| 主权项 |
1. A compound of the formula Iwhere:
X is S or SO2; R1 is
a radical of the formula Ia in which
R5 is hydrogen or (C1-C3)-alkyl;R6, R7, R8, R9, and R10are each independently hydrogen, CN, OCF3, OCHF2, O—(C1-C6)-alkyl, O—(C1-C4)-alkoxy-(C1-C4)-alkyl, S—(C1-C6)-alkyl, (C2-C4)-haloalkyl, O—(C2-C4)-haloalkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, N(R11)(R12), SO2—CH3, SO2—N(R13)(R14), SF5, SCF3, COOH, COO—(C1-C6)-alkyl, CON(R15)(R16), N(R17)CO(R18), N(R19)SO2(R20), CO(R21), (CR22R23)x-O(R24), (CR22R23)x-CO—O(R24), O—(CR22R23)x-CO—O(R24), (CR22R23)x-N(R25)(R26), O—(CR22R23)x-N(R25)(R26), (CR22R23)x-CON(R25)(R26), O—(CR22R23)x-CON(R25)(R26), O—CO—N(R25)(R26), O—CO—(C1-C6)-alkylene-CO—O—(C1-C6)-alkyl, O—CO—(C1-C6)-alkylene-CO—OH, or O—CO—(C1-C6)-alkylene-CO—N(R27)(R28);with the proviso that at least one R6, R7, R8, R9, or R10 radical is not hydrogen;x is independently 0, 1, 2, 3, 4, 5, or 6;orR7 or R8 is(O)y—(CH2—)y′—(O)y″—(CH2)y′″—R100;y and y″ are each independently 0, or 1;y′ and y′″ are each independently 1, 2, 3, 4, 5, or 6;R100 is a 4- to 10-membered mono- or bicyclic saturated, partly unsaturated or aromatic ring which may contain 1 to 4 heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the ring system may optionally be mono- or polysubstituted by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, O—(C1-C4)-alkoxy-(C1-C4)-alkyl, S—(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C4)-haloalkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, O—(C3-C8)-cycloalkyl, (C2-C6)-alkynyl, N(R29)(R30), SO2—CH3, SF5, COOH, COO—(C1-C6)-alkyl, CON(R31)(R32), N(R33)CO(R34), N(R35)SO2(R36), CO(R37), (CR38R39)x-O(R40), (CR38R39)x′-CO—O(R40), O—(CR22R23)x′-CO—O(R40), (CR22R23)x′-N(R41)(R42), O—(CR38R39)x′-N(R41)(R42), (CR38R39)x′-CON(R41)(R42), O—(CR38R39)x′-CON(R41)(R42), O—CO—N(R41)(R42), O—CO—(C1-C6)-alkylene-CO—O—(C1-C6)-alkyl, O—CO—(C1-C6)-alkylene-CO—OH, or O—CO—(C1-C6)-alkylene-CO—N(R43)(R44);x′ is 0, 1, 2, 3, 4, 5, or 6;orR7 and R8, or R8 and R9, or R9 and R10together with the carbon atom which bears them form a monocyclic, 5- to 7-membered saturated, partly unsaturated or aromatic ring system whose individual members may be optionally substituted by —CHR45-, —CR46R47-, ═(C—R46)-, O, N or S; with the proviso that no two units from the group of —O—, N and —S— may be adjacent;R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, R42, R43, and R44
are each independently hydrogen or (C1-C6)-alkyl;orR11 and R12, R13 and R14, R15 and R16, R25 and 26, R27 and R28, R29 and R30, R31 and R32, R41 and 42, R43 and 44each independently form, optionally together with the nitrogen atom to which they are bonded, a 5-6-membered ring which, apart from the nitrogen atom, may optionally include 0-1 further heteroatom from the group of NH, N—(C1-C6)-alkyl, oxygen and sulfur;R45, R46, and R47 are the same or different and are each F, Cl, Br, I, OH, CF3, NO2, CN, OCHF2, OCF3, SF5, O—(C1-C6)-alkyl, O—(C1-C4)-alkoxy-(C1-C4)-alkyl, S—(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C4)-haloalkyl, O—(C2-C4)-haloalkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, O—(C3-C8)-cycloalkyl, (C2-C6)-alkynyl, N(R134)(R135), SO2—CH3, COOH, COO—(C1-C6)-alkyl, CON(R136)(R137), N(R138)CO(R139), N(R140)SO2(R141), CO(R142), (CR143R144)x″—O(R145), (CR143R144)x″—CO—O(R145), O—(CR143R144)x″—CO—O(R145), (CR143R144)x″—N(R146)(R147), O—(CR143R144)x″—N(R146)(R147), (CR143R144)x″—CON(R146)(R147), O—(CR143R144)x″—CON(R146)(R147), O—CO—N(R146)(R147), O—CO—(C1-C6)-alkylene-CO—O—(C1-C6)-alkyl, O—CO—(C1-C6)-alkylene-CO—OH, or O—CO—(C1-C6)-alkylene-CO—N(R148)(R149);x″ is independently 1, 2, 3, 4, 5, or 6;R134, R135, R136, R137, R138, R139, R140, R141, R142, R143, R144, R145, R146, R147, R148, and R149are the same or different and are each hydrogen or (C1-C6)-alkyl; a radical of the formula Ib in whichR5 is hydrogen or (C1-C3)-alkyl;Het is a 4- to 10-membered mono- or bicyclic aromatic ring containing 1 to 4 heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the ring system may optionally be mono- or polysubstituted independently by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, OCHF2, O—(C1-C6)-alkyl, O—(C1-C4)-alkoxy-(C1-C4)-alkyl, S—(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C4)-haloalkyl, O—(C2-C4)-haloalkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, N(R48)(R49), SO2—CH3, SO2—N(R50)(R51), SF5, SCF3, COOH, COO—(C1-C6)-alkyl, CON(R52)(R53), N(R54)CO(R55), N(R56)SO2(R57), CO(R58), (CR59R60)x′″-O—(R61), (CR59R60)x′″—CO—O(R61), O—(CR59R60)x′″—CO—O(R61), (CR59R60)x′″—N(R62)(R63), O—(CR59R60)x′″—N(R62)(R63), (CR59R60)x′″—CON(R62)(R63), O—(CR59R60)x′″—CON(R62)(R63), O—CO—N(R62)(R63), O—CO—(C1-C6)-alkylene-CO—O—(C1-C6)-alkyl, O—CO—(C1-C6)-alkylene-CO—OH, or O—CO—(C1-C6)-alkylene-CO—N(R64)(R65);or (O)y—(CH2-)y′—(O)y″—(CH2)y′″—R101,x′″ is independently 1, 2, 3, 4, 5, or 6;y and y″ are each independently 0, or 1;y′ and y′″ are each independently 0, 1, 2, 3, 4, 5, or 6;R101 is a 4- to 10-membered mono- or bicyclic saturated, partly unsaturated or aromatic ring which may contain 1 to 4 heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the ring system may optionally be mono- or polysubstituted by F, Cl, Br, I, OH, CF3, NO2, CN, OCHF2, OCF3, O—(C1-C6)-alkyl, O—(C1-C4)-alkoxy-(C1-C4)-alkyl, S—(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C4)-haloalkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, O—(C3-C8)-cycloalkyl, (C2-C6)-alkynyl, N(R66)(R67), SO2—CH3, SF5, COOH, COO—(C1-C6)-alkyl, CON(R68)(R69), (C), N(R70)CO(R71), N(R72)SO2(R73), CO(R74), (CR75R76)x″″-O(R77R75R76)x″″-CO-O(R77), O—(CR75R76)x″″-CO—O(R77), (CR75R76)x″″-N(R78)(R79), O—(CR75R76)x″″-N(R78)(R79), (CR75R76)x″″-CON(R78)(R79), O—(CR75R76)x″″-CON(R78)(R79), O—CO—N(R78)(R79), O—CO—(C1-C6)-alkylene-CO—O—(C1-C6)-alkyl, O—CO—(C1-C6)-alkylene-CO—OH, or O—CO—(C1-C6)-alkylene-CO—N(R80)(R81);x″″ is independently 1, 2, 3, 4, 5, or 6;R48, R49, R50, R51, R52, R53, R54, R55, R56, R57, R58, R59, R60, R61, R62, R63, R64, R65, R66, R67, R68, R69, R70, R71, R72, R73, R74, R75, R76, R77, R78, R79, R80, and R81
are each independently hydrogen or (C1-C6)-alkyl;orR48 and R49, R50 and R51, R52 and R53, R62 and R63, R64 and R65, R66 and R67, R68 and R69, R78 and R79, R80 and R81each independently form, optionally together with the nitrogen atom to which they are bonded, a 5-6-membered ring which, apart from the nitrogen atom, may optionally include 0-1 further heteroatom from the group of NH, N—(C1-C6)-alkyl, oxygen and sulfur; a radical of the formula Ic in which
W is —C(R126)(R127)-, —C(R126)(R127)-C(R128)(R129)-, or —C(R126)(R127)-O—;R120, R121, R123, R125, R126, R127, R128, and R129
are the same or different and are each hydrogen, F, Cl, Br, I, OH, CF3, NO2, CN, OCHF2, OCF3, SF5, O—(C1-C6)-alkyl, O—(C1-C4)-alkoxy-(C1-C4)-alkyl, S—(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C4)-haloalkyl, O—(C2-C4)-haloalkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkenyl, (C2-C6)-alkynyl, N(R90)(R91), SO2—CH3, COOH, COO—(C1-C6)-alkyl, CON(R92)(R93), N(R94)CO(R95), N(R96)SO2(R97), CO(R98), (CR99R102)z-O(R103), (CR99R76)zCO—O(R103), O—(CR99R102)z-CO—O(R103), (CR99R102)z-N(R104)(R105), O—(CR99R102)z-N(R104)(R105), (CR99R102)z-CON(R104)(R105), O—(CR99R102)z-CON(R104)(R105), O—CO—N(R104)(R105), O—CO—(C1-C6)-alkylene-CO—O—(C1-C6)-alkyl, O—CO—(C1-C6)-alkylene-CO—OH, or O—CO—(C1-C6)-alkylene-CO—N(R106)(R107);z is independently 1, 2, 3, 4, 5, or 6;R90, R91, R92, R93, R94, R95, R96, R97, R98, R99, R102, R103, R104, R105, R106, and R107
are the same or different and are each hydrogen or (C1-C6)-alkyl;R122 and R124, together with the carbon atom which bears them form a monocyclic, 5- or 6-membered saturated, partly unsaturated or aromatic ring system whose individual members may be optionally substituted by —CHR130-, —CR131R132-, or ═(C—R133)-;R130, R131, R132, and R133 are the same or different and are each F, Cl, Br, I, OH, CF3, NO2, CN, OCHF2, OCF3, SF5, O—(C1-C6)-alkyl, O—(C1-C4)-alkoxy-(C1-C4)-alkyl, S—(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C4)-haloalkyl, O—(C2-C4)-haloalkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, N(R160)(R161), SO2—CH3, COOH, COO—(C1-C6)-alkyl, CON(R162)(R163), N(R164)CO(R165), N(R166)SO2(R167), CO(R168), (CR169R170)z′-O(R171), (CR169R170)z′-CO—O(R77), O—(CR169R170)z′-CO—O(R171), (CR169R170)z′-N(R172)(R173), O—(CR169R170)z′-N(R172)(R173), (CR169R170)z′-CON(R172)(R173), O—(CR169R170)z′-CON(R172)(R173), O—CO—N(R172)(R173), O—CO—(C1-C6)-alkylene-CO—O—(C1-C6)-alkyl, O—CO—(C1-C6)-alkylene-CO—OH, or O—CO—(C1-C6)-alkylene-CO—N(R172)(R173);
z′ is independently 1, 2, 3, 4, 5, or 6;R160, R161, R162, R163, R164, R165, R166, R167, R168, R169, R170, R171, R172, and R173
are the same or different and are each hydrogen or (C1-C6)-alkyl; or
R160 and R161, R162 and R163, R172 and R173 each independently form, optionally together with the nitrogen atom to which they are bonded, a 5-6-membered ring which, apart from the nitrogen atom, may optionally include 0-1 further heteroatom from the group of NH, N—(C1-C6)-alkyl, oxygen and sulfur; R2, R3, and R4 are the same or different and are each hydrogen, F, Cl, Br, I, OH, CF3, NO2, CN, OCHF2, OCF3, SF5, O—(C1-C6)-alkyl, O—(C1-C4)-alkoxy-(C1-C4)-alkyl, S—(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C4)-haloalkyl, O—(C2-C4)-haloalkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, O—(C3-C8)-cycloalkyl, (C3-C8)-cycloalkenyl, aryl, (C2-C6)-alkynyl, N(R200)(R201), SO2—CH3, COOH, COO—(C1-C6)-alkyl, CON(R202)(R203), N(R204)CO(R205), N(R206)SO2(R207), CO(R208), (CR209R210)z″-O(R211), (CR209R210)z″-CO—O(R211), O—(CR209R210)z″-CO—O(R211), (CR209R210)z″-N(R212)(R213), O—(CR209R210)z″-N(R212)(R213), (CR209R210)z″-CON(R212)(R213), O—(CR209R210)z″-CON(R212)(R213), O—CO—N(R212)(R213), O—CO—(C1-C6)-alkylene-CO—O—(C1-C6)-alkyl, O—CO—(C1-C6)-alkylene-CO—OH, or O—CO—(C1-C6)-alkylene-CO—N(R212)(R213); z″ is independently 1, 2, 3, 4, 5, or 6; R200, R201, R202, R203, R204R205, R206, R207, R208, R209, R210, R211, R212, and R213
are the same or different and are each hydrogen or (C1-C6)-alkyl; or R200 and R201, R202 and R203, R212 and R213
each independently form, optionally together with the nitrogen atom to which they are bonded, a 5-6-membered ring which, apart from the nitrogen atom, may optionally include 0-1 further heteroatom from the group of NH, N—(C1-C6)-alkyl, oxygen and sulfur; the tautomeric forms of the compound and the physiologically compatible salts and N-oxides thereof. |
