RU2011146363A - Производные n-ацил-n-фенилпиперазина, используемые (кроме того) для профилактики или лечения диабета - Google Patents

Производные n-ацил-n-фенилпиперазина, используемые (кроме того) для профилактики или лечения диабета Download PDF

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RU2011146363A
RU2011146363A RU2011146363/04A RU2011146363A RU2011146363A RU 2011146363 A RU2011146363 A RU 2011146363A RU 2011146363/04 A RU2011146363/04 A RU 2011146363/04A RU 2011146363 A RU2011146363 A RU 2011146363A RU 2011146363 A RU2011146363 A RU 2011146363A
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Сизуо КАСАЙ
МЛ. Кевин Фрэнсис МАКГИ
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Такеда Фармасьютикал Компани Лимитед
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    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
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    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
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    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
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Abstract

1. Соединение, представленное формулойгде кольцо A представляет собой бензольное кольцо, необязательно дополнительно замещенное;кольцо B представляет собой пиперазиновое кольцо, необязательно дополнительно замещенное; иR представляет собой заместитель,при условии, что трет-бутил 4-[2-трет-бутил-5-({[2-(1H-индазол-6-иламино)пиридин-3-ил]карбонил}амино)фенил]пиперазин-1-карбоксилат,или его соль.2. Соединение или его соль по п.1, где R представляет собой необязательно замещенную углеводородную группу, необязательно замещенную гетероциклическую группу, необязательно замещенную аминогруппу или ацильную группу.3. Соединение или его соль по п.1, где кольцо A представляет собой бензольное кольцо, необязательно замещенное 1-3 заместителями, выбранными из (a) атома галогена и (b) Cалкильной группы.4. Соединение или его соль по п.1, где кольцо A представляет собой бензольное кольцо.5. Соединение или его соль по п.1, где кольцо B представляет собой пиперазиновое кольцо.6. Соединение или его соль по п.1, где R представляет собой:(1) Cалкильную группу, необязательно замещенную 1-3 заместителями, выбранными из:(a) карбамоильной группы, необязательно моно- или дизамещенной:(i) Cалкилсульфонильной группой и(ii) сульфамоильной группой, необязательно замещенной Cалкильной группой, необязательно замещенной Cциклоалкилом,(b) 5- или 6-членной ароматической гетероциклической группы, необязательно замещенной 1-3 заместителями, выбранными из:(i) карбоксигруппы и(ii) Cалкильной группы,(c) 5- или 6-членной неароматической гетероциклической группы, необязательно замещенной 1-3 карбоксигруппами, и(d) карбоксигруппы;(2) Cарильную группу, необязательно замещенную 1-3 заместит�

Claims (19)

1. Соединение, представленное формулой
Figure 00000001
где кольцо A представляет собой бензольное кольцо, необязательно дополнительно замещенное;
кольцо B представляет собой пиперазиновое кольцо, необязательно дополнительно замещенное; и
R представляет собой заместитель,
при условии, что трет-бутил 4-[2-трет-бутил-5-({[2-(1H-индазол-6-иламино)пиридин-3-ил]карбонил}амино)фенил]пиперазин-1-карбоксилат,
или его соль.
2. Соединение или его соль по п.1, где R представляет собой необязательно замещенную углеводородную группу, необязательно замещенную гетероциклическую группу, необязательно замещенную аминогруппу или ацильную группу.
3. Соединение или его соль по п.1, где кольцо A представляет собой бензольное кольцо, необязательно замещенное 1-3 заместителями, выбранными из (a) атома галогена и (b) C1-6 алкильной группы.
4. Соединение или его соль по п.1, где кольцо A представляет собой бензольное кольцо.
5. Соединение или его соль по п.1, где кольцо B представляет собой пиперазиновое кольцо.
6. Соединение или его соль по п.1, где R представляет собой:
(1) C1-10 алкильную группу, необязательно замещенную 1-3 заместителями, выбранными из:
(a) карбамоильной группы, необязательно моно- или дизамещенной:
(i) C1-6 алкилсульфонильной группой и
(ii) сульфамоильной группой, необязательно замещенной C1-6 алкильной группой, необязательно замещенной C3-10 циклоалкилом,
(b) 5- или 6-членной ароматической гетероциклической группы, необязательно замещенной 1-3 заместителями, выбранными из:
(i) карбоксигруппы и
(ii) C1-6 алкильной группы,
(c) 5- или 6-членной неароматической гетероциклической группы, необязательно замещенной 1-3 карбоксигруппами, и
(d) карбоксигруппы;
(2) C6-14 арильную группу, необязательно замещенную 1-3 заместителями, выбранными из:
(a) карбоксигруппы,
(b) C1-6 алкоксигруппы, необязательно замещенной 1-3 карбоксигруппами,
(c) 5- или 6-членной неароматической гетероциклической группы, необязательно замещенной 1-3 карбоксигруппами, и
(d) C6-14 арильной группы, необязательно замещенной карбокси-C1-6 алкильной группой;
(3) 5- или 6-членную ароматическую гетероциклическую группу, необязательно замещенную 1-3 заместителями, выбранными из:
(a) C1-6 алкильной группы, необязательно замещенной 1-3 карбоксигруппами, и
(b) C1-6 алкоксигруппы, необязательно замещенной 1-3 карбоксигруппами;
(4) аминогруппу, необязательно моно- или дизамещенную заместителями, выбранными из:
(a) C6-14 арильной группы, необязательно замещенной 1-3 карбокси-C1-6 алкоксигруппами,
(b) C1-6 алкильной группы, необязательно замещенной 1-3 карбоксигруппами, и
(c) 5- или 6-членной ароматической гетероциклической группы, необязательно замещенной 1-3 заместителями, выбранными из:
(i) гидроксигруппы и
(ii) карбамоильной группы;
(5) карбоксигруппу; или
(6) карбамоильную группу, необязательно моно- или дизамещенную заместителями, выбранными из:
(a) C1-6 алкильной группы, необязательно замещенной 1-3 заместителями, выбранными из:
(i) C6-14 арильной группы, необязательно замещенной 1-3 заместителями, выбранными из:
(A) карбоксигруппы и
(B) карбокси-C1-6 алкильной группы,
(ii) карбоксигруппы и
(iii) C1-6 алкилсульфонильной группы, и
(b) 5- или 6-членной неароматической гетероциклической группы, необязательно замещенной 1-3 заместителями, выбранными из:
(i) карбоксигруппы,
(ii) карбоксикарбонильной группы и
(iii) карбокси-C1-6 алкоксигруппы.
7. Соединение или его соль по п.1, где кольцо A представляет собой бензольное кольцо, необязательно замещенное 1-3 заместителями, выбранными из (a) атома галогена и (b) C1-6 алкильной группы;
кольцо B представляет собой пиперазиновое кольцо и
R представляет собой:
(1) C1-10 алкильную группу, необязательно замещенную 1-3 заместителями, выбранными из:
(a) карбамоильной группы, необязательно моно- или дизамещенной:
(i) C1-6 алкилсульфонильной группы и
(ii) сульфамоильной группой, необязательно замещенной C1-6 алкильной группой, необязательно замещенной C3-10 циклоалкилом,
(b) 5- или 6-членной ароматической гетероциклической группы, необязательно замещенной 1-3 заместителями, выбранными из:
(i) карбоксигруппы и
(ii) C1-6 алкильной группы,
(c) 5- или 6-членной неароматической гетероциклической группы, необязательно замещенной 1-3 карбоксигруппами, и
(d) карбоксигруппы;
(2) C6-14 арильную группу, необязательно замещенную 1-3 заместителями, выбранными из:
(a) карбоксигруппы,
(b) C1-6 алкоксигруппы, необязательно замещенной 1-3 карбоксигруппами,
(c) 5- или 6-членной неароматической гетероциклической группы, необязательно замещенной 1-3 карбоксигруппами, и
(d) C6-14 арильной группы, необязательно замещенной карбокси-C1-6 алкильной группой;
(3) 5- или 6-членную ароматическую гетероциклическую группу, необязательно замещенную 1-3 заместителями, выбранными из:
(a) C1-6 алкильной группы, необязательно замещенной 1-3 карбоксигруппами, и
(b) C1-6 алкоксигруппы, необязательно замещенной 1-3 карбоксигруппами;
(4) аминогруппу, необязательно моно- или дизамещенную заместителями, выбранными из:
(a) C6-14 арильной группы, необязательно замещенной 1-3 карбокси-C1-6 алкоксигруппами,
(b) C1-6 алкильной группы, необязательно замещенной 1-3 карбоксигруппами, и
(c) 5- или 6-членной ароматической гетероциклической группы, необязательно замещенной 1-3 заместителями, выбранными из:
(i) гидроксигруппы и
(ii) карбамоильной группы;
(5) карбоксигруппу или
(6) карбамоильную группу, необязательно моно- или дизамещенную заместителями, выбранными из:
(a) C1-6 алкильной группы, необязательно замещенной 1-3 заместителями, выбранными из:
(i) C6-14 арильной группы, необязательно замещенной 1-3 заместителями, выбранными из:
(A) карбоксигруппы и
(B) карбокси-C1-6 алкильной группы,
(ii) карбоксигруппы и
(iii) C1-6 алкилсульфонильной группы, и
(b) 5- или 6-членной неароматической гетероциклической группы, необязательно замещенной 1-3 заместителями, выбранными из:
(i) карбоксигруппы,
(ii) карбоксикарбонильной группы и
(iii) карбокси-C1-6 алкоксигруппы.
8. N-{[4-(2-трет-Бутилфенил)пиперазин-1-ил]карбонил}глицин или его соль.
9. 3-[4-(2-трет-Бутилфенил)пиперазин-1-ил]-3-оксопропановая кислота или ее соль.
10. [4-(2-трет-Бутил-4-хлорфенил)пиперазин-1-ил](оксо)уксусная кислота или ее соль.
11. Пролекарство соединения или соли по п.1.
12. Фармацевтическая композиция, содержащая соединение или соль по п.1 или его(ее) пролекарство.
13. Фармацевтическая композиция по п.12, которая является композицией для профилактики или лечения заболевания, связанного с ретинол-связывающим белком 4.
14. Средство, снижающее ретинол-связывающий белок 4, содержащее соединение, представленное формулой
Figure 00000002
где кольцо A представляет собой бензольное кольцо, необязательно дополнительно замещенное;
кольцо B представляет собой пиперазиновое кольцо, необязательно дополнительно замещенное; и
R представляет собой заместитель,
или его соль или его пролекарство.
15. Средство для профилактики или лечения диабета, содержащее соединение, представленное формулой
Figure 00000003
где кольцо A представляет собой бензольное кольцо, необязательно дополнительно замещенное;
кольцо B представляет собой пиперазиновое кольцо, необязательно дополнительно замещенное; и
R представляет собой заместитель,
или его соль или его пролекарство.
16. Способ снижения ретинол-связывающего белка 4 у млекопитающего, содержащий введение млекопитающему эффективного количества соединения, представленного формулой
Figure 00000001
где кольцо A представляет собой бензольное кольцо, необязательно дополнительно замещенное;
кольцо B представляет собой пиперазиновое кольцо, необязательно дополнительно замещенное; и
R представляет собой заместитель,
или его соли или его пролекарства.
17. Способ профилактики или лечения диабета у млекопитающего, содержащий введение млекопитающему эффективного количества соединения, представленного формулой
Figure 00000001
где кольцо A представляет собой бензольное кольцо, необязательно дополнительно замещенное;
кольцо B представляет собой пиперазиновое кольцо, необязательно дополнительно замещенное; и
R представляет собой заместитель,
или его соли или его пролекарства.
18. Применение соединения, представленного формулой
Figure 00000001
где кольцо A представляет собой бензольное кольцо, необязательно дополнительно замещенное;
кольцо B представляет собой пиперазиновое кольцо, необязательно дополнительно замещенное; и
R представляет собой заместитель,
или его соли или его пролекарства для изготовления средства, снижающего ретинол-связывающий белок 4.
19. Применение соединения, представленного формулой
Figure 00000001
где кольцо A представляет собой бензольное кольцо, необязательно дополнительно замещенное;
кольцо B представляет собой пиперазиновое кольцо, необязательно дополнительно замещенное; и
R представляет собой заместитель,
или его соли или его пролекарства для изготовления фармацевтической композиции для профилактики или лечения диабета.
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