RU2004117874A - Производные соединения карбоновой кислоты и средства, содержащие соединения в качестве активных ингредиентов - Google Patents

Производные соединения карбоновой кислоты и средства, содержащие соединения в качестве активных ингредиентов Download PDF

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RU2004117874A
RU2004117874A RU2004117874/04A RU2004117874A RU2004117874A RU 2004117874 A RU2004117874 A RU 2004117874A RU 2004117874/04 A RU2004117874/04 A RU 2004117874/04A RU 2004117874 A RU2004117874 A RU 2004117874A RU 2004117874 A RU2004117874 A RU 2004117874A
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allyl
ethoxy
benzyl
amino
acetic acid
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RU2296760C2 (ru
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Хисао ТАДЗИМА (JP)
Хисао ТАДЗИМА
Есисуке НАКАЯМА (JP)
Есисуке НАКАЯМА
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Оно Фармасьютикал Ко., Лтд. (Jp)
Оно Фармасьютикал Ко., Лтд.
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Claims (16)

1. Производное соединения карбоновой кислоты, представленное формулой (I)
Figure 00000001
где X и Y, каждый независимо, представляет собой C1-4 алкилен;
Z означает -O- или -S-;
R1, R2, R3 и R4, каждый независимо, означает атом водорода, или C1-8 алкил;
R5 означает C2-8 алкенил;
A означает -O- или -S-;
D является D1, D2, D3, D4 или D5;
D1 означает C1-8 алкил;
D2 является
Figure 00000002
кольцо 1 является насыщенным 3-7-членным моногетероарилом, содержащим один атом азота и, необязательно, другой один гетероатом, выбранный из атома кислорода, серы и азота;
D3 является
Figure 00000003
кольцо 2 является
(1) необязательно, частично или полностью насыщенным С3-10 моно- или бикарбоциклическим арилом, или
(2) необязательно, частично или полностью насыщенным 3-10-членным моно- или бигетероарилом, содержащим 1-4 гетероатома, выбранного из атомов кислорода, азота и серы;
D4 является
Figure 00000004
D5 является
Figure 00000005
R6 представляет собой (1) атом водорода, (2) C1-8 алкил, (3) C1-8 алкокси, (4) CF3, (5) OCF3, (6) атом галогена, (7) нитро или (8) NR7R8;
R7 или R8 представляют собой атом водорода или C1-8 алкил, или
R7 и R8, взятые вместе с атомом азота, к которому они присоединены, образуют насыщенный 3-7-членный моногетероарил, содержащий один атом азота и, необязательно, другой один гетероатом, выбранный из атомов кислорода, серы и азота, и насыщенный гетероарил, необязательно, является замещенным С1-8 алкилом;
E означает CH или атом азота; и
m равно целому числу 1-3, или
его нетоксичная соль.
2. Соединение по п.1, где Z является -S-.
3. Соединение по п.1, где Z является -O- и D является D1, D2 D3 или D4.
4. Соединение по п.1, где D является D1.
5. Соединение по п.1, где D является D2.
6. Соединение по п.1, где D является D3.
7. Соединение по п.1, где D является D4.
8. Соединение по п.1, где D является D5.
9. Соединение по п.4, которое представляет собой
(1) этиловый эфир 2-(N-аллил-N-(3-(2-(2-изопропил-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты, или
(2) 2-(N-аллил-N-(3-(2-(2-изопропил-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту.
10. Соединение по п.5, которое представляет собой
(1) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(4-метилпиперазин-1-ил)-5-метилтиазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(2) этиловый эфир 2-(N-аллил-N-(3-(2-(5-метил-2-пиперидинотиазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(3) трет-бутиловый эфир 2-(N-аллил-N-(3-(2-(2-морфолино-5-метилтиазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(4) 2-(N-аллил-N-(3-(2-(2-(4-метилпиперазин-1-ил)-5-метилтиазол-4-ил)этокси)бензил)амино)уксусную кислоту,
(5) 2-(N-аллил-N-(3-(2-(5-метил-2-пиперидинотиазол-4-ил)этокси)бензил)амино)уксусную кислоту или
(6) 2-(N-аллил-N-(3-(2-(5-метил-2-морфолинотиазол-4-ил)этокси)бензил)амино)уксусную кислоту.
11. Соединение по п.6, которое представляет собой
(1) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(4-(1,2,3-тиадиазол-4-ил)фенил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(2) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(4-циклогексилфенил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(3) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(4-(тетрагидропиран-4-ил)фенил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(4) 2-(N-аллил-N-(3-(2-(2-(4-(1,2,3-тиадиазол-4-ил)фенил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту,
(5) 2-(N-аллил-N-(3-(2-(2-(4-циклогексилфенил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту, или
(6) 2-(N-аллил-N-(3-(2-(2-(4-(тетрагидропиран-4-ил)фенил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту.
12. Соединение по п.7, которое представляет собой
(1) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(6-(пергидроазепин-1-ил)пиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты, или
(2) 2-(N-аллил-N-(3-(2-(2-(6-(пергидроазепин-1-ил)пиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту.
13 Соединение по п.8, которое представляет собой
(1) этиловый эфир 2-(N-аллил-N-(3-(2-(2-фенил-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(2) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(6-диметиламинопиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(3) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(4-диметиламинофенил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(4) метиловый эфир 2-(N-аллил-N-(3-(2-(5-метил-2-фенилоксазол-4-ил)этокси)бензил)амино)-2-метилпропионовой кислоты,
(5) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(6-морфолинопиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(6) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(6-пиперидинопиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(7) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(6-диэтиламинопиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(8) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(6-пирролидинопиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(9) этиловый эфир 2-(N-аллил-N-(3-(2-(2-(4-морфолинофенил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(10) этиловый эфир 2-(N-аллил-N-(4-(2-(5-метил-2-фенилоксазол-4-ил)этокси)бензил)амино)уксусной кислоты,
(11) 2-(N-аллил-N-(3-(2-(5-метил-2-фенилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту,
(12) 2-(N-аллил-N-(3-(2-(2-(6-диметиламинопиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту,
(13) 2-(N-аллил-N-(3-(2-(2-(4-диметиламинофенил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту,
(14) 2-(N-аллил-N-(3-(2-(2-фенил-5-метилоксазол-4-ил)этокси)бензил)амино)-2-метилпропионовую кислоту,
(15) 2-(N-аллил-N-(3-(2-(2-(6-морфолинопиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту,
(16) 2-(N-аллил-N-(3-(2-(2-(6-пиперидинопиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту,
(17) 2-(N-аллил-N-(3-(2-(2-(6-диэтиламинопиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту,
(18) 2-(N-аллил-N-(3-(2-(2-(6-пирролидинопиридин-3-ил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту,
(19) 2-(N-аллил-N-(3-(2-(2-(4-морфолинофенил)-5-метилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту, или
(20) 2-(N-аллил-N-(4-(2-(5-метил-2-фенилоксазол-4-ил)этокси)бензил)амино)уксусную кислоту.
14. Регулятор активируемого пероксисомным пролифератором рецептора, включающий в себя, в качестве активного ингредиента, соединение, представленное формулой (I) согласно п.1, или его нетоксичную соль.
15. Средство для профилактики и/или лечения заболеваний, связанных с нарушениями метаболизма, таких как диабет, ожирение, синдром Х, гиперхолестеринемия или гиперлипопротеинемия, гиперлипидемия, атеросклероз, гипертензия, болезни, протекающие с расстройством кровообращения, переедание или ишемическая болезнь сердца, которое содержит, в качестве активного ингредиента, соединение, представленное формулой (I) согласно п.1, или его нетоксичную соль.
16. Средство, которое повышает уровень холестерина, связанного с HDL, снижает уровень холестерина, связанного с LDL и/или VLDL, устраняет фактор риска появления диабета и/или синдрома Х, содержащее, в качестве активного ингредиента, соединение, представленное формулой (I) согласно п.1, или его нетоксичную соль.
RU2004117874/04A 2001-11-12 2002-11-11 Производные соединения карбоновой кислоты и средства, содержащие соединения в качестве активных ингредиентов RU2296760C2 (ru)

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