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RU2506256C2 - Лиганды для визуализации иннервации сердца - Google Patents

Лиганды для визуализации иннервации сердца Download PDF

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RU2506256C2
RU2506256C2 RU2009128591/04A RU2009128591A RU2506256C2 RU 2506256 C2 RU2506256 C2 RU 2506256C2 RU 2009128591/04 A RU2009128591/04 A RU 2009128591/04A RU 2009128591 A RU2009128591 A RU 2009128591A RU 2506256 C2 RU2506256 C2 RU 2506256C2
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Эджей ПЬЮРОХИТ
Томас Д. ХЭРРИС
Хайке С. РАДЕКЕ
Саймон П. РОБИНСОН
Мин Ю
Дэвид С. КЕЙСБИР
Майкл Т. ЭЖЕР
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Abstract

Изобретение относится к новым соединениям, пригодным для визуализации иннервации сердца, структурной формулы
Figure 00000079
где n=0, R и R1 независимо выбраны из группы, состоящей из H, (C1-C4)алкила, NR4(C(=NR5)NHR6, NR4C(=O)N(R5)2; R2 отсутствует; R3 представляет собой Н; R4, R5 и R6 независимо выбраны из группы, состоящей из H и (C1-C8)алкила; или любые два из R4, R5 и R6 могут образовывать циклическую структуру, состоящую из -CH2-CH2- или -CH=CH-; W и X независимо выбраны из группы, состоящей из H и Br; и A отсутствует; если соединение содержит связующую группу Q между Y и Z, Y и Z независимо выбираются из группы, состоящей из CH и NR7, и Q представляет собой CH, a R7 представляет собой (C1-C8)алкил, или если связующая группа Q отсутствует между Y и Z, Y и Z независимо выбраны из группы, состоящей из H, OR4, Cl, Br, (C6-C10)арила и CF3; где один или более из R4, R5, R6 или R7 могут быть замещены визуализирующим фрагментом; при условии, что по меньшей мере один визуализирующий фрагмент находится в любой группе Y или Z, когда Y или Z представляет собой OR4, или в R7, или в R5, или R6, когда R или R1 представляет собой NR4(C(=NR5)NHR6, и представляет собой 18F. Изобретение также относится к способу визуализации иннервации сердца и применению соединений для изготовления средства для визуализации иннервации сердца. 4 н. и 16 з.п. ф-лы, 2 ил., 2 табл., 25 пр.

Description

Текст описания приведен в факсимильном виде.
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Claims (20)

1. Соединение, имеющее следующую формулу:
Figure 00000067

где n=0,
R и R1 независимо выбраны из группы, состоящей из Н, (C1-C4)алкила, NR4(C(=NR5)NHR6, NR4C(=O)N(R5)2;
R2 отсутствует;
R3 представляет собой H;
R4, R5 и R6 независимо выбраны из группы, состоящей из H и (C1-C8)алкила;
при этом возможно, что любые два из R4, R5 и R6 могут образовывать циклическую структуру, состоящую из -CH2-CH2- или -CH=CH-;
W и X независимо выбраны из группы, состоящей из H и Br; и
A отсутствует;
причем, если соединение содержит связующую группу Q между Y и Z, Y и Z независимо выбираются из группы, состоящей из CH и NR7, и Q представляет собой CH, a R7 представляет собой (C1-C8)алкил, или
если связующая группа Q отсутствует между Y и Z, Y и Z независимо выбраны из группы, состоящей из H, OR4, Cl, Br, (C6-C10)арила и CF3; где
один или более из R4, R5, R6 или R7 могут быть замещены визуализирующим фрагментом;
при условии, что по меньшей мере один визуализирующий фрагмент находится в любой группе Y или Z, когда Y или Z представляет собой OR4, или в R7, или в R5 или R6 когда R или R1 представляет собой NR4(C(=NR5)NHR6, и представляет собой 18F;
или его соль.
2. Соединение по п.1, где R представляет собой NR4(C(=NR5)NHR6.
3. Соединение по п.2, где R4, R5 и R6, каждый, представляют собой H.
4. Соединение по п.1, где W и X, каждый, представляет собой H.
5. Соединение по п.1, где Z представляет собой OR4.
6. Соединение по п.5, где R4 представляет собой (C1-C8)алкил, замещенный 18F.
7. Соединение по п.1, где Z представляет собой (C6-C10)арил, замещенный l8F.
8. Соединение по п.1, где любые два из R4, R5 или R6 образуют циклическую структуру, состоящую из -CH2-CH2- или -CH=CH-.
9. Соединение по п.1, где:
X, W, R3 и R1 представляют собой Н;
R представляет собой NHC(=NH)NH2;
Z представляет собой OR4;
R4 представляет собой (C1-C8)алкил, замещенный 18F; и
Y представляет собой H, CF3, Cl или Br, или его соль.
10. Соединение по п.1, которое имеет структурную формулу, выбранную из группы, состоящей из:
Figure 00000068
Figure 00000069

Figure 00000070
Figure 00000071

или его соль.
11. Соединение по п.1, которое имеет структурную формулу, выбранную из группы, состоящей из:
Figure 00000072
Figure 00000073
и
Figure 00000074

или его соль.
12. Соединение по п.1, которое имеет структурную формулу:
Figure 00000075
,
или его соль.
13. Соединение по п.1, которое представляет собой N-[3-бpoм-4(3-[18F]фторпропокси)-бензил]-гуанидина гидрохлорид.
14. Соединение, имеющее формулу:
Figure 00000076

где n=1;
R, R1 и R2 независимо выбраны из группы, состоящей из H, (C1-C4)алкила, C(=NR4)NHR5 и NR4C(=NR5)NHR6;
R3 представляет собой H;
где R4, R5 и R6 выбраны из группы, состоящей из H и (C1-C8)алкила; при этом возможно, что любые два из R4, R5 и R6 могут образовывать циклическую структуру, состоящую из -CH=CH-;
W и X представляют собой Н;
Y выбран из группы, состоящей из H, OR4, O и Br;
Z представляет собой OR4, где R4 содержит по меньшей мере один 18F;
A представляет собой O или отсутствует, или его соль.
15. Соединение по п.14, где R обозначает NR4(C(=NR5)NHR6.
16. Соединение по п.15, где R4, R5 и R6, каждый, представляет собой H.
17. Соединение по п.14, где любые два из R4, R5 или R6 образуют циклическую структуру, состоящую из -CH=CH-.
18. Соединение по п.14, имеющее структуру, выбранную из группы, состоящей из:
Figure 00000077
и
Figure 00000078

или его соль.
19. Способ визуализации иннервации сердца, включающий стадии: введения эффективного количества соединения по пп.1-18 пациенту; выявления гамма-излучения, излучаемого указанным соединением; и формирования его изображения.
20. Применение соединения по любому из пп.1-18 для изготовления средства для визуализации иннервации сердца.
RU2009128591/04A 2006-12-26 2007-12-21 Лиганды для визуализации иннервации сердца RU2506256C2 (ru)

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