RU2013122834A - Соединения, композиции и способы, подходящие для мобилизации холестерина - Google Patents

Соединения, композиции и способы, подходящие для мобилизации холестерина Download PDF

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RU2013122834A
RU2013122834A RU2013122834/04A RU2013122834A RU2013122834A RU 2013122834 A RU2013122834 A RU 2013122834A RU 2013122834/04 A RU2013122834/04 A RU 2013122834/04A RU 2013122834 A RU2013122834 A RU 2013122834A RU 2013122834 A RU2013122834 A RU 2013122834A
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alkyl
compound
subject
pharmaceutically acceptable
acceptable salt
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RU2013122834/04A
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RU2576402C2 (ru
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Даниела Кармен ОНИСИЮ
Жан-Луи Анри ДАССЕ
Рональд БАРБАРА
Валерий КОЧУБЕЙ
Дмитрий КОВАЛЬСКИЙ
Олег Геннадьевич РОДИН
Отто ЖОФФРУА
Анна РЗЕПИЛА
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Серенис Терапьютикс Холдинг Са
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Abstract

1. Соединение Формулы (II):или его фармацевтически приемлемая соль, гдекаждый Rнезависимо представляет собой -Н, -гидрокарбил, арил, -аралкил, -гетероарил, -гетероциклил, -С(О)О(алкил), -ОС(O)(алкил), -C(O)NH, -С(О)NH(алкил), -С(О)N(алкил)(алкил), -NHC(O)(алкил), N(алкил)С(O)(алкил) или -SONH;каждый Rнезависимо представляет собой -Н, -ОН, -NH, -NH(алкил), -N(алкил)(алкил), гидрокарбил, -O-алкил, -O-алкенил, арил, -O-арил, аралкил, -O-аралкил, гетероарил, -O-гетероарил, гетероциклил, -O-гетероциклил, галоген, -OCF, -С(О)О(алкил), -ОС(О)(алкил), -C(O)NH, -С(О)NH(алкил), -С(О)N(алкил)(алкил), NHC(O)(С-С-алкил), N(алкил)С(О)(алкил), -ОС(О)О(алкил), -OC(O)NH, -ОС(О)NH(алкил), -ОС(О)N(алкил)(алкил), -CHNH, -CHN(алкил) или -SONH;каждый из Q, Qи Qнезависимо представляет собой CRили N;Х представляет собой CHR, S, О или NR; икаждый m независимо представляет собой целое число от 0 до 3.2. Соединение или фармацевтически приемлемая соль по п.1, отличающиеся тем, что Rпредставляет собой Н, а Rпредставляет собой ОН;3. Соединение или фармацевтически приемлемая соль по п.2, отличающееся тем, что каждый m равен 1.4. Соединение по п.1, отличающееся тем, что соединение представляет собой:или фармацевтически приемлемую соль любого из приведенных выше соединений.5. Композиция, содержащая эффективное количество соединения или фармацевтически приемлемой соли соединения по п.1 и фармацевтически приемлемый наполнитель или носитель.6. Композиция по п.5, отличающаяся тем, что указанная композиция приготовлена в форме для перорального введения.7. Композиция по п.5, отличающаяся тем, что указанная композиция находится в форме таблетки или капсулы.8. Композиция по п.5, отличающаяся тем, что соединение или его соль присутствуют в количестве от примерно 1 мг до п�

Claims (28)

1. Соединение Формулы (II):
Figure 00000001
или его фармацевтически приемлемая соль, где
каждый R9 независимо представляет собой -Н, -гидрокарбил, арил, -аралкил, -гетероарил, -гетероциклил, -С(О)О(алкил), -ОС(O)(алкил), -C(O)NH2, -С(О)NH(алкил), -С(О)N(алкил)(алкил), -NHC(O)(алкил), N(алкил)С(O)(алкил) или -SO2NH2;
каждый R10 независимо представляет собой -Н, -ОН, -NH2, -NH(алкил), -N(алкил)(алкил), гидрокарбил, -O-алкил, -O-алкенил, арил, -O-арил, аралкил, -O-аралкил, гетероарил, -O-гетероарил, гетероциклил, -O-гетероциклил, галоген, -OCF3, -С(О)О(алкил), -ОС(О)(алкил), -C(O)NH2, -С(О)NH(алкил), -С(О)N(алкил)(алкил), NHC(O)(С2-С10-алкил), N(алкил)С(О)(алкил), -ОС(О)О(алкил), -OC(O)NH2, -ОС(О)NH(алкил), -ОС(О)N(алкил)(алкил), -CHNH, -CHN(алкил) или -SO2NH2;
каждый из Q1, Q2 и Q3 независимо представляет собой CR10 или N;
Х представляет собой CHR10, S, О или NR9; и
каждый m независимо представляет собой целое число от 0 до 3.
2. Соединение или фармацевтически приемлемая соль по п.1, отличающиеся тем, что R9 представляет собой Н, а R10 представляет собой ОН;
3. Соединение или фармацевтически приемлемая соль по п.2, отличающееся тем, что каждый m равен 1.
4. Соединение по п.1, отличающееся тем, что соединение представляет собой:
Figure 00000002
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
Figure 00000011
Figure 00000012
или фармацевтически приемлемую соль любого из приведенных выше соединений.
5. Композиция, содержащая эффективное количество соединения или фармацевтически приемлемой соли соединения по п.1 и фармацевтически приемлемый наполнитель или носитель.
6. Композиция по п.5, отличающаяся тем, что указанная композиция приготовлена в форме для перорального введения.
7. Композиция по п.5, отличающаяся тем, что указанная композиция находится в форме таблетки или капсулы.
8. Композиция по п.5, отличающаяся тем, что соединение или его соль присутствуют в количестве от примерно 1 мг до примерно 1000 мг.
9. Способ лечения нарушения метаболизма липопротеинов, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
10. Способ по п.9, отличающийся тем, что нарушение метаболизма липопротеинов представляет собой дислипидемию, дислипопротеинемию, избыточную выработку или дефицит липопротеинов, повышение уровня общего холестерина, повышение концентрации липопротеинов низкой плотности, повышение концентрации триглицеридов, выведение липидов в желчь, метаболическое нарушение, выведение фосфолипидов в желчь, выведение оксистерола в желчь или нарушение, связанное с рецептором, активируемым пролифератором пероксисом.
11. Способ лечения нарушения метаболизма глюкозы, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
12. Способ по п.11, отличающийся тем, что нарушение метаболизма глюкозы представляет собой инсулинорезистентность, нарушенную переносимость глюкозы, аномальный уровень глюкозы в крови натощак, сахарный диабет, липодистрофию, центральное ожирение, периферическую липоатрофию, диабетическую нефропатию, диабетическую ретинопатию, заболевания почек или септицемию.
13. Способ лечения сердечно-сосудистого нарушения, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
14. Способ по п.13, отличающийся тем, что сердечно-сосудистое нарушение или родственные сосудистые нарушения представляют собой гипертензию, ишемическую болезнь сердца, инфаркт миокарда, аритмию, мерцание предсердий, заболевания сердечного клапана, сердечную недостаточность, кардиомиопатию или перикардит.
15. Способ по п.13, отличающийся тем, что указанный способ обеспечивает ослабление по меньшей мере одного симптома сердечно-сосудистого нарушения.
16. Способ по п.15, отличающийся тем, что указанный симптом представляет собой импотенцию.
17. Способ лечения воспаления, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
18. Способ лечения ишемического некроза, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
19. Способ лечения рака толстой кишки, рака легкого, рака груди или рака кожи, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
20. Способ лечения тромботического нарушения, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
21. Способ лечения болезни Альцгеймера, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
22. Способ лечения болезни Паркинсона, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
23. Способ лечения панкреатита, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
24. Способ лечения воспаления поджелудочной железы, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
25. Способ лечения аномальной выработки желчи, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения или фармацевтически приемлемой соли соединения по п.1.
26. Способ отслеживания хода лечения сердечно-сосудистого нарушения у субъекта, включающий:
а. определение уровня свободного холестерина в липопротеинах высокой плотности в крови субъекта;
b. введение субъекту соединения по п.1;
с. отслеживание уровня свободного холестерина в крови субъекта в течение периода времени после введения соединения; и
d. оценку уровня улучшения состояния субъекта на основании сравнения результатов, полученных на стадиях а. и с.
27. Способ по п.26, отличающийся тем, что сердечно-сосудистое нарушение представляет собой обратный транспорт холестерина от артерии к печени или выведение холестерина в желчные кислоты.
28. Способ определения уровня активности P2Y13 у субъекта, включающий:
а. определение уровня свободного холестерина в липопротеинах высокой плотности в крови субъекта;
b. введение субъекту соединения по п.31;
с. отслеживание уровня свободного холестерина в крови субъекта в течение периода времени после введения соединения; и
d. оценку уровня активности P2Y13 у субъекта на основании сравнения результатов, полученных на стадиях а. и с.
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