Arildihidroisoquinolinonas replaced with azaciclilo, Process for their Preparation and their use as medicines

摘要

It refers to arildhioquinolinones, its derivatives, physiologically tolerant salts and physiological functional derivatives, its preparation, arildhioquinonia (alternative) drug containing at least one azacnil or its derivatives, Arildhiisoquinone and its derivatives, which are currently replaced by azacyclo, are used as the opposite cubes of vinyl chloride monomer. Item 1: a formula compound (1)This means, R1, R1 ',R1,8-1-1-1-1-8, or 8-8-8-1-1-1-1-1-8, or 8-8 (R3) (R4),So2-ch3, COOH, COO asphalt C1-6, con (R5) (R6),N (R7) CO (R8)N (R9) SO2 (R10)CO (R11)(C (R12) (R13)) x-O (R14)R3, R4, R5, R6, R7, R9 independently of each other H, C1-8 alkyl; or R3 and R4, R5 and R6 form independently of each other optionally together with the nitrogen atom to which a 5-6 membered ring is attached which, apart from the nitrogen atom, can also comprise 0-1 additional heteroatoms of the NH group , N 1-8 alkyl, oxygen and sulfur; R8, R10, R11 independently of each other H, C1-8 alkyl, aryl; R12, R13 independently of each other H, C1-8 alkyl; R14 H, C1-6 alkyl, aryl; x 0, 1, 2, 3, 4, 5 or 6; R2 H, F, CI, Br, I, OH, CF3, NO2, CN, OCF3, O-C1-6 alkyl, O-C1-4 alkoxy C1-4 alkyl, S-C1-6 alkyl, C1-6 alkyl, C2-6 alkenyl, C3-8 cycloalkyl,O-cycloquino C3-8, cycloquinoo C3-8, tar c2-6, c0-8-arilo, o-coquileno c0-8-arilo, s-arilo, n (R15) (R16),So2-ch3, COOH, COO tar c1-8, con (R17) (R18),N (R19) CO (R20)N (R21) SO2 (R22)CO (R23)(C (R24) (R25)) x -O (R26)R15, R16, R17, R18, R19, R21 independently of each other H, C1-8 alkyl; or R15 and R16, R17 and R18 independently form each other and optionally together with the nitrogen atom to which a 5-6 membered ring is attached which, apart from the nitrogen atom, can also comprise 0-1 additional heteroatoms of the group of NH, N 1-6 alkyl, oxygen and sulfur; R20, R22, R23 independently of each other H, C1-8 alkyl, aryl; R24, R25 independently of each other H, C1-8 alkyl; R26 H, C1-6 alkyl, aryl; x '0, 1, 2, 3, 4, 5 or 6; And C (R27) (R27 ') C (R28) (R28'),C (R29) 3DC (R29)R27, R27 ',R28, R28 ',R29, R29 'is independent of H, F, CI, Br, CN, c1-8, alquenilo c2-6, c2-6, x s, O, C (R30) = C (R30';6, or c3-8-8-8-8-8-8-8-8, or c8-8-8-8 n (R15) (R16),So2ch3, COOH, COO asphalt C1-6, con (R17) (R18),N (R19) CO (R20)N (R21) SO2 (R22)CO (R23)(C (R24) (R25)) x -O (R26)A liaison or canning consisting of 1 to 8 members selected from the group consisting of O, s, SO2, n (R31);CO C (R32) (R33)C (R34) 3DC (R34)cyclopropylene, C? C, resulting in a chemically reasonable radical; R31, R34, R34 'independently from each other H, C1-8 alkyl; R32, R33 independently of each other H, C1-6 alkyl, OH, O-C1-6 alkyl; B H, N (R35) (R36),1. Hydroxy-c1-4 tar, c1-8 tar, Alcoy c1-4-c1-4-tar, C1-4 alquenilo C2-8, c12-8 tar, a monkey ring,Double...tri- o espiroc clico de 3 a 10 miembros que puede comprender de 0 a 4 hetero tomos seleccionados entre el grupo de oxigeno nitrogeno y azufre donde el sistema de anillos puede estar sustituido adicionalmente con uno oms de los siguientes sustituyentes F CI Br CF3 NO2 CN CON (R38) (R39)hidroxi COO (R40)N (R41) COalquilo C1-6 N (R42) (R43)SO2CH3, SCF3 or S-C1-6 alkyl; R35, R36, R37, R38, R39, R40, R41, R42, R43 independently of each other H, C1-8 alkyl; or R38 and R39, R42 and R43 form independently of each other optionally together with the nitrogen atom to which a 5-6 membered ring is attached which, apart from the nitrogen atom, can also comprise 0-1 additional heteroatoms of the NH group , N 1-6 alkyl, oxygen and sulfur; Q mono-ring structure,Double...For a saturated or partially unsaturated three ring helix, select one nitrogen atom and 0-3 additional heteroatoms from group n or group s. The rings on the structure can be helix unity, capacitance or connection, The ring system can be combined with one or more of the following alternatives: F, oh, CF3, CN, ocf3, oxo, o-tar c1-8, Alcoy c1-4-c1-4-tar, C1-6 tar, alquenilo c2-6, c12-6 tar, CO (R44),(C (R45) (R46)) or -R47, CO (C (R45) (R46)) p-R48, where Q comprises at least two atoms of N; R44 H, C1-8 alkyl; R45, R46 independently of each other H, C1-8 alkyl, OH, C3-8 cycloalkyl, C1-4 alkoxy-C1-4 alkyl; or, p independently from each other 0, 1, 2, 3, 4, 5 or 6; R47, R48 independently of each other OH, F, O-C1-8 alkyl, CON (R49) (R50),N (R51) CO (R52)N (R53) (R54)CO2 (R55)So2me, CN, a 3-10 ring system consisting of 0 to 3 heteroatoms selected from group n or group s, can be replaced by one or more of the following alternatives: F, CI, Br, CF3, c1-8 tar, c1-8 tar, alcoxi c1-4-c1-4 tar, CO (R56),oxo, OH; R49, R50, R51, R52, R55, R56 independently of each other H, C1-8 alkyl; or R49 and R50 optionally form together with the nitrogen atom to which a 5-6 membered ring is attached which, apart from the nitrogen atom, can also comprise 0-1 additional heteroatoms of the NH group, N-C1-6 alkyl , oxygen and sulfur; R53, R54 independently of each other H, C1-8 alkyl, C1-4 alkoxy-C1-4 alkyl, C3-8 alkenyl, C3-8 alkynyl, CO (R57),(C (R58) (R59)) q-R60 CO (C (R61) (R62)) r-R63 CO-O-alquilo C1-8 o R53 y R54 forman junto con el tomo de nitrogeno al que est n unidos un Double...O 4 to 10 member helical helices, in addition to nitration atoms, include 0 to 3 other heteroatoms selected from group n, O and s, and can be replaced by one or more of the following substitutes: F, CI, Br, CF3, c1-8 tar, C1-6 tar, CO (R64),Oxy, oh, alcoxi c1-4-c1-4-tar, c1-4-alkyl, with (R65) (R66),N (R67) CO (R68)N (R69) (R70)CO2 (R71)SO2-C1-6 alkyl; R58, R59 independently of each other H, C1-6 alkyl, OH; R57, R61, R62, R64, R65, R66, R67, R68, R69, R70, R71 independently of each other H, C1-6 alkyl; or R69 and R70 optionally form together with the nitrogen atom to which a 5-6 membered ring is attached which, apart from the nitrogen atom, can also comprise 0-1 additional heteroatoms of the NH group, N-C1-6 alkyl , oxygen and sulfur; q, r independently from each other 0, 1, 2, 3, 4, 5 or 6; R60, R63 independently of each other OH, F, O-C1-6 alkyl, CN, COO (R78),N (R74) COalquilo C1-6 N (R76) (R77)And (R72) (R73),So2-c1-6, a monkey ringThe helix of b1-o 3-12 members, which may include one or more N, O and s heteroatoms, and the ring of 3-12 members may include additional substitutes, such as F, CI, Br, oh, CF3, NO2, CN, ocf3, oxo, o-hc-6, alcox c1-4-tar, C1-4, C1-4 salicylic, C1-6, C1-6 tar, alquinio c2-6, Cycloquinolo C3-8, o-cycloquinolo C3-8, cycloquinolo C3-8, o-cycloquinoo C3-8, tar layer c2-6, n (R76) (r77),COO (R78)So2-c1-8y COOH; R72, R73, r74, R76, r77, R78, independent of H, c1-8, or whether R72 and R73, R76 and r77 form rings of 5-6 members together with nitrogen atoms attached together; except nitrogen atoms, It may also include additional 0-1 heteroatoms of the NH group, C1-6 normal tar, oxygen and sulfur.