC_1-4alkyl; R¹⁹ is hydrogen; R³ is nitrogroup; aryl is phenyl; "Гет"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