RU2017122971A - Новые производные peg - Google Patents

Новые производные peg Download PDF

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RU2017122971A
RU2017122971A RU2017122971A RU2017122971A RU2017122971A RU 2017122971 A RU2017122971 A RU 2017122971A RU 2017122971 A RU2017122971 A RU 2017122971A RU 2017122971 A RU2017122971 A RU 2017122971A RU 2017122971 A RU2017122971 A RU 2017122971A
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RU2697551C2 (ru
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Киеси ЕСИМА
Масаказу ФУКУСИМА
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Дельта-Флай Фарма, Инк.
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Claims (20)

1. Соединение формулы (1) или его соль:
Figure 00000001
,
где R1 представляет собой простую связь, -N(R3)(CH2)n1CO- или -N(R4)(CH2)n2N(R5)CO(CH2)n3CO- (где R3 представляет собой атом водорода или алкильную группу; R4 и R5, которые являются одинаковыми или отличаются друг от друга, каждый представляет собой атом водорода или алкильную группу, или R4 и R5 связаны вместе и представляют собой алкиленовую группу, имеющую 1-4 атома углерода; и n1, n2 и n3, которые являются одинаковыми или отличаются друг от друга, каждый равен целому числу от 1 до 3;
R2 представляет собой группу формул (a), (b), (c), (d), (e) или (f):
Figure 00000002
Figure 00000003
Figure 00000004
,
где R6 представляет собой гидроксильную группу, цианогруппу или атом галогена; R7 представляет собой атом водорода или атом галогена; R8 представляет собой атом водорода или этинильную группу; R9 и R10, которые являются одинаковыми или отличаются друг от друга, каждый представляет собой атом водорода или триалкилсилильную группу, или R9 и R10 связаны вместе и представляют собой тетраалкилсилоксисилильную группу; R11 представляет собой атом галогена или этинильную группу; R12 представляет собой атом водорода или атом галогена; R13 представляет собой алкильную группу или алкоксиалкильную группу; R14 представляет собой алкоксиалкильную группу или морфолиноалкильную группу; R15 представляет собой алкильную группу; и R16 представляет собой атом водорода или алканоильную группу;
m равен числу от 10 до 1000; и
стрелка обозначает место связывания.
2. Соединение по п.1 или его соль, где R2 представляет собой группу формулы (a) или (b).
3. Соединение по п.1 или 2 или его соль, где R2 представляет собой группу формулы (a).
4. Соединение по любому из пп.1-3 или его соль, где R2 представляет собой группу формулы (a); R6 представляет собой гидроксильную группу или атом галогена; R7 представляет собой атом водорода или атом галогена; R8 представляет собой атом водорода, цианогруппу или этинильную группу; и R9 и R10, оба представляют собой атом водорода.
5. Соединение по любому из пп.1-4 или его соль, где R1 представляет собой простую связь, -NH(CH2)n1CO-, -NH(CH2)n2NHCO(CH2)n3CO- или следующую формулу:
Figure 00000005
,
где n1, n2 и n3 имеют такие же значения, как определено выше, соответственно.
6. Лекарственное средство, содержащее соединение по любому из пп.1-5 или его соль.
7. Лекарственное средство по п.6, где указанное лекарственное средство представляет собой терапевтическое средство против злокачественной опухоли.
8. Фармацевтическая композиция, содержащая соединение по любому из пп.1-5 или его соль и фармацевтически приемлемую соль.
9. Применение соединения по любому из пп.1-5 или его соли для изготовления терапевтического средства для лечения злокачественной опухоли.
10. Соединение по любому из пп.1-5 или его соль, для применения при лечении злокачественной опухоли.
11. Способ лечения злокачественной опухоли, включающий введение эффективного количества соединения по любому из пп.1-5 или его соли.
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