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RU2199534C2 - СОЕДИНЕНИЕ ПИПЕРАЗИНА, ИНГИБИТОР ПРОДУЦИРОВАНИЯ TNF-α И /ИЛИ ПРОМОТОР ПРОДУЦИРОВАНИЯ IL-10 И СРЕДСТВО ДЛЯ ПРОФИЛАКТИКИ ИЛИ ЛЕЧЕНИЯ БОЛЕЗНЕЙ НА ЕГО ОСНОВЕ - Google Patents

СОЕДИНЕНИЕ ПИПЕРАЗИНА, ИНГИБИТОР ПРОДУЦИРОВАНИЯ TNF-α И /ИЛИ ПРОМОТОР ПРОДУЦИРОВАНИЯ IL-10 И СРЕДСТВО ДЛЯ ПРОФИЛАКТИКИ ИЛИ ЛЕЧЕНИЯ БОЛЕЗНЕЙ НА ЕГО ОСНОВЕ Download PDF

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RU2199534C2
RU2199534C2 RU2000112020/04A RU2000112020A RU2199534C2 RU 2199534 C2 RU2199534 C2 RU 2199534C2 RU 2000112020/04 A RU2000112020/04 A RU 2000112020/04A RU 2000112020 A RU2000112020 A RU 2000112020A RU 2199534 C2 RU2199534 C2 RU 2199534C2
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Russia
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different
hydrogen
lower alkyl
methyl
acetamide
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RU2000112020/04A
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RU2000112020A (ru
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Кунитомо АДАТИ (JP)
Кунитомо АДАТИ
Токуси ХАНАНО (JP)
Токуси Ханано
Хироси МОРИМОТО (JP)
Хироси МОРИМОТО
Масао ХИСАДОМЕ (JP)
Масао ХИСАДОМЕ
Йосиюки АОКИ (JP)
Йосиюки АОКИ
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Мицубиси Фарма Корпорейшн
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Abstract

Описывается соединение пиперазина общей формулы I или его фармацевтически приемлемая соль, где R1 и R2 являются одинаковыми или различными и каждый обозначает водород, галоген, низший алкил, амино, амино, монозамещенный низшим ацилом; нитро, R3, R4 и R5-одинаковые или различные и каждый обозначает водород, галоген, низший алкил, низший алкокси, нитро, амино, гидрокси, амино, моно- или дизамещенный группой, которую выбирают из группы, включающей низший алкил или низший ацил; R6 и R7 - одинаковые или различные и каждый обозначает водород, ацил, R8 и R9 - одинаковые или различные и каждый обозначает водород или низший алкил, Y обозначает
Figure 00000001

где R10 и R11 обозначают водород, R12 и R13 - одинаковые или различные и каждый обозначает водород или низший алкил, либо R12 и R13 вместе образуют алкилен, R14 и R15 обозначают водород, m - целое число 0-2, n - целое число 0 - 2 и 0≤m+n≤2; цикл А обозначает фенил, пиримидинил, тиазолил, пиридил, пиразолил или имидазолил. Описывается также ингибитор продуцирования TNF-α и/или промотор продуцирования IL-10, содержащий в качестве активного ингредиента соединение формулы I или его фармацевтически приемлемую соль, и средство для профилактики или лечения болезней, вызванных аномальным продуцированием TNF-α, болезней, опосредованных TNF-α, или болезней, излечиваемых IL-10, содержащее в качестве активного ингредиента соединение формулы I или его фармацевтически приемлемую соль. 3 с. и 19 з.п. ф-лы, 2 табл.

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Claims (22)

1. Соединение пиперазина формулы
Figure 00000005

где R1 и R2 являются одинаковыми или различными и каждый обозначает водород, галоген, низший алкил, амино, амино, монозамещенный низшим ацилом; нитро;
R3, R4 и R5 являются одинаковыми или различными и каждый обозначает водород, галоген, низший алкил, низший алкокси, нитро, амино, гидрокси или амино, моно- или дизамещенный группой, которую выбирают из группы, включающей низший алкил и низший ацил;
R6 и R7 являются одинаковыми или различными и каждый обозначает водород, ацил;
R8 и R9 являются одинаковыми или различными и каждый обозначает водород или низший алкил;
Y обозначает группу формулы
Figure 00000006

где R10 и R11 обозначают водород, R12 и R13 являются одинаковыми или различными и каждый обозначает водород или низший алкил, либо R12 и R13 вместе образуют алкилен, R14 и R15 обозначают водород, m обозначает целое число 0-2, n обозначает целое число 0-2 и 0≤m+n≤2;
цикл А обозначает фенил, пиримидинил, тиазолил, пиридил, пиразолил или имидазолил,
или его фармацевтически приемлемая соль.
2. Соединение пиперазина по п.1, имеющее следующую формулу:
Figure 00000007

где R1 и R2 являются одинаковыми или различными и каждый обозначает водород, галоген, низший алкил, амино, амино, монозамещенный низшим ацилом; нитро;
R3, R4 и R5 являются одинаковыми или различными и каждый обозначает водород, галоген, низший алкил, низший алкокси, нитро, амино, гидрокси или амино, монозамещенный ацилом;
R6 и R7 являются различными и каждый обозначает водород, ацил;
Y1 обозначает группу формулы
Figure 00000008

где R12 и R13 являются одинаковыми или различными и каждый обозначает водород или низший алкил, либо R12 и R13 вместе образуют алкилен,
или его фармацевтически приемлемая соль.
3. Соединение пиперазина по п.1, имеющее следующую формулу:
Figure 00000009

где R1 и R2 обозначают водород;
R3, R4 и R5 являются одинаковыми или различными и каждый обозначает галоген;
R6 и R7 являются различными и каждый обозначает водород, ацил;
R8a обозначает алкил;
Y1 обозначает группу формулы
Figure 00000010

где R12 и R13 являются одинаковыми или различными и каждый обозначает водород или низший алкил, либо R12 и R13 вместе образуют алкилен,
или его фармацевтически приемлемая соль.
4. Соединение пиперазина по п.3, где R8a обозначает метил и его фармацевтически приемлемая соль.
5. Соединение пиперазина по п.1, имеющее следующую формулу:
Figure 00000011

где R1 и R2 обозначают водород;
R3, R4 и R5 являются одинаковыми или различными и каждый обозначает водород, галоген;
R6 и R7 являются различными и каждый обозначает водород, ацил;
R8a и R9a являются одинаковыми и каждый обозначает низший алкил;
Y1 обозначает группу формулы
Figure 00000012

где R12 и R13 обозначают водород,
или его фармацевтически приемлемая соль.
6. Соединение пиперазина по п.5, где R8a и R9a оба обозначают метил, или его фармацевтически приемлемая соль.
7. Соединение пиперазина по любому из пп.1-6, где R3, R4 и R5 являются одинаковыми или различными и каждый обозначает водород, галоген, или его фармацевтически приемлемая соль.
8. Соединение пиперазина по п.1, имеющее следующую формулу:
Figure 00000013

где R1 и R2 обозначают водород;
цикл А' обозначает группу формулы
Figure 00000014

Figure 00000015

Figure 00000016

Figure 00000017

Figure 00000018

или
Figure 00000019

где R16 и R17 являются одинаковыми или различными и каждый обозначает водород, галоген, низший алкил, низший алкокси или амино, дизамещенный низшим алкилом, R18 обозначает низший алкил;
R6 и R7 являются одинаковыми или различными и каждый обозначает водород, ацил;
Y1 обозначает группу формулы
Figure 00000020

где R12 и R13 являются одинаковыми или различными и каждый обозначает водород или низший алкил, либо R12 и R13 вместе образуют алкилен,
или его фармацевтически приемлемая соль.
9. Соединение пиперазина по п.1, имеющее следующую формулу:
Figure 00000021

где R1 и R2 обозначают водород;
цикл А' обозначает группу формулы
Figure 00000022

Figure 00000023

Figure 00000024

или
Figure 00000025

где R16 и R17 являются одинаковыми или различными и каждый обозначает водород, галоген, R18 обозначает низший алкил;
R6 и R7 являются различными и каждый обозначает водород, ацил;
R8a обозначает низший алкил;
Y1 обозначает группу формулы
Figure 00000026

где R12 и R13 являются одинаковыми или различными и каждый обозначает водород или низший алкил, либо R12 и R13 вместе образуют алкилен,
или его фармацевтически приемлемая соль.
10. Соединение пиперазина по п.9, где R8a обозначает метил, и его фармацевтически приемлемая соль.
11. Соединение пиперазина по любому из пп.1-10, где один из R6 и R7 обозначает водород, а другой обозначает ацил, или его фармацевтически приемлемая соль.
12. Соединение пиперазина по любому из пп.1-11, где R12 и R13 являются одинаковыми или различными и каждый обозначает водород или метил, либо R12 и R13 вместе образуют этилен, или его фармацевтически приемлемая соль.
13. Соединение пиперазина по любому из пп.1, 2, 7, 11 или 12, являющееся членом, выбираемым из группы, включающей
N-(4-((4-фенилпиперазин-1-ил)метил)фенилметил)ацетамид,
N-(4-((4-(4-фторфенил)пиперазин-1-ил)метил)фенилметил)-ацетамид,
N-(4-((4-(2-фторфенил)пиперазин-1-ил)метил)фенилметил)-ацетамид,
N-(4-((4-(2,4-дифторфенил)пиперазин-1-ил)метил)фенилметил)ацетамид,
N-(2-(4-((4-фенилпиперазин-1-ил)метил)фенил)этил)ацетамид,
N-(2-(4-((4-(4-фторфенил)пиперазин-1-ил)метил)фенил)этил)-ацетамид,
N-(1-(4-((4-фенилпиперазин-1-ил)метил)фенил)этил)ацетамид,
N-(1-(4-((4-(4-фторфенил)пиперазин-1-ил)метил)фенил)этил)-ацетамид,
N-(1-(4-((4-(2,4-дифторфенил)пиперазин-1-ил)метил)фенил)этил)ацетамид,
N-(1-(4-((4-(4-фторфенил)пиперазин-1-ил)метил)фенил)-1-метилэтил)ацетамид,
N-(1-(4-((4-фенилпиперазин-1-ил)метил)фенил)циклопропил)ацетамид и
N-(1-(4-((4-(4-фторфенил)пиперазин-1-ил)метил)фенил)-циклопропил)ацетамид,
или его фармацевтически приемлемая соль.
14. Соединение пиперазина по любому из пп.1, 3, 4, 7, 11 или 12, являющееся членом, выбираемым из группы, включающей
N-(4-(1-(4-фенилпиперазин-1-ил)этил)фенилметил)ацетамид,
N-(4-(1-(4-(4-фторфенил)пиперазин-1-ил)этил)фенилметил)ацетамид и
N-(4-(1-(4-(2,4-дифторфенил)пиперазин-1-ил)этил)фенилметил)ацетамид,
или его фармацевтически приемлемая соль.
15. Соединение пиперазина по любому из пп.1, 5-7, 11 или 12, которым является N-(4-(1-(4-(4-фторфенил)пиперазин-1-ил)-1-метилэтил)фенилметил)ацетамид, или его фармацевтически приемлемая соль.
16. Соединение пиперазина по любому из пп.1, 7, 8, 11 или 12, являющееся членом, выбранным из группы, включающей
N-(4-((4-(пиримидин-2-ил)пиперазин-1-ил)метил)фенилметил)ацетамид,
N-(1-(4-((4-(пиримидин-2-ил)пиперазин-1-ил)метил)фенил)-этил)ацетамид,
N-(1-(4-((4-(пиримидин-2-ил)пиперазин-1-ил)метил)фенил)-циклопропил)ацетамид,
N-(4-((4-(пиримидин-2-ил)пиперазин-1-ил)метил)фенилметил)формамид,
N-(4-((4-(пиримидин-2-ил)пиперазин-1-ил)метил)фенилметил)пропионамид,
N-(4-((4-(тиазол-2-ил)пиперазин-1-ил)метил)фенилметил)-ацетамид и
N-(4-((4-(пиридин-2-ил)пиперазин-1-ил)метил)фенилметил)-ацетамид,
или его фармацевтически приемлемая соль.
17. Соединение пиперазина по любому из пп.1, 7, 9, 10, 11 или 12, которым является N-(1-(4-(1-(4-(пиримидин-2-ил)пиперазин-1-ил)этил)фенил)циклопропил)ацетамид, или его фармацевтически приемлемая соль.
18. Ингибитор продуцирования TNF-α и/или промотор продуцирования IL-10, содержащий в качестве активного ингредиента соединение пиперазина по любому из пп.1-17 или его фармацевтически приемлемую соль.
19. Средство для профилактики или лечения болезней, вызванных аномальным продуцированием TNF-α, болезней, опосредованных TNF-α, или болезней, излечиваемых IL-10, содержащее в качестве активного ингредиента соединение пиперазина по любому из пп.1-17 или его фармацевтически приемлемую соль.
20. Средство по п.19, где болезнь представляет собой воспалительное заболевание.
21. Средство по п.19, где болезнь представляет собой аутоиммунное заболевание.
22. Средство по п.19, где болезнь представляет собой ревматоидный артрит.
Приоритеты по пунктам и признакам:
14.10.1997 - по пп.1-3, 5, 7, 12, 18-22 - при всех указанных значениях R1, R2, R6, R7, R8, Y, R10, R11, R14, R15, m, n; при R3 и R4 - одинаковые или различные и каждый обозначает водород, галоген, низший алкокси, амино или гидрокси; при R5 и R9 - водород; при R12 и R13 - одинаковые или различные и каждый обозначает водород или низший алкил; когда цикл А обозначает фенил; по п.4, 11, по п.13 - для всех указанных соединений, кроме двух последних по ходу изложения; по п.14 и 15;
16.09.1998 - по пп.1-3, 5, 7, 12, 18-22 - при R3 и R4 - одинаковые или различные и каждый обозначает нитро, амино, моно- или дизамещенный группой, которую выбирают из группы, включающей низший алкил и низший ацил; при R5 - галоген, низший алкокси, нитро, амино, гидрокси, амино, моно- или дизамещенный группой, которую выбирают из группы, включающей низший алкил и низший ацил; при R9 - низший алкил; при R12 и R13 вместе - алкилен; когда цикл А обозначает пиримидинил, тиазолил, пиридил, пиразолил или имидазолил; по п.6; 8-10; по п.13 - для последних двух по ходу изложения соединений; по пп.16 и 17.
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KR20010031122A (ko) 2001-04-16
AU744577B2 (en) 2002-02-28
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