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RU2015122801A - 3-аминоциклопентанкарбоксамидные производные - Google Patents

3-аминоциклопентанкарбоксамидные производные Download PDF

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RU2015122801A
RU2015122801A RU2015122801A RU2015122801A RU2015122801A RU 2015122801 A RU2015122801 A RU 2015122801A RU 2015122801 A RU2015122801 A RU 2015122801A RU 2015122801 A RU2015122801 A RU 2015122801A RU 2015122801 A RU2015122801 A RU 2015122801A
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atoms
het
pharmaceutically acceptable
tautomers
stereoisomers
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RU2015122801A
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RU2641913C2 (ru
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Христос ТСАКЛАКИДИС
Вольфганг Штеле
Бригитта ЛОЙТНЕР
Пауль ЧОДРОВСКИ
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Мерк Патент Гмбх
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    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
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Claims (97)

1. Соединения формулы I
Figure 00000001
в которой
R представляет собой Ar, Het, -С≡С-Ar или -C≡C-Het,
W представляет собой NR2R2' или Het1,
R1 представляет собой A, [C(R3)2]nAr1 или [C(R3)2]nCyc,
R2, R2' каждый, независимо друг от друга, представляет собой Н, А или [C(R3)2]nCyc,
R4 представляет собой Н, F, Cl, Br, ОН, CN, NO2, A', OA', SA', SO2Me, СОА', CONH2, CONHA' или CONA'2,
X1, X2, X3, X4 каждый, независимо друг от друга, представляет собой СН или N,
А представляет собой неразветвленный или разветвленный алкил с 1-10 атомами С, в котором два расположенных рядом атома углерода могут образовывать двойную связь и/или одна или две не расположенные рядом СН- и/или СН2-группы могут быть заменены на атомы N, О и/или S и в котором 1-7 атомов Н могут быть заменены на R5,
Cyc представляет собой циклоалкил с 3-7 атомами С, который является незамещенным или монозамещенным посредством ОН, Hal или А,
А' представляет собой неразветвленный или разветвленный алкил с 1-6 атомами С, в котором 1-5 атомов Н могут быть заменены на F,
R5 представляет собой F, Cl или ОН,
Ar представляет собой фенил, который является незамещенным или моно-, ди-, три-, тетра- или пентазамещенным посредством Hal, A, O[C(R3)2]nHet1, Ar1, [C(R3)2]pOR3, [C(R3)2]pN(R3)2, NO2, CN, [C(R3)2]pCOOR3, CON(R3)2, [C(R3)2]pN(R3)2, N(R3)2COA, NR3SO2A, [C(R3)2]pSO2N(R3)2, S(O)nA, O[C(R3)2]mN(R3)2, NHCOOA, NHCON(R3)2 и/или СОА,
Ar1 представляет собой фенил или нафтил, который является незамещенным или моно-, ди-, три-, тетра- или пентазамещенным посредством Hal, A, [C(R3)2]pOR3, [C(R3)2]pN(R3)2, NO2, CN, [C(R3)2]pCOOR3, [C(R3)2]pN(R3)2, N(R3)2COA, NR3SO2A, [C(R3)2]pSO2N(R3)2, S(O)nA, O[C(R3)2]mN(R3)2, NHCOOA, NHCON(R3)2 и/или СОА,
R3 представляет собой H или неразветвленный или разветвленный алкил с 1-6 атомами С,
Het представляет собой моно- и бициклический насыщенный, ненасыщенный или ароматический гетероцикл, содержащий от 1 до 4 атомов N, О и/или S, который является незамещенным или моно-, ди-, три-, тетра- или пентазамещенным посредством Hal, A, [C(R3)2]nOA', [C(R3)2]nN(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, COHet1, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, O[C(R3)2]mN(R3)2, NHCOOA, NHCON(R3)2, CHO, COA, =S, =NH, =NA и/или =O (карбонильный кислород),
Het1 представляет собой моно- и бициклический насыщенный, ненасыщенный или ароматический гетероцикл, содержащий от 1 до 4 атомов N, О и/или S, который является незамещенным или моно-, ди-, три-, тетра- или пентазамещенным посредством Hal, A, [C(R3)2]nOR3, [C(R3)2]nN(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, O[C(R3)2]mN(R3)2, NHCOOA, NHCON(R3)2, CHO, COA, =S, =NH, =NA и/или =O (карбонильный кислород),
Hal представляет собой F, Cl, Br или I,
m представляет собой 1, 2 или 3,
n представляет собой 0, 1 или 2,
р представляет собой 0, 1, 2, 3 или 4,
q 0, 1, 2 или 3,
при условии, что только один или два из X1, X2, X3, X4 представляют собой N,
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
2. Соединения по п. 1, в которых
R4 представляет собой Н, F, Cl, OA' или А',
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
3. Соединения по п. 1 или 2, в которых
А представляет собой неразветвленный или разветвленной алкил с 1-10 атомами С, где одна или две не расположенные рядом СН- и/или СН2-группы могут быть заменены на атомы N и/или О и 1-7 атомов Н могут быть заменены на R5,
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
4. Соединения по п. 1, в которых
Ar представляет собой фенил, который является незамещенным или моно-, ди-, три-, тетра- или пентазамещенным посредством O[C(R3)2]nHet1, Ar1, A, CN и/или [C(R3)2]pOR3,
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
5. Соединения по п. 1, в которых
Ar1 представляет собой фенил или нафтил,
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
6. Соединения по п. 1, в которых
Het представляет собой моно- и бициклический ароматический гетероцикл, содержащий от 1 до 4 атомов N, О и/или S, который является незамещенным или моно- или дизамещенным посредством Hal, A, [C(R3)2]nOA', S(O)nA, CN, SO2N(R3)2 и/или COHet1,
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
7. Соединения по п. 1, в которых
Het1 представляет собой моноциклический насыщенный гетероцикл, содержащий от 1 до 4 атомов N, О и/или S, который является незамещенным или моно- или дизамещенным посредством А,
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
8. Соединения по п. 1, в которых
Het представляет собой фурил, тиенил, пирролил, имидазолил, пиразолил, оксазолил, изоксазолил, тиазолил, изотиазолил, пиридил, пиримидинил, триазолил, тетразолил, оксадиазолил, тиадиазолил, пиридазинил, пиразинил, бензоксазолил, бензотиазолил, бензимидазолил, бензотриазолил, индолил, бензо-1,3-диоксолил, бензодиоксанил, бензотиадиазолил, индазолил, бензофуранил, хинолил, изохинолил, оксазоло[5,4-b]пиридил, имидазо[1,2-а]пиридинил или оксазоло[5,4-с]пиридил, каждый из которых является незамещенным или моно- или дизамещенным посредством Hal, A, [C(R3)2]nOA', S(O)nA, CN, SO2N(R3)2 и/или COHet1,
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
9. Соединения по п. 1, в которых
Het1 представляет собой пирролидинил, азетидинил, оксетанил, тетрагидроимидазолил, тетрагидропиразолил, тетрагидрофуранил, пиперидинил, пиперазинил, морфолинил, гексагидропиридазинил, гексагидропиримидинил, [1,3]диоксоланил или тетрагидропиранил, каждый из которых является незамещенным или моно- или дизамещенным посредством А,
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
10. Соединения по п. 1, в которых
R представляет собой Ar, Het, -С≡С-Ar или -C≡C-Het,
W представляет собой NR2R2' или Het1,
R1 представляет собой A, [C(R3)2]nAr1 или [C(R3)2]nCyc,
R2, R2' каждый, независимо друг от друга, представляет собой Н, А или [C(R3)2]nCyc,
R4 представляет собой Н, F, Cl, OA' или А',
X1, X2, X3, X4 каждый, независимо друг от друга, представляет собой СН или N,
А представляет собой неразветвленный или разветвленный алкил с 1-10 атомами С, в котором одна или две не расположенные рядом СН- и/или СН2-группы могут быть заменены на атомы N и/или О и 1-7 атомов Н могут быть заменены на R5,
Cyc представляет собой циклоалкил с 3-7 атомами С, который является замещенным или монозамещенным посредством ОН или А,
А' представляет собой неразветвленный или разветвленный алкил с 1-6 атомами С, в котором 1-5 атомов Н могут быть заменены на F,
R5 представляет собой F, Cl или ОН,
Ar представляет собой фенил, который является незамещенным или моно-, ди-, три-, тетра- или пентазамещенным посредством O[C(R3)2]nHet1, Ar1, A, CN и/или [C(R3)2]pOR3,
Ar1 представляет собой фенил или нафтил,
R3 представляет собой Н или неразветвленный или разветвленный алкил с 1-6 атомами С,
Het представляет собой фурил, тиенил, пирролил, имидазолил, пиразолил, оксазолил, изоксазолил, тиазолил, изотиазолил, пиридил, пиримидинил, триазолил, тетразолил, оксадиазолил, тиадиазолил, пиридазинил, пиразинил, бензоксазолил, бензотиазолил, бензимидазолил, бензотриазолил, индолил, бензо-1,3-диоксолил, бензодиоксанил, бензотиадиазолил, индазолил, бензофуранил, хинолил, изохинолил, оксазоло[5,4-b]пиридил, имидазо[1,2-а]пиридинил или оксазоло[5,4-с]пиридил, каждый из которых является незамещенным или моно- или дизамещенным посредством Hal, A, [C(R3)2]nOA', S(O)nA, CN, SO2N(R3)2 и/или COHet1,
Het1 представляет собой пирролидинил, азетидинил, оксетанил, тетрагидроимидазолил, тетрагидропиразолил, тетрагидрофуранил, пиперидинил, пиперазинил, морфолинил, гексагидропиридазинил, гексагидропиримидинил, [1,3]диоксоланил или тетрагидропиранил, каждый из которых является незамещенным или моно- или дизамещенным посредством А,
Hal представляет собой F, Cl, Br или I,
n представляет собой 0, 1 или 2,
р представляет собой 0, 1, 2, 3 или 4,
q 0, 1, 2 или 3,
при условии, что только один или два из X1, X2, X3, X4 представляют собой N,
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
11. Соединения по п. 1, выбранные из группы:
Figure 00000002
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, включая их смеси во всех соотношениях.
12. Способ получения соединений формулы I по пп. 1-11 и их фармацевтически приемлемых солей, таутомеров и стереоизомеров, отличающийся тем, что
соединение формулы II
Figure 00000008
в которой R1 и W имеют значения, указанные в пункте 1,
вводят в реакцию с соединением формулы III
Figure 00000009
в которой R, R4, X1, X2, X3, X4 и q имеют значения, указанные в пункте 1,
и L представляет собой Cl, Br, I или свободную или реакционноспособную функционально модифицированную ОН-группу,
и/или
основание или кислоту формулы I превращают в одну из его солей.
13. Лекарственные средства, которые содержат, по меньшей мере, одно соединение формулы I и/или их фармацевтически приемлемые соли, таутомеры и стереоизомеры, в том числе их смеси во всех соотношениях, и, необязательно, фармацевтически приемлемый носитель, наполнитель или вспомогательное вещество.
14. Соединения формулы I и их фармацевтически приемлемые соли, таутомеры и стереоизомеры, в том числе их смеси во всех соотношениях, для применения для лечения и/или профилактики рака, рассеянного склероза, сердечно-сосудистых заболеваний, поражений центральной нервной системы и различных форм воспаления.
15. Соединения по п. 14 для применения для лечения и/или профилактики заболеваний, выбранных из группы, включающей рак головы, шеи, глаза, рта, горла, пищевода, бронхов, гортани, глотки, груди, костей, легких, толстой кишки, прямой кишки, желудка, предстательной железы, мочевого пузыря, матки, шейки матки, молочной железы, яичников, яичек или других репродуктивных органов, кожи, щитовидной железы, крови, лимфатических узлов, почек, печени, поджелудочной железы, головного мозга, центральной нервной системы, солидные опухоли и злокачественные перерождения крови.
16. Лекарственные средства, которые содержат, по меньшей мере, одно соединение формулы I и/или его фармацевтически приемлемые соли, таутомеры и стереоизомеры, в том числе их смеси во всех соотношениях, и по меньшей мере один дополнительный активный компонент лекарственного средства.
17. Комплект (набор), состоящий из отдельных пакетов, включающих
(а) эффективное количество соединения формулы I и/или его фармацевтически приемлемых солей, таутомеров и стереоизомеров, включая их смеси во всех соотношениях,
и
(б) эффективное количество еще одного активного компонента лекарственного средства.
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JP6316835B2 (ja) 2018-04-25
ZA201504323B (en) 2017-09-27
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JP2016504280A (ja) 2016-02-12
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CN104797553A (zh) 2015-07-22
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KR20150085045A (ko) 2015-07-22
WO2014075754A1 (en) 2014-05-22
BR112015010512A2 (pt) 2017-07-11
AR093461A1 (es) 2015-06-10
EP2920146B1 (en) 2016-09-28
CN104797553B (zh) 2017-07-21

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