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RU2005110061A - Замещенные пиперазины, (1,4)-диазепины и 2,5-диазабицикло(2,2,1)гептаны в качестве н1-и/или н3-антагонистов гистамина или обратных н3-антагонистов гистамина - Google Patents

Замещенные пиперазины, (1,4)-диазепины и 2,5-диазабицикло(2,2,1)гептаны в качестве н1-и/или н3-антагонистов гистамина или обратных н3-антагонистов гистамина Download PDF

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RU2005110061A
RU2005110061A RU2005110061/04A RU2005110061A RU2005110061A RU 2005110061 A RU2005110061 A RU 2005110061A RU 2005110061/04 A RU2005110061/04 A RU 2005110061/04A RU 2005110061 A RU2005110061 A RU 2005110061A RU 2005110061 A RU2005110061 A RU 2005110061A
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Russia
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alkyl
aryl
group
heterocyclyl
heteroaryl
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RU2005110061/04A
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RU2328494C2 (ru
Inventor
Рейчел ЭНКЛИФФ (GB)
Рейчел ЭНКЛИФФ
Колин Дейвид ЭЛДРЕД (GB)
Колин Дейвид Элдред
Ивонн К. ФОГДЕН (GB)
Ивонн К. ФОГДЕН
Эшли Пол ХЭНКОК (GB)
Эшли Пол ХЭНКОК
Томас Дэниел ХЕЙТМАН (GB)
Томас Дэниел Хейтман
Хизер ХОББЗ (GB)
Хизер ХОББЗ
Саймон Тинби ХОДЖСОН (GB)
Саймон Тинби Ходжсон
Мэттью Дж. ЛИНДОН (GB)
Мэттью Дж. ЛИНДОН
Дейвид Мэттью УИЛСОН (GB)
Дейвид Мэттью УИЛСОН
Original Assignee
Глаксо Груп Лимитед (GB)
Глаксо Груп Лимитед
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
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Claims (8)

1. Соединение формулы (I)
Figure 00000001
где R1 представляет собой водород, -С1-6алкил, -С1-6алкокси, -С3-8циклоалкил, -С1-6алкил-С3-8циклоалкил, арил, гетероциклил, гетероарил, -С1-6алкил-арил, -С1-6алкил-гетероарил, -С1-6алкил-гетероциклил, -арил-арил, -арил-гетероарил, -арил-гетероциклил, -гетероарил-арил, -гетероарил-гетероарил, -гетероарил-гетероциклил, -гетероциклил-арил, -гетероциклил-гетероарил, -гетероциклил-гетероциклил, где R1 может быть возможно замещен одним или более чем одним заместителем, которые могут быть одинаковыми или разными и которые выбраны из группы, состоящей из галогена, гидрокси, COOR15, циано, -С1-6алкил-циано, нитро, оксо, трифторметила, трифторметокси, фторметокси, дифторметокси, С1-6алкила (возможно замещенного группой COOR15), С2-6алкенила (возможно замещенного группой COOR15), С2-6алкинила (возможно замещенного группой COOR15), С1-6алкокси (возможно замещенного группой COOR15), пентафторэтила, C1-6алкокси, С2-6алкенокси, арила, арилС1-6алкила, -СО-арила (возможно замещенного атомом галогена), -СО-гетероарила, -С1-6алкил-СО-арила, арилС1-6алкокси, С1-6алкилтио, С1-6алкоксиС1-6алкила, С3-7циклоалкила, С3-7циклоалкилС1-6алкокси, С1-6алкоксикарбонила, С1-6алкилсульфонила, С1-6алкилсульфинила, С1-6алкилсульфонилокси, С1-6алкилсульфонилС1-6алкила, сульфонила, арилсульфонила, арилсульфонилокси, арилсульфонилС1-6алкила, арилокси, С1-6алкилсульфонамидо, С1-6алкиламидо, С1-6алкилсульфонамидоС1-6алкила, С1-6алкиламидоС1-6алкила, арилсульфонамидо, арилкарбоксамидо, арилсульфонамидоС1-6алкила, арилкарбоксамидоС1-6алкила, ароила, ароилС1-6алкила, арилС1-6алканоила или группы -COR15, -NR15R16, -CONR15R16, -NR15COR16, -NR15SO2R16 или -SO2NR15R16, где R15 и R16 независимо представляют собой водород, С1-6алкил или С3-8циклоалкил либо вместе могут быть конденсированы с образованием 5-7-членного неароматического гетероциклического кольца, возможно прерванного атомом О или S и возможно замещенного галогеном, С1-6алкилом или группой -С1-6алкилС1-6алкокси;
Z представляет собой связь, СО, -CON(R10)- или SO2, так что, когда R1 представляет собой водород, тогда Z представляет собой CONR10;
р представляет собой 1 или 2;
m, n и r независимо представляют собой 0, 1 или 2;
R2 представляет собой галоген, С1-6алкил, С1-6алкокси, циано, амино или трифторметил, так что, когда n представляет собой 2, тогда две группы R2 взамен могут быть связаны с образованием фенильного кольца;
R4 представляет собой С1-6алкил, так что, когда r представляет собой 2, тогда две группы R4 взамен могут быть связаны с образованием группы СН2, (СН2)2 или (СН2)3;
R10 представляет собой водород или С1-6алкил, либо R10 вместе с R1 образуют гетероциклическую группу;
R3 представляет собой -(CH2)q-NR11R12 или группу формулы (i)
Figure 00000002
где q представляет собой 2, 3 или 4;
R11 и R12 независимо представляют собой С1-6алкил или С3-8циклоалкил, либо вместе с атомом азота, к которому они присоединены, представляют собой N-связанную азотсодержащую гетероциклильную группу, возможно замещенную одной или более чем одной группой R17;
R13 представляет собой водород, С1-6алкил, -С1-6алкил-С1-6алкокси, С3-8циклоалкил, -С1-6алкил-С3-8циклоалкил, -С1-6алкил-арил или гетероциклил;
R14 и R17 независимо представляют собой галоген, С1-6алкил, галогеноалкил, ОН, диС1-6алкиламино, С1-6алкокси или гетероциклил;
f и k независимо представляют собой 0, 1 или 2;
g представляет собой 0, 1 или 2, и h представляет собой 0, 1, 2 или 3, так что g и h оба не могут представлять собой 0;
при условии, что когда m представляет собой 1, n и r оба представляют собой 0 и R3 представляет собой -(CH2)3-N-пиперидин или -(СН2)3-N(этил)2, тогда R1-Z представляет собой группу, отличную от метила, -СО-O-С(СН3)3 или бензила;
и при условии, что когда m, n и r все представляют собой 0, р представляет собой 1, R3 представляет собой -(CH2)3-N-пирролидин или -(СН2)3-N-пиперидин, R1 представляет собой бензил, тогда Z представляет собой группу, отличную от связи;
и при условии, что когда m, n и r все представляют собой 0, р представляет собой 1, R3 представляет собой -(СН2)3-N-пиперидин, R1 представляет собой изопропил, тогда Z представляет собой группу, отличную от связи;
и при условии, что когда m представляет собой 1, n и r оба представляют собой 0, р представляет собой 1, R3 представляет собой -(CH2)3-N-пиперидин, R1 представляет собой метил, изопропил, арил или бензил, тогда Z представляет собой группу, отличную от связи;
и при условии, что когда тип оба представляют собой 0, R3 представляет собой -(СН2)3-N(этил)2, р представляет собой 1, r представляет собой 2, и R1 и R4 оба представляют собой метил, тогда Z представляет собой группу, отличную от связи,
или его фармацевтически приемлемая соль.
2. Соединение по п.1, представляющее собой соединение формулы П1-П503 или его фармацевтически приемлемую соль.
3. Фармацевтическая композиция, включающая соединение формулы (I) по п.1 или п.2 или его фармацевтически приемлемую соль и фармацевтически приемлемый носитель или эксципиент.
4. Соединение, как оно определено в п.1 или 2, для применения в терапии.
5. Соединение, как оно определено в п.1 или 2, для применения в лечении неврологических заболеваний или воспалительных заболеваний верхних дыхательных путей.
6. Применение соединения по п.1 или 2 в изготовлении лекарства для лечения неврологических заболеваний или воспалительных заболеваний верхних дыхательных путей.
7. Способ лечения неврологических заболеваний или воспалительных заболеваний верхних дыхательных путей, включающий введение хозяину, нуждающемуся в этом, эффективного количества соединения формулы (I) по п.1 или 2 или его фармацевтически приемлемой соли.
8. Фармацевтическая композиция для применения в лечении неврологических заболеваний или воспалительных заболеваний верхних дыхательных путей, включающая соединение формулы (I) по п.1 или 2 или его фармацевтически приемлемую соль и фармацевтически приемлемый носитель.
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