RU2005128551A - SUBSTITUTED N-ARILGETEROCYCLES, METHOD FOR PRODUCING THEM AND THEIR APPLICATION AS MEDICINES - Google Patents

SUBSTITUTED N-ARILGETEROCYCLES, METHOD FOR PRODUCING THEM AND THEIR APPLICATION AS MEDICINES Download PDF

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RU2005128551A
RU2005128551A RU2005128551/04A RU2005128551A RU2005128551A RU 2005128551 A RU2005128551 A RU 2005128551A RU 2005128551/04 A RU2005128551/04 A RU 2005128551/04A RU 2005128551 A RU2005128551 A RU 2005128551A RU 2005128551 A RU2005128551 A RU 2005128551A
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alkyl
independently
another
contain
nitrogen atom
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Лотар ШВИНК (DE)
Лотар ШВИНК
Зигфрид ШТЕНГЕЛИН (DE)
Зигфрид ШТЕНГЕЛИН
Маттиас ГОССЕЛЬ (DE)
Маттиас Госсель
Томас БЕМЕ (DE)
Томас Беме
Герхард ХЕССЛЕР (DE)
Герхард ХЕССЛЕР
Петра ШТАЛЬ (DE)
Петра Шталь
Дирк ГРЕТЦКЕ (DE)
Дирк Гретцке
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Санофи-Авентис Дойчланд Гмбх (De)
Санофи-Авентис Дойчланд Гмбх
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Claims (17)

1. Соединение формулы (I)1. The compound of formula (I)
Figure 00000001
Figure 00000001
 где R1, R2, независимо друг от друга, представляют собой H, (C1-C8)алкил, -(CR78R79)o-R12, (C1-C4)алкокси-(C1-C4)алкил, (C3-C8)алкенил, CO-(C1-C8)алкил, -CO-(CH2)o-R12, CO-арилокси-(C1-C4)алкил, COCH=CH(R13), COCC(R14), CO(C(R15)(R16))qN(R17)(R18), CO(C(R19)(R20))rCON(R21)(R22), CO(C(R23)(R24))sO(R25); или R1 и R2 образуют вместе с атомом азота, с которым они связаны, 4-10-членное моно-, би- или спироциклическое кольцо, которое, помимо атома азота, может содержать 0-2 дополнительных гетероатома, выбранных из группы, включающей кислород, азот и серу, где гетероциклическая кольцевая система может быть дополнительно замещена F, Cl, Br, CF3, (C1-C6)алкилом, O-(C1-C4)алкилом, (C1-C4)алкокси-(C1-C4)алкилом, гидрокси-(C1-C4)алкилом, (C0-C2)алкиленарилом, оксо, CO(R26), CON(R27)(R28), гидрокси, COO(R29), N(R30)CO(C1-C6)алкилом, N(R31)(R32) или SO2CH3;where R1, R2, independently of one another, are H, (C 1 -C 8 ) alkyl, - (CR78R79) o -R12, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, ( C 3 -C 8 ) alkenyl, CO- (C 1 -C 8 ) alkyl, -CO- (CH 2 ) o -R12, CO-aryloxy- (C 1 -C 4 ) alkyl, COCH = CH (R13), COCC (R14), CO (C (R15) (R16)) q N (R17) (R18), CO (C (R19) (R20)) r CON (R21) (R22), CO (C (R23) ( R24)) s O (R25); or R1 and R2 form, together with the nitrogen atom to which they are attached, a 4-10 membered mono-, bi- or spirocyclic ring, which, in addition to the nitrogen atom, may contain 0-2 additional heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur, where the heterocyclic ring system may be further substituted with F, Cl, Br, CF 3 , (C 1 -C 6 ) alkyl, O- (C 1 -C 4 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, hydroxy- (C 1 -C 4 ) alkyl, (C 0 -C 2 ) alkylene aryl, oxo, CO (R26), CON (R27) (R28), hydroxy, COO (R29) , N (R30) CO (C 1 -C 6 ) alkyl, N (R31) (R32) or SO 2 CH 3 ; o имеет значение 0, 1, 2, 3, 4, 5, 6;o has the value 0, 1, 2, 3, 4, 5, 6; q, r, независимо друг от друга, имеют значение 1, 2, 3;q, r, independently of each other, have a value of 1, 2, 3; s имеет значение 0, 1, 2, 3, 4;s is 0, 1, 2, 3, 4; R13, R14, независимо друг от друга, представляют собой другое фенильное кольцо, которое может содержать 0-1 атом азота;R13, R14, independently of each other, represent another phenyl ring, which may contain 0-1 nitrogen atom; R15, R16, R17, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R31, R32, независимо друг от друга, представляют собой H, (C1-C6)алкил;R15, R16, R17, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R31, R32, independently of each other, are H, (C 1 -C 6 ) alkyl; R18 представляет собой H, (C1-C6)алкил, CO(R33); илиR18 represents H, (C 1 -C 6 ) alkyl, CO (R33); or R17 и R18, R21 и R22, R27 и R28, R31 и R32, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу;R17 and R18, R21 and R22, R27 and R28, R31 and R32, independently of each other, optionally together with the nitrogen atom to which they are bonded, form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0 -1 additional heteroatom selected from the group consisting of N- (C 1 -C 6) -alkyl, oxygen and sulfur; R33 представляет собой 5-10-членную ароматическую кольцевую систему, которая может содержать дополнительный гетероатом, выбранный из группы, включающей азот, кислород и серу, и может быть замещена F, Cl, (C1-C6)алкилом, O-(C1-C8)алкилом;R33 is a 5-10 membered aromatic ring system that may contain an additional heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, and may be substituted with F, Cl, (C 1 -C 6 ) alkyl, O- (C 1 -C 8 ) alkyl; R12 представляет собой OH, O-(C1-C6)алкил, O(C0-C8)алкиленарил, CN, S-(C1-C6)алкил, COO(R80), CON(R81)(R82), 3-12-членное моно-, би- или спироциклическое кольцо, которое может содержать один или несколько гетероатомов, выбранных из группы, включающей N, O и S, и указанное 3-12-членное кольцо может содержать дополнительные заместители, такие как F, Cl, Br, OH, CF3, CN, оксо, O-(C1-C6)алкил, (C1-C4)алкокси-(C1-C4)алкил, (C1-C6)алкил, O-(C0-C8)алкиленарил, (C0-C8)алкиленарил, N(R34)(R35), COCH=CH(R36), (C(R37)(R38))t(R39), CO(C(R37)(R38))t(R39), CO(C1-C6)алкил, COCOO(C1-C6)алкил, COO(R40), S(O)u(R41);R12 is OH, O- (C 1 -C 6 ) alkyl, O (C 0 -C 8 ) alkylenearyl, CN, S- (C 1 -C 6 ) alkyl, COO (R80), CON (R81) (R82 ), A 3-12 membered mono-, bi- or spirocyclic ring, which may contain one or more heteroatoms selected from the group consisting of N, O and S, and said 3-12-membered ring may contain additional substituents, such as F, Cl, Br, OH, CF 3 , CN, oxo, O- (C 1 -C 6 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, (C 1 -C 6 ) alkyl, O- (C 0 -C 8) alkylene-, (C 0 -C 8) alkylene-, N (R34) (R35) , COCH = CH (R36), (C (R37) (R38)) t (R39 ), CO (C (R37) (R38)) t (R39), CO (C 1 -C 6 ) alkyl, COCOO (C 1 -C 6 ) alkyl, COO (R40), S (O) u (R41) ; t имеет значение 0, 1, 2, 3, 4, 5, 6;t is 0, 1, 2, 3, 4, 5, 6; u имеет значение 0, 1, 2;u has the value 0, 1, 2; R34, R35, R37, R38, независимо друг от друга, представляют собой H, (C1-C8)алкил; илиR34, R35, R37, R38, independently of one another, are H, (C 1 -C 8 ) alkyl; or R34 и R35, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6 членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу, и может необязательно быть замещенным 1-2 оксогруппами;R34 and R35, optionally together with the nitrogen atom to which they are attached, form a 5-6 membered ring, which, in addition to the nitrogen atom, can also contain 0-1 additional heteroatoms selected from the group consisting of N- (C 1 -C 6 ) alkyl, oxygen and sulfur, and may optionally be substituted with 1-2 oxo groups; R36, R39, независимо друг от друга, представляют собой (C3-C8)циклоалкил, 5-10-членную ароматическую кольцевую систему, которая может содержать 0-2 дополнительных гетероатома, выбранных из группы, включающей азот, кислород и серу, и может быть замещена F, Cl, (C1-C6)алкилом, O-(C1-C8)алкилом;R36, R39, independently of each other, are (C 3 -C 8 ) cycloalkyl, a 5-10 membered aromatic ring system that may contain 0-2 additional heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and may be substituted with F, Cl, (C 1 -C 6) alkyl, O- (C 1 -C 8) alkyl; R40 представляет собой H, (C1-C8)алкил, (C2-C6)алкенил, (C0-C8)алкиленарил;R40 represents H, (C 1 -C 8 ) alkyl, (C 2 -C 6 ) alkenyl, (C 0 -C 8 ) alkylenearyl; R41 представляет собой (C1-C6)алкил, 5-10-членную ароматическую кольцевую систему, которая может содержать 0-2 дополнительных гетероатома, выбранных из группы, включающей азот, кислород и серу, и может быть замещена F, Cl, (C1-C6)алкилом, O-(C1-C8)алкилом;R41 represents a (C 1 -C 6) -alkyl, 5-10 membered aromatic ring system which may contain 0-2 additional heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and may be substituted with F, Cl, ( C 1 -C 6 ) alkyl; O- (C 1 -C 8 ) alkyl; R78, R79, независимо друг от друга, представляют собой H, (C1-C8)алкил, гидрокси-(C1-C4)алкил, OH, (C1-C4)алкокси-(C1-C4)алкил;R78, R79, independently of one another, are H, (C 1 -C 8 ) alkyl, hydroxy- (C 1 -C 4 ) alkyl, OH, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl; R80, R81, независимо друг от друга, представляют собой H, (C1-C8)алкил;R80, R81, independently of one another, are H, (C 1 -C 8 ) alkyl; R3 представляет собой H, (C1-C6)алкил;R3 is H, (C 1 -C 6 ) alkyl; R4, R5, независимо друг от друга, представляют собой H, (C1-C6)алкил, OH, O-(C1-C6)алкил, O-CO(C1-C6)алкил, S-(C1-C6)алкил;R4, R5, independently of one another, are H, (C 1 -C 6 ) alkyl, OH, O- (C 1 -C 6 ) alkyl, O-CO (C 1 -C 6 ) alkyl, S- ( C 1 -C 6 ) alkyl; R6, R7, R8, R9 представляют собой H; илиR6, R7, R8, R9 are H; or R6 и R7, R8 и R9, независимо друг от друга, необязательно, представляют собой оксо;R6 and R7, R8 and R9, independently of one another, are optionally oxo; n имеет значение 1;n is 1; m имеет значение 1;m is 1; A, B, D, G, независимо друг от друга, представляет собой N, C(R42); илиA, B, D, G, independently of each other, represents N, C (R42); or группы A и B или группы D и G, каждая, представляет собой C(R42) и вместе образуют ортофениленовое звено, в целом образуя 1,4-бизамещенную нафталиновую систему;groups A and B or groups D and G each represent C (R42) and together form an orthophenylene unit, generally forming a 1,4-bisubstituted naphthalene system; R42 представляет собой H, F, Cl, Br, CF3, CN, O-(C1-C6)алкил, O-(C1-C4)алкокси-(C1-C4)алкил, S-(C1-C6)алкил, (C1-C6)алкил, (С0-С8)алкиленарил, O-(C0-C8)алкиленарил, N(R43)(R44), SO2-CH3, CON(R45)(R46), N(R47)CO(R48), CO(R51), -(CR84R85)x-O(R86);R42 represents H, F, Cl, Br, CF 3 , CN, O- (C 1 -C 6 ) alkyl, O- (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, S- ( C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkyl, (C 0 -C 8 ) alkylene aryl, O- (C 0 -C 8 ) alkylene aryl, N (R43) (R44), SO 2 -CH 3 , CON (R45) (R46), N (R47) CO (R48), CO (R51), - (CR84R85) x- O (R86); R43, R44, R45, R46, R47, независимо друг от друга, представляют собой H, (C1-C8)алкил; илиR43, R44, R45, R46, R47, independently of one another, are H, (C 1 -C 8 ) alkyl; or R43 и R44, R45 и R46, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу;R43 and R44, R45 and R46, independently of each other, optionally together with the nitrogen atom to which they are bonded, form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0-1 additional heteroatoms selected from the group including N- (C 1 -C 6 ) alkyl, oxygen and sulfur; R48, R50, R51, независимо друг от друга, представляют собой H, (C1-C8)алкил, арил;R48, R50, R51, independently of one another, are H, (C 1 -C 8 ) alkyl, aryl; R84, R85 представляют собой H;R84, R85 are H; R86 представляет собой H, (C1-C6)алкил;R86 is H, (C 1 -C 6 ) alkyl; x имеет значение 0, 1, 2;x has the value 0, 1, 2; R10 представляет собой H, (C1-C8)алкил;R10 represents H, (C 1 -C 8 ) alkyl; X представляет собой N(R52), связь, C=C, C(R53)(R54), СН2-СН2;X represents N (R52), a bond, C = C, C (R53) (R54), CH 2 —CH 2 ; Y представляет собой O, S, N(R89);Y represents O, S, N (R89); R89 представляет собой H, (C1-C8)алкил;R89 represents H, (C 1 -C 8 ) alkyl; R52, R53, R54, независимо друг от друга, представляют собой H, (C1-C8)алкил;R52, R53, R54, independently of one another, are H, (C 1 -C 8 ) alkyl; E выбран из группы, включающейE is selected from the group including
Figure 00000002
Figure 00000002
Figure 00000003
Figure 00000003
 которые могут необязательно содержать заместители, выбранные из группы, включающей H, F, Cl, Br, OH, CF3, NO2, OCF3, O-(C1-C6)алкил, (C1-C6)алкил, (C2-C6)алкенил, N(R57)(R58), SO2-CH3, CO(R65);which can optionally contain substituents selected from the group consisting of H, F, Cl, Br, OH, CF 3, NO 2, OCF 3, O- (C 1 -C 6) alkyl, (C 1 -C 6) alkyl, (C 2 -C 6 ) alkenyl, N (R57) (R58), SO 2 -CH 3 , CO (R65); R57, R58, независимо друг от друга, представляют собой H, (C1-C8)алкил;R57, R58, independently of one another, are H, (C 1 -C 8 ) alkyl; R65, независимо друг от друга, представляют собой H, (C1-C8)алкил, арил;R65, independently of one another, are H, (C 1 -C 8 ) alkyl, aryl; K представляет собой связь, O, OCH2, CH2O, S, SO, SO2, N(R66), N(R67)CO, CON(R68), (C(R69)(R70))v, CO, C=C, C≡C, SCH2, SO2CH2;K is a bond, O, OCH 2, CH 2 O, S, SO, SO 2, N (R66), N ( R67) CO, CON (R68), (C (R69) (R70)) v, CO, C = C, C≡C, SCH 2 , SO 2 CH 2 ; v имеет значение 1, 2, 3, 4v is 1, 2, 3, 4 R66, R67, R68, R69, R70, независимо друг от друга, представляют собой H, (C1-C8)алкил;R66, R67, R68, R69, R70, independently of one another, are H, (C 1 -C 8 ) alkyl; R11 представляет собой H, (C1-C8)алкил, (C1-C4)алкокси-(C1-C4)алкил, (C3-C8)алкенил, (C3-C8)алкинил, 3-10-членное моно-, би-, три- или спироциклическое кольцо, которое может содержать 0-4 гетероатома, выбранных из группы, включающей кислород, азот и серу, где указанная кольцевая система может быть дополнительно замещена F, Cl, Br, CF3, CN, (C1-C6)алкилом, O-(C1-C8)алкилом, (C1-C4)алкокси-(C1-C4)алкилом, гидрокси-(С1-С4)алкилом, -(C0-C8)алкиленарилом, оксо, CO(R71), CON(R72)(R73), гидрокси, COO(R74), N(R75)CO(C1-C6)алкилом, N(R76)(R77) или SO2CH3;R11 represents H, (C 1 -C 8 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, (C 3 -C 8 ) alkenyl, (C 3 -C 8 ) alkynyl, 3-10 membered mono-, bi-, tri- or spirocyclic ring, which may contain 0-4 heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur, where this ring system may be further substituted by F, Cl, Br, CF 3 , CN, (C 1 -C 6 ) alkyl, O- (C 1 -C 8 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, hydroxy- (C 1 -C 4 ) alkyl, - (C 0 -C 8 ) alkylene aryl, oxo, CO (R71), CON (R72) (R73), hydroxy, COO (R74), N (R75) CO (C 1 -C 6 ) alkyl, N (R76) (R77) or SO 2 CH 3 ; R71, R72, R73, R74, R75, R76, R77, независимо друг от друга, представляют собой H, (C1-C8)алкил; илиR71, R72, R73, R74, R75, R76, R77, independently of one another, are H, (C 1 -C 8 ) alkyl; or R72 и R73, R76 и R77, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу, илиR72 and R73, R76 and R77, independently of each other, optionally together with the nitrogen atom to which they are bonded, form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0-1 additional heteroatoms selected from the group consisting of N- (C 1 -C 6) -alkyl, oxygen and sulfur, or их N-оксиды и физиологически приемлемые соли.their N-oxides and physiologically acceptable salts. 2. Соединение формулы (I) по п.1,2. The compound of formula (I) according to claim 1, где R1, R2, независимо друг от друга, представляют собой H, (C1-C8)алкил, -(CR78R79)o-R12, (C1-C4)алкокси-(C1-C4)алкил, CO-(C1-C8)алкил, -CO-(CH2)o-R12, COCH=CH(R13), COCC(R14), CO(C(R15)(R16))qN(R17)(R18), CO(C(R23)(R24))sO(R25); или R1 и R2 образуют вместе с атомом азота, с которым они связаны, 4-10-членное моно- или бициклическое кольцо, которое, помимо атома азота, может содержать 0-2 дополнительных гетероатома, выбранных из группы, включающей кислород, азот и серу, где гетероциклическая кольцевая система может быть дополнительно замещена F, Cl, CF3, (C1-C6)алкилом, O-(C1-C4)алкилом, (C1-C4)алкокси-(C1-C4)алкилом, (C0-C2)алкиленарилом, оксо, CO(R26), гидрокси, N(R31)(R32) или SO2CH3;wherein R1, R2, independently, represent H, (C 1 -C 8) -alkyl, - (CR78R79) o -R12, (C 1 -C 4) alkoxy- (C 1 -C 4) alkyl, CO - (C 1 -C 8 ) alkyl, -CO- (CH 2 ) o -R12, COCH = CH (R13), COCC (R14), CO (C (R15) (R16)) q N (R17) (R18 ), CO (C (R23) (R24)) s O (R25); or R1 and R2 form, together with the nitrogen atom to which they are attached, a 4-10 membered mono- or bicyclic ring, which, in addition to the nitrogen atom, may contain 0-2 additional heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur where the heterocyclic ring system may be further substituted with F, Cl, CF 3 , (C 1 -C 6 ) alkyl, O- (C 1 -C 4 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, (C 0 -C 2 ) alkylene aryl, oxo, CO (R26), hydroxy, N (R31) (R32) or SO 2 CH 3 ; o имеет значение 0, 1, 2, 3, 4;o has the value 0, 1, 2, 3, 4; q имеет значение 1 или 2;q is 1 or 2; s имеет значение 0, 1, 2, 3;s is 0, 1, 2, 3; R13, R14, независимо друг от друга, представляют собой другое фенильное кольцо, которое может содержать 0-1 атом азота;R13, R14, independently of each other, represent another phenyl ring, which may contain 0-1 nitrogen atom; R15, R16, R17, R23, R24, R26, R31, R32, независимо друг от друга, представляют собой H, (C1-C6)алкил;R15, R16, R17, R23, R24, R26, R31, R32, independently of one another, are H, (C 1 -C 6 ) alkyl; R18 представляет собой H, (C1-C6)алкил, CO(C1-C6)алкил; илиR18 represents H, (C 1 -C 6 ) alkyl, CO (C 1 -C 6 ) alkyl; or R17 и R18, R31 и R32, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, выбранное из пирролидина, пиперидина, N-метилпиперазина, морфолина;R17 and R18, R31 and R32, independently of each other, optionally together with the nitrogen atom to which they are attached, form a 5-6 membered ring selected from pyrrolidine, piperidine, N-methylpiperazine, morpholine; R12 представляет собой OH, O-(C1-C6)алкил, O(C0-C8)алкиленарил, CN, 3-10-членное моно- или бициклическое кольцо, которое может содержать 1-3 гетероатома, выбранных из группы, включающей N, O и S, и указанное 3-10 членное кольцо может содержать дополнительные заместители, такие как F, Cl, Br, OH, CF3, CN, оксо, O-(C1-C6)алкил, (C1-C4)алкокси-(C1-C4)алкил, (C1-C6)алкил, (C0-C2)алкиленарил, N(R34)(R35), CO(C1-C6)алкил;R12 represents OH, O- (C 1 -C 6 ) alkyl, O (C 0 -C 8 ) alkylenearyl, CN, a 3-10 membered mono- or bicyclic ring, which may contain 1-3 heteroatoms selected from the group including N, O and S, and the specified 3-10 membered ring may contain additional substituents, such as F, Cl, Br, OH, CF 3 , CN, oxo, O- (C 1 -C 6 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, (C 1 -C 6 ) alkyl, (C 0 -C 2 ) alkylene aryl, N (R34) (R35), CO (C 1 -C 6 ) alkyl; t имеет значение 0, 1, 2, 3, 4, 5, 6;t is 0, 1, 2, 3, 4, 5, 6; u имеет значение 0 или 2;u has a value of 0 or 2; R34, R35, независимо друг от друга, представляют собой H, (C1-C8)алкил; илиR34, R35, independently of one another, are H, (C 1 -C 8 ) alkyl; or R34 и R35, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу, и может быть замещенным 1-2 оксогруппами;R34 and R35, optionally together with the nitrogen atom to which they are attached, form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0-1 additional heteroatoms selected from the group consisting of N- (C 1 -C 6 ) alkyl, oxygen and sulfur, and may be substituted with 1-2 oxo groups; R78, R79, независимо друг от друга, представляют собой H, (C1-C8)алкил, гидрокси-(C1-C4)алкил, OH, (C1-C4)алкокси-(C1-C4)алкил;R78, R79, independently of one another, are H, (C 1 -C 8 ) alkyl, hydroxy- (C 1 -C 4 ) alkyl, OH, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl; R3 представляет собой H;R3 represents H; R4, R5, независимо друг от друга, представляют собой H, (C1-C6)алкил, OH, O-(C1-C6)алкил, O-CO(C1-C6)алкил;R4, R5, independently of one another, are H, (C 1 -C 6 ) alkyl, OH, O- (C 1 -C 6 ) alkyl, O-CO (C 1 -C 6 ) alkyl; R6, R7, R8, R9 представляют собой H;R6, R7, R8, R9 are H; n имеет значение 1;n is 1; m имеет значение 1;m is 1; A, B, D, G: В представляет собой N, C(R42); и A, D, G представляют собой C(R42);A, B, D, G: B represents N, C (R42); and A, D, G are C (R42); R42 представляет собой H, F, Cl, Br, CF3, CN, O-(C1-C6)алкил, (C1-C6)алкил, SO2-CH3, CON(R45)(R46), N(R47)CO(R48), CO(R51), -(CR84R85)x-O(R86);R42 is H, F, Cl, Br, CF 3 , CN, O- (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkyl, SO 2 -CH 3 , CON (R45) (R46), N (R47) CO (R48) , CO (R51), - (CR84R85) x -O (R86); R45, R46, R47, независимо друг от друга, представляют собой H, (C1-C8)алкил; илиR45, R46, R47, independently of one another, are H, (C 1 -C 8 ) alkyl; or R45 и R46, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу;R45 and R46, independently of each other, optionally together with the nitrogen atom to which they are bonded, form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0-1 additional heteroatoms selected from the group consisting of N- (C 1 -C 6 ) alkyl, oxygen and sulfur; R48, R51, независимо друг от друга, представляют собой H, (C1-C8)алкил;R48, R51, independently of one another, are H, (C 1 -C 8 ) alkyl; R84, R85 представляют собой H;R84, R85 are H; R86 представляет собой H, (C1-C6)алкил;R86 is H, (C 1 -C 6 ) alkyl; x имеет значение 0, 1;x has the value 0, 1; R10 представляет собой H, (C1-C8)алкил;R10 represents H, (C 1 -C 8 ) alkyl; X представляет собой N(R52), связь, C=C, C(R53)(R54), СН2-СН2;X represents N (R52), a bond, C = C, C (R53) (R54), CH 2 —CH 2 ; R52, R53, R54, независимо друг от друга, представляют собой H, (C1-C8)алкил;R52, R53, R54, independently of one another, are H, (C 1 -C 8 ) alkyl; E выбран из группы, включающейE is selected from the group including
Figure 00000004
Figure 00000004
 которые могут необязательно содержать заместители, выбранные из группы, включающей H, F, Cl, Br, OH, CF3, NO2, OCF3, O-(C1-C6)алкил, (C1-C6)алкил, (C2-C6)алкенил, N(R57)(R58), SO2-CH3, CO(R65);which may optionally contain substituents selected from the group consisting of H, F, Cl, Br, OH, CF 3 , NO 2 , OCF 3 , O- (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkyl, (C 2 -C 6 ) alkenyl, N (R57) (R58), SO 2 -CH 3 , CO (R65); R57, R58, независимо друг от друга, представляют собой H, (C1-C8)алкил;R57, R58, independently of one another, are H, (C 1 -C 8 ) alkyl; R65, независимо друг от друга, представляют собой H, (C1-C8)алкил;R65, independently of one another, are H, (C 1 -C 8 ) alkyl; K представляет собой связь, O, OCH2, CH2O, N(R66), CON(R68), (C(R69)(R70))v, CO, C≡C, SCH2;K represents a bond, O, OCH 2 , CH 2 O, N (R66), CON (R68), (C (R69) (R70)) v , CO, C≡C, SCH 2 ; v имеет значение 1, 2, 3;v has a value of 1, 2, 3; R66, R68, R69, R70, независимо друг от друга, представляют собой H, (C1-C8)алкил;R66, R68, R69, R70, independently of one another, are H, (C 1 -C 8 ) alkyl; R11 представляет собой (C1-C8)алкил, (C1-C4)алкокси-(C1-C4)алкил, 3-10-членное моно-, би-, три- или спироциклическое кольцо, которое может содержать 0-3 гетероатома, выбранных из группы, включающей кислород, азот и серу, где указанная кольцевая система может быть дополнительно замещена F, Cl, Br, CF3, CN, (C1-C6)алкилом, O-(C1-C8)алкилом, -(C0-C2)алкиленарилом, оксо, CO(R71), CON(R72)(R73), гидрокси, N(R75)CO(C1-C6)алкилом, N(R76)(R77) или SO2CH3;R11 is a (C 1 -C 8 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, 3-10 membered mono-, bi-, tri- or spirocyclic ring, which may contain 0-3 heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur, wherein said ring system may be further substituted with F, Cl, Br, CF 3 , CN, (C 1 -C 6 ) alkyl, O- (C 1 - C 8 ) alkyl, - (C 0 -C 2 ) alkylene aryl, oxo, CO (R71), CON (R72) (R73), hydroxy, N (R75) CO (C 1 -C 6 ) alkyl, N (R76) (R77) or SO 2 CH 3 ; R71, R72, R73, R75, R76, R77, независимо друг от друга, представляют собой H, (C1-C8)алкил; илиR71, R72, R73, R75, R76, R77, independently of one another, are H, (C 1 -C 8 ) alkyl; or R72 и R73, R76 и R77, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу; илиR72 and R73, R76 and R77, independently of each other, optionally together with the nitrogen atom to which they are bonded, form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0-1 additional heteroatoms selected from the group including N- (C 1 -C 6 ) alkyl, oxygen and sulfur; or их N-оксиды и физиологически приемлемые соли.their N-oxides and physiologically acceptable salts. 3. Соединение формулы (I) по п.1,3. The compound of formula (I) according to claim 1, где R1, R2, независимо друг от друга, представляют собой H, (C1-C8)алкил, -(CR78R79)o-R12, (C1-C4)алкокси-(C1-C4)алкил, CO-(C1-C8)алкил, -CO-(CH2)o-R12, O(C(R15)(R16))qN(R17)(R18); или R1 и R2 образуют вместе с атомом азота, с которым они связаны, 4-10-членное моно- или бициклическое кольцо, которое, помимо атома азота, может содержать 0-2 дополнительных гетероатома, выбранных из группы, включающей кислород и азот, где гетероциклическая кольцевая система может быть дополнительно замещена F, (C1-C6)алкилом, (C1-C4)алкокси-(C1-C4)алкилом, оксо, CO(R26), гидрокси, N(R31)(R32);where R1, R2, independently of one another, are H, (C 1 -C 8 ) alkyl, - (CR78R79) o -R12, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, CO - (C 1 -C 8 ) alkyl, -CO- (CH 2 ) o -R12, O (C (R15) (R16)) q N (R17) (R18); or R1 and R2 form, together with the nitrogen atom to which they are bonded, a 4-10 membered mono- or bicyclic ring, which, in addition to the nitrogen atom, may contain 0-2 additional heteroatoms selected from the group consisting of oxygen and nitrogen, where the heterocyclic ring system may be further substituted with F, (C 1 -C 6 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, oxo, CO (R26), hydroxy, N (R31) ( R32); o имеет значение 0, 1, 2, 3;o has a value of 0, 1, 2, 3; q имеет значение 1 или 2;q is 1 or 2; R15, R16, R17, R26, R31, R32, независимо друг от друга, представляют собой H, (C1-C6)алкил;R15, R16, R17, R26, R31, R32, independently of one another, are H, (C 1 -C 6 ) alkyl; R18 представляет собой H, (C1-C6)алкил; илиR18 represents H, (C 1 -C 6 ) alkyl; or R17 и R18, R21 и R22, R27 и R28, R31 и R32, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, выбранное из пирролидина, пиперидина, N-метилпиперазина, морфолина;R17 and R18, R21 and R22, R27 and R28, R31 and R32, independently of each other, optionally together with the nitrogen atom to which they are attached, form a 5-6 membered ring selected from pyrrolidine, piperidine, N-methylpiperazine, morpholine; R12 представляет собой OH, O-(C1-C6)алкил, 3-10-членное моно- или бициклическое кольцо, которое может содержать 1-2 гетероатома, выбранных из группы, включающей N, O и S, и указанное 3-10-членное кольцо может содержать дополнительные заместители, такие как F, OH, оксо, (C1-C6)алкил, CO(C1-C6)алкил,;R12 represents OH, O- (C 1 -C 6 ) alkyl, a 3-10 membered mono- or bicyclic ring, which may contain 1-2 heteroatoms selected from the group consisting of N, O and S, and said 3- The 10 membered ring may contain additional substituents, such as F, OH, oxo, (C 1 -C 6 ) alkyl, CO (C 1 -C 6 ) alkyl ,; R78, R79, независимо друг от друга, представляют собой H, (C1-C8)алкил, гидрокси-(C1-C4)алкил, OH, (C1-C4)алкокси-(C1-C4)алкил;R78, R79, independently of one another, are H, (C 1 -C 8 ) alkyl, hydroxy- (C 1 -C 4 ) alkyl, OH, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl; R3 представляет собой H;R3 represents H; R4, R5, независимо друг от друга, представляют собой H, OH, O-(C1-C6)алкил;R4, R5, independently of one another, are H, OH, O- (C 1 -C 6 ) alkyl; R6, R7, R8, R9, представляют собой H;R6, R7, R8, R9 are H; n имеет значение 1;n is 1; m имеет значение 1;m is 1; A, B, D, G представляют собой C(R42);A, B, D, G are C (R42); R42 представляет собой H, F, Cl, CF3, CN, (C1-C6)алкил, -(CR84R85)x-O(R86);R42 represents H, F, Cl, CF 3 , CN, (C 1 -C 6 ) alkyl, - (CR84R85) x —O (R86); R84, R85 представляют собой H;R84, R85 are H; R86 представляет собой H, (C1-C6)алкил;R86 is H, (C 1 -C 6 ) alkyl; x имеет значение 0, 1, 2; предпочтительно, 0, 1; особенно предпочтительно 1;x has the value 0, 1, 2; preferably 0, 1; particularly preferably 1; R10 представляет собой H, (C1-C8)алкил;R10 represents H, (C 1 -C 8 ) alkyl; X представляет собой связь, C=C, C(R53)(R54), СН2-СН2;X is a bond, C = C, C (R53) (R54), CH 2 —CH 2 ; R53, R54, независимо друг от друга, представляют собой H, (C1-C8)алкил;R53, R54, independently of one another, are H, (C 1 -C 8 ) alkyl; E выбран из группы, включающейE is selected from the group including
Figure 00000005
Figure 00000005
 которые могут необязательно содержать заместители, выбранные из группы, включающей H, F, Cl, Br, OH, CF3, NO2, OCF3, O-(C1-C6)алкил, (C1-C6)алкил, (C2-C6)алкенил, N(R57)(R58), SO2-CH3, CO(R65);which may optionally contain substituents selected from the group consisting of H, F, Cl, Br, OH, CF 3 , NO 2 , OCF 3 , O- (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkyl, (C 2 -C 6 ) alkenyl, N (R57) (R58), SO 2 -CH 3 , CO (R65); R57, R58, независимо друг от друга, представляют собой H, (C1-C8)алкил;R57, R58, independently of one another, are H, (C 1 -C 8 ) alkyl; R65, независимо друг от друга, представляют собой H, (C1-C8)алкил;R65, independently of one another, are H, (C 1 -C 8 ) alkyl; K представляет собой связь, O, OCH2, CH2O, CON(R68), (C(R69)(R70))v, CO, C≡C;K is a bond, O, OCH 2 , CH 2 O, CON (R68), (C (R69) (R70)) v , CO, C≡C; v имеет значение 1, 2;v has a value of 1, 2; R68, R69, R70, независимо друг от друга, представляют собой H, (C1-C8)алкил;R68, R69, R70, independently of one another, are H, (C 1 -C 8 ) alkyl; R11 представляет собой (C1-C8)алкил, (C1-C4)алкокси-(C1-C4)алкил, 3-10-членное моно- или бициклическое кольцо, которое может содержать 0-2 гетероатома, выбранных из группы, включающей кислород, азот и серу, где указанная кольцевая система может быть дополнительно замещена F, Cl, Br, CF3, CN, (C1-C6)алкилом, O-(C1-C8)алкилом, оксо, CO(R71), CON(R72)(R73), N(R75)CO(C1-C6)алкилом или SO2CH3;R11 is a (C 1 -C 8 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, 3-10 membered mono- or bicyclic ring, which may contain 0-2 heteroatoms selected from the group comprising oxygen, nitrogen and sulfur, where the specified ring system may be further substituted by F, Cl, Br, CF 3 , CN, (C 1 -C 6 ) alkyl, O- (C 1 -C 8 ) alkyl, oxo , CO (R71), CON (R72) (R73), N (R75) CO (C 1 -C 6 ) alkyl or SO 2 CH 3 ; R71, R72, R75, независимо друг от друга, представляют собой H, (C1-C8)алкил; илиR71, R72, R75, independently of one another, are H, (C 1 -C 8 ) alkyl; or R72 и R73, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу, илиR72 and R73, independently of each other, optionally together with the nitrogen atom to which they are bonded, form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0-1 additional heteroatoms selected from the group consisting of N- (C 1 -C 6 ) alkyl, oxygen and sulfur, or их N-оксиды и физиологически приемлемые соли.their N-oxides and physiologically acceptable salts. 4. Соединение по п.1, отличающееся тем, что имеет формулу (Ia)4. The compound according to claim 1, characterized in that it has the formula (Ia)
Figure 00000006
Figure 00000006
 R1, R2, независимо друг от друга, представляют собой H, (C1-C8)алкил, -(CR78R79)o-R12, (C1-C4)алкокси-(C1-C4)алкил, или R1 и R2 образуют вместе с атомом азота, с которым они связаны, 4-10-членное моно-, би- или спироциклическое кольцо, которое, помимо атома азота, может содержать 0-2 дополнительных гетероатома, выбранных из группы, включающей кислород, азот и серу, где гетероциклическая кольцевая система может быть дополнительно замещена F, (C1-C6)алкилом, О-(С1-С4)алкилом, (C1-C4)алкокси-(C1-C4)алкилом, гидрокси-(C1-C4)алкилом, (C0-C2)алкиленарилом, оксо, CO(R26), CON(R27)(R28), гидрокси, N(R31)(R32) или SO2CH3; где R1 и R2 оба не являются СО(R26);R1, R2, independently of one another, are H, (C 1 -C 8 ) alkyl, - (CR78R79) o-R12, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, or R1 and R2 form, together with the nitrogen atom to which they are bonded, a 4-10 membered mono-, bi- or spirocyclic ring, which, in addition to the nitrogen atom, may contain 0-2 additional heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur, where the heterocyclic ring system may be further substituted with F, (C 1 -C 6 ) alkyl, O- (C 1 -C 4 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, hydroxy (C 1 -C 4) alkyl, (C 0 -C 2) alkilenarilom, oxo, CO (R26), CON ( R27) (R28), idroksi, N (R31) (R32) or SO 2 CH 3; where R 1 and R 2 are not both CO (R26); o имеет значение 0, 1, 2, 3, 4;o has the value 0, 1, 2, 3, 4; q имеет значение 1, 2, 3;q is 1, 2, 3; s имеет значение 0, 1, 2;s is 0, 1, 2; R15, R16, R17, R18, R23, R24, R25, R26, R27, R28, R31, R32, независимо друг от друга, представляют собой H, (C1-C6)алкил; илиR15, R16, R17, R18, R23, R24, R25, R26, R27, R28, R31, R32, independently of one another, are H, (C1-C6) alkyl; or R17 и R18, R27 и R28, R31 и R32, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу;R17 and R18, R27 and R28, R31 and R32, independently of each other, optionally together with the nitrogen atom to which they are attached form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0-1 additional heteroatom selected from the group comprising N- (C 1 -C 6 ) alkyl, oxygen and sulfur; R12 представляет собой OH, O-(C1-C6)алкил, O(C0-C2)алкиленарил, CN, S-(C1-C6)алкил, 3-12 членное моно-, би- или спироциклическое кольцо, которое может содержать 1-3 гетероатома, выбранных из группы, включающей N, O и S, и указанное 3-12 членное кольцо может содержать дополнительные заместители, такие как F, OH, CF3, CN, оксо, (C1-C6)алкил, (C0-C2)алкиленарил, N(R34)(R35), COO(R40), CO(C1-C6)алкил;R12 is OH, O- (C 1 -C 6 ) alkyl, O (C 0 -C 2 ) alkylene aryl, CN, S- (C 1 -C 6 ) alkyl, 3-12 membered mono-, bi- or spirocyclic a ring which may contain 1-3 heteroatoms selected from the group consisting of N, O and S, and said 3-12 membered ring may contain additional substituents, such as F, OH, CF 3 , CN, oxo, (C 1 - C 6 ) alkyl, (C 0 -C 2 ) alkylenearyl, N (R34) (R35), COO (R40), CO (C 1 -C 6 ) alkyl; R34, R35, независимо друг от друга, представляют собой H, (C1-C4)алкил;R34, R35, independently of one another, are H, (C 1 -C 4 ) alkyl; R40 представляет собой H, (C1-C6)алкил, (C0-C2)алкиленарил;R40 represents H, (C 1 -C 6 ) alkyl, (C 0 -C 2 ) alkylene aryl; R78, R79, независимо друг от друга, представляют собой H, (C1-C8)алкил, гидрокси-(C1-C4)алкил, OH, (C1-C4)алкокси-(C1-C4)алкил;R78, R79, independently of one another, are H, (C 1 -C 8 ) alkyl, hydroxy- (C 1 -C 4 ) alkyl, OH, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl; R42, R42', независимо друг от друга, представляют собой H, F, Cl, Br, CF3, CN, (C1-C6)алкил;R42, R42 ', independently of one another, are H, F, Cl, Br, CF 3 , CN, (C 1 -C 6 ) alkyl; R10 представляет собой H, (C1-C8)алкил;R10 represents H, (C 1 -C 8 ) alkyl; X представляет собой N(R52), связь, C=C, C(R53)(R54), СН2СН2;X represents N (R52), a bond, C = C, C (R53) (R54), CH 2 CH 2 ; R52, R53, R54, независимо друг от друга, представляют собой H, (C1-C8)алкил;R52, R53, R54, independently of one another, are H, (C 1 -C 8 ) alkyl; E выбран из группы, включающейE is selected from the group including
Figure 00000004
Figure 00000004
 которые могут необязательно содержать заместители, выбранные из группы, включающей H, F, Cl, Br, OH, CF3, NO2, OCF3, O-(C1-C6)алкил, (C1-C6)алкил, (C2-C6)алкенил, N(R57)(R58), SO2-CH3, CO(R65);which may optionally contain substituents selected from the group consisting of H, F, Cl, Br, OH, CF 3 , NO 2 , OCF 3 , O- (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkyl, (C 2 -C 6 ) alkenyl, N (R57) (R58), SO 2 -CH 3 , CO (R65); R57, R58, независимо друг от друга, представляют собой H, (C1-C8)алкил;R57, R58, independently of one another, are H, (C 1 -C 8 ) alkyl; R65 представляют собой H, (C1-C8)алкил;R65 is H, (C 1 -C 8 ) alkyl; K представляет собой связь, O, OCH2, CH2O, S, SO2, N(R66), N(R67)CO, CON(R68), (C(R69)(R70))v, CO, C≡C, SCH2, SO2CH2;K is a bond, O, OCH 2 , CH 2 O, S, SO 2 , N (R66), N (R67) CO, CON (R68), (C (R69) (R70)) v , CO, C≡ C, SCH 2 , SO 2 CH 2 ; v имеет значение 1, 2, 3;v has a value of 1, 2, 3; R66, R67, R68, R69, R70, независимо друг от друга, представляют собой H, (C1-C8)алкил;R66, R67, R68, R69, R70, independently of one another, are H, (C 1 -C 8 ) alkyl; R11 представляет собой (C1-C8)алкил, (C1-C4)алкокси-(C1-C4)алкил, 3-10-членное моно-, би-, три- или спироциклическое кольцо, которое может содержать 0-4 гетероатома, выбранных из группы, включающей кислород, азот и серу, где указанная кольцевая система может быть дополнительно замещена F, Cl, Br, CF3, CN, (C1-C6)алкилом, O-(C1-C8)алкилом, оксо, CO(R71), гидрокси, N(R75)CO(C1-C6)алкилом или SO2CH3;R11 represents a (C 1 -C 8) alkyl, (C 1 -C 4) alkoxy- (C 1 -C 4) -alkyl, 3-10 membered mono-, bi-, tri- or spirocyclic ring which may comprise 0-4 heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur, wherein said ring system may be further substituted with F, Cl, Br, CF 3 , CN, (C 1 -C 6 ) alkyl, O- (C 1 - C 8 ) alkyl, oxo, CO (R71), hydroxy, N (R75) CO (C 1 -C 6 ) alkyl or SO 2 CH 3 ; R71, R72, R73, R74, R75, R76, R77, независимо друг от друга, представляют собой H, (C1-C8)алкил; илиR71, R72, R73, R74, R75, R76, R77, independently of one another, are H, (C 1 -C 8 ) alkyl; or R72 и R73, R76 и R77, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу, илиR72 and R73, R76 and R77, independently of each other, optionally together with the nitrogen atom to which they are bonded, form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0-1 additional heteroatoms selected from the group including N- (C 1 -C 6 ) alkyl, oxygen and sulfur, or их N-оксиды и физиологически приемлемые соли.their N-oxides and physiologically acceptable salts. 5. Соединение по п.1, отличающееся тем, что имеет формулу (Ib)5. The compound according to claim 1, characterized in that it has the formula (Ib)
Figure 00000007
Figure 00000007
 где R1, R2, независимо друг от друга, представляют собой H, (C1-C8)алкил, -(CR78R79)o-R12, (C1-C4)алкокси-(C1-C4)алкил, (C3-C8)алкенил, CO-(C1-C8)алкил, -CO-(CH2)o-R12, CO-арилокси-(C1-C4)алкил, COCH=CH(R13), COCC(R14), CO(C(R15)(R16))qN(R17)(R18), CO(C(R19)(R20))rCON(R21)(R22), CO(C(R23)(R24))sO(R25); или R1 и R2 образуют вместе с атомом азота, с которым они связаны, 4-10-членное моно-, би- или спироциклическое кольцо, которое, помимо атома азота, может содержать 0-2 дополнительных гетероатома, выбранных из группы, включающей кислород, азот и серу, где гетероциклическая кольцевая система может быть дополнительно замещена F, Cl, CF3, (C1-C6)алкилом, O-(C1-C4)алкилом, (C1-C4)алкокси-(C1-C4)алкилом, гидрокси-(C1-C4)алкилом, (C0-C2)алкиленарилом, оксо, CO(R26), CON(R27)(R28), гидрокси, COO(R29), N(R30)CO(C1-C6)алкилом, N(R31)(R32) или SO2CH3, где R1 и R2 оба не являются CO(R26);where R1, R2, independently of one another, are H, (C 1 -C 8 ) alkyl, - (CR78R79) o -R12, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, ( C 3 -C 8 ) alkenyl, CO- (C 1 -C 8 ) alkyl, -CO- (CH 2 ) o -R12, CO-aryloxy- (C 1 -C 4 ) alkyl, COCH = CH (R13), COCC (R14), CO (C (R15) (R16)) q N (R17) (R18), CO (C (R19) (R20)) r CON (R21) (R22), CO (C (R23) ( R24)) s O (R25); or R1 and R2 form, together with the nitrogen atom to which they are attached, a 4-10 membered mono-, bi- or spirocyclic ring, which, in addition to the nitrogen atom, may contain 0-2 additional heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur, where the heterocyclic ring system may be further substituted with F, Cl, CF 3 , (C 1 -C 6 ) alkyl, O- (C 1 -C 4 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, hydroxy- (C 1 -C 4 ) alkyl, (C 0 -C 2 ) alkylene aryl, oxo, CO (R26), CON (R27) (R28), hydroxy, COO (R29), N (R30) CO (C 1 -C 6 ) alkyl, N (R31) (R32) or SO 2 CH 3 , where R1 and R2 are not both CO (R26); o имеет значение 0, 1, 2, 3, 4, 5, 6;o has the value 0, 1, 2, 3, 4, 5, 6; q, r, независимо друг от друга, имеют значение 1, 2, 3;q, r, independently of each other, have a value of 1, 2, 3; s имеет значение 0, 1, 2, 3, 4;s is 0, 1, 2, 3, 4; R13, R14, независимо друг от друга, представляют собой другое фенильное кольцо, которое может содержать 0-1 атом азота;R13, R14, independently of each other, represent another phenyl ring, which may contain 0-1 nitrogen atom; R15, R16, R17, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R31, R32, независимо друг от друга, представляют собой H, (C1-C6)алкил;R15, R16, R17, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R31, R32, independently of each other, are H, (C 1 -C 6 ) alkyl; R18 представляет собой H, (C1-C6)алкил, СО-(C1-C6)алкил, CO(R33); илиR18 represents H, (C 1 -C 6 ) alkyl, CO- (C 1 -C 6 ) alkyl, CO (R33); or R17 и R18, R21 и R22, R27 и R28, R31 и R32, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу;R17 and R18, R21 and R22, R27 and R28, R31 and R32, independently of each other, optionally together with the nitrogen atom to which they are bonded, form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0 -1 an additional heteroatom selected from the group consisting of N- (C 1 -C 6 ) alkyl, oxygen and sulfur; R33 представляет собой 5-10-членную ароматическую кольцевую систему, которая может содержать дополнительный гетероатом, выбранный из группы, включающей азот, кислород и серу, и может быть замещена F, Cl, (C1-C6)алкилом, O-(C1-C8)алкилом;R33 represents a 5-10 membered aromatic ring system which may contain an additional heteroatom selected from the group consisting of nitrogen, oxygen and sulfur and may be substituted with F, Cl, (C 1 -C 6) alkyl, O- (C 1 -C 8 ) alkyl; R12 представляет собой OH, O-(C1-C6)алкил, O(C0-C8)алкиленарил, CN, S-(C1-C6)алкил, COO(R80), CON(R81)(R82), 3-12 членное моно-, би- или спироциклическое кольцо, которое может содержать один или несколько гетероатомов, выбранных из группы, включающей N, O и S, и указанное 3-12 членное кольцо может содержать дополнительные заместители, такие как F, Cl, Br, OH, CF3, CN, оксо, O-(C1-C6)алкил, (C1-C4)алкокси-(C1-C4)алкил, (C1-C6)алкил, O-(C0-C8)алкиленарил, (C0-C8)алкиленарил, N(R34)(R35), COCH=CH(R36), (C(R37)(R38))t(R39), CO(C(R37)(R38))t(R39), CO(C1-C6)алкил, COCOO(C1-C6)алкил, COO(R40), S(O)u(R41);R12 is OH, O- (C 1 -C 6 ) alkyl, O (C 0 -C 8 ) alkylenearyl, CN, S- (C 1 -C 6 ) alkyl, COO (R80), CON (R81) (R82 ), A 3-12 membered mono-, bi- or spirocyclic ring, which may contain one or more heteroatoms selected from the group consisting of N, O and S, and said 3-12 membered ring may contain additional substituents, such as F, Cl, Br, OH, CF 3 , CN, oxo, O- (C 1 -C 6 ) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, (C 1 -C 6 ) alkyl , O- (C 0 -C 8 ) alkylene aryl, (C 0 -C 8 ) alkylene aryl, N (R34) (R35), COCH = CH (R36), (C (R37) (R38)) t (R39), CO (C (R37) (R38)) t (R39), CO (C 1 -C 6 ) alkyl, COCOO (C 1 -C 6 ) alkyl, COO (R40), S (O) u (R41); t имеет значение 0, 1, 2, 3, 4, 5, 6;t is 0, 1, 2, 3, 4, 5, 6; u имеет значение 0, 1, 2;u has the value 0, 1, 2; R34, R35, R37, R38, независимо друг от друга, представляют собой H, (C1-C8)алкил; илиR34, R35, R37, R38, independently of one another, are H, (C 1 -C 8 ) alkyl; or R34 и R35 необязательно вместе с атомом азота, с которым они связаны, образуют 5-6 членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу, и может необязательно быть замещенным 1-2 оксогруппами;R34 and R35 optionally together with the nitrogen atom to which they are bonded form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0-1 additional heteroatoms selected from the group consisting of N- (C 1 -C 6 ) alkyl, oxygen and sulfur, and may optionally be substituted with 1-2 oxo groups; R36, R39, независимо друг от друга, представляет собой (C3-C8)циклоалкил, 5-10-членную ароматическую кольцевую систему, которая может содержать 0-2 дополнительных гетероатома, выбранных из группы, включающей азот, кислород и серу, и может быть замещена F, Cl, (C1-C6)алкилом, O-(C1-C8)алкилом;R36, R39, independently of one another, is a (C 3 -C 8 ) cycloalkyl, 5-10 membered aromatic ring system which may contain 0-2 additional heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and may be substituted with F, Cl, (C 1 -C 6 ) alkyl, O- (C 1 -C 8 ) alkyl; R40 представляет собой H, (C1-C8)алкил, (C2-C6)алкенил, (C0-C8)алкиленарил;R40 represents H, (C 1 -C 8 ) alkyl, (C 2 -C 6 ) alkenyl, (C 0 -C 8 ) alkylenearyl; R41 представляет собой (C1-C6)алкил, 5-10-членную ароматическую кольцевую систему, которая может содержать 0-2 дополнительных гетероатома, выбранных из группы, включающей азот, кислород и серу, и может быть замещена F, Cl, (C1-C6)алкилом, O-(C1-C8)алкилом;R41 is a (C 1 -C 6 ) alkyl, 5-10 membered aromatic ring system that may contain 0-2 additional heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and may be substituted with F, Cl, ( C 1 -C 6 ) alkyl; O- (C 1 -C 8 ) alkyl; R78, R79, независимо друг от друга, представляют собой H, (C1-C8)алкил, гидрокси-(C1-C4)алкил, OH, (C1-C4)алкокси-(C1-C4)алкил;R78, R79, independently of one another, are H, (C 1 -C 8 ) alkyl, hydroxy- (C 1 -C 4 ) alkyl, OH, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl; R80, R81, независимо друг от друга, представляют собой H, (C1-C8)алкил;R80, R81, independently of one another, are H, (C 1 -C 8 ) alkyl; R10 представляет собой H, (C1-C8)алкил;R10 represents H, (C 1 -C 8 ) alkyl; E выбран из группы, включающейE is selected from the group including
Figure 00000004
Figure 00000004
 которые могут необязательно содержать заместители, выбранные из группы, включающей H, F, Cl, Br, OH, CF3, NO2, OCF3, O-(C1-C6)алкил, (C1-C6)алкил, (C2-C6)алкенил, N(R57)(R58), SO2-CH3, CO(R65);which may optionally contain substituents selected from the group consisting of H, F, Cl, Br, OH, CF 3 , NO 2 , OCF 3 , O- (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkyl, (C 2 -C 6 ) alkenyl, N (R57) (R58), SO 2 -CH 3 , CO (R65); R57, R58, независимо друг от друга, представляют собой H, (C1-C8)алкил;R57, R58, independently of one another, are H, (C 1 -C 8 ) alkyl; R65, независимо друг от друга, представляют собой H, (C1-C8)алкил, арил;R65, independently of one another, are H, (C 1 -C 8 ) alkyl, aryl; K представляет собой связь, O, OCH2, CH2O, S, SO, SO2, N(R66), N(R67)CO, CON(R68), (C(R69)(R70))v, CO, С=С, C≡C, SCH2, SO2CH2;K is a bond, O, OCH 2, CH 2 O, S, SO, SO 2, N (R66), N ( R67) CO, CON (R68), (C (R69) (R70)) v, CO, C = C, C≡C, SCH 2 , SO 2 CH 2 ; v имеет значение 1, 2, 3, 4;v is 1, 2, 3, 4; R66, R67, R68, R69, R70, независимо друг от друга, представляют собой H, (C1-C8)алкил;R66, R67, R68, R69, R70, independently of one another, are H, (C 1 -C 8 ) alkyl; R11 представляет собой (C1-C8)алкил, (C1-C4)алкокси-(C1-C4)алкил, (С3-С8)алкенил, (С3-С8)алкинил, 3-10-членное моно-, би-, три- или спироциклическое кольцо, которое может содержать 0-4 гетероатома, выбранных из группы, включающей кислород, азот и серу, где указанная кольцевая система может быть дополнительно замещена F, Cl, Br, CF3, CN, (C1-C6)алкилом, O-(C1-C8)алкилом, (С1-С4)алкокси-(С1-С4)алкилом, гидрокси-(С1-С4)алкилом, (С0-С8)алкиленарилом, оксо, CO(R71), CON(R73)(R73), гидрокси, COO(R74), N(R75)CO(C1-C6)алкилом, N(R76)(R77) или SO2CH3;R11 is (C1-C8) alkyl, (C1-C4) alkoxy- (C1-C4) alkyl, (C 3 -C 8 ) alkenyl, (C 3 -C 8 ) alkynyl, 3-10 membered mono, a bi-, tri- or spirocyclic ring, which may contain 0-4 heteroatoms selected from the group comprising oxygen, nitrogen and sulfur, where said ring system may be further substituted by F, Cl, Br, CF 3 , CN, (C1- C6) alkyl, O- (C1-C8) alkyl, (C 1 -C 4 ) alkoxy- (C 1 -C 4 ) alkyl, hydroxy- (C 1 -C 4 ) alkyl, (C 0 -C 8 ) alkylene aryl oxo, CO (R71), CON (R73) (R73), hydroxy, COO (R74), N (R75) CO (C1-C6) alkyl, N (R76) (R77) or SO 2 CH 3 ; R71, R72, R73, R74, R75, R76, R77, независимо друг от друга, представляют собой H, (C1-C8)алкил; илиR71, R72, R73, R74, R75, R76, R77, independently of one another, are H, (C1-C8) alkyl; or R72 и R73, R76 и R77, независимо друг от друга, необязательно вместе с атомом азота, с которым они связаны, образуют 5-6-членное кольцо, которое, помимо атома азота, может также содержать 0-1 дополнительный гетероатом, выбранный из группы, включающей N-(C1-C6)алкил, кислород и серу, илиR72 and R73, R76 and R77, independently of each other, optionally together with the nitrogen atom to which they are bonded, form a 5-6 membered ring, which, in addition to the nitrogen atom, may also contain 0-1 additional heteroatoms selected from the group including N- (C1-C6) alkyl, oxygen and sulfur, or их N-оксиды и физиологически приемлемые соли.their N-oxides and physiologically acceptable salts. 6. Лекарственное средство, включающее одно или несколько соединений по пп.1-5.6. A medicine comprising one or more compounds according to claims 1-5. 7. Лекарственное средство, включающее одно или несколько соединений по пп.1-5 и один или несколько анорексически активных ингредиентов.7. A medicament comprising one or more compounds according to claims 1-5 and one or more anorexic active ingredients. 8. Соединение формулы (I) по пп.1-5 для применения в качестве лекарственного средства для профилактики и лечения ожирения.8. The compound of formula (I) according to claims 1-5 for use as a medicine for the prevention and treatment of obesity. 9. Соединение формулы (I) по пп.1-5 для применения в качестве лекарственного средства для профилактики и лечения диабета типа II.9. The compound of formula (I) according to claims 1-5 for use as a medicine for the prevention and treatment of type II diabetes. 10. Соединение формулы (I) по пп.1-5 в сочетании с по меньшей мере одним дополнительным анорексически активным ингредиентом для применения в качестве лекарственного средства для профилактики и лечения ожирения.10. The compound of formula (I) according to claims 1-5 in combination with at least one additional anorexic active ingredient for use as a medicament for the prevention and treatment of obesity. 11. Соединение формулы (I) по пп.1-5 в сочетании с по меньшей мере одним дополнительным анорексически активным ингредиентом для применения в качестве лекарственного средства для профилактики и лечения диабета типа II.11. The compound of formula (I) according to claims 1-5 in combination with at least one additional anorexic active ingredient for use as a medicament for the prevention and treatment of type II diabetes. 12. Способ получения лекарственного средства, включающего одно или несколько соединений формулы (I) по пп.1-5, который включает смешивание активного ингредиента с фармацевтически приемлемым носителем и преобразование полученной смеси в форму, подходящую для введения.12. A method for producing a medicament comprising one or more compounds of formula (I) according to claims 1-5, which comprises mixing the active ingredient with a pharmaceutically acceptable carrier and converting the resulting mixture into a form suitable for administration. 13. Применение соединения формулы (I) по пп.1-5 для получения лекарственного средства для снижения массы у млекопитающих.13. The use of the compounds of formula (I) according to claims 1-5 for the preparation of a medicament for weight loss in mammals. 14. Применение соединения формулы (I) по пп.1-5 для получения лекарственного средства для профилактики и лечения ожирения.14. The use of the compounds of formula (I) according to claims 1-5 for the manufacture of a medicament for the prevention and treatment of obesity. 15. Применение соединения формулы (I) по пп.1-5 для получения лекарственного средства для профилактики и лечения диабета типа II.15. The use of the compounds of formula (I) according to claims 1-5 for the manufacture of a medicament for the prevention and treatment of type II diabetes. 16. Применение соединения формулы (I) по пп.1-5 для получения лекарственного средства для лечения тревожности и других психиатрических показаний, для лечения расстройств, связанных с циркадным ритмом, и для лечения злоупотребления лекарственными средствами.16. The use of the compounds of formula (I) according to claims 1-5 for the manufacture of a medicament for the treatment of anxiety and other psychiatric indications, for the treatment of circadian rhythm disorders, and for the treatment of drug abuse. 17. Применение соединения формулы (I) по пп.1-5 для получения лекарственного средства, обладающего активностью антагониста МСН-рецептора.17. The use of the compounds of formula (I) according to claims 1-5 for the preparation of a medicament having an MCH receptor antagonist activity.
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