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RU2016132759A - Дуокармициновые adc, демонстрирующие улучшенную противоопухолевую активность in vivo - Google Patents

Дуокармициновые adc, демонстрирующие улучшенную противоопухолевую активность in vivo Download PDF

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Publication number
RU2016132759A
RU2016132759A RU2016132759A RU2016132759A RU2016132759A RU 2016132759 A RU2016132759 A RU 2016132759A RU 2016132759 A RU2016132759 A RU 2016132759A RU 2016132759 A RU2016132759 A RU 2016132759A RU 2016132759 A RU2016132759 A RU 2016132759A
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use according
compound
her2
cancer
human solid
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RU2016132759A
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RU2016132759A3 (ru
RU2689779C2 (ru
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Виллем ДОКТЕР
Патрик Хенри БЕСКЕР
Петер Йоханнес ГУДИНГС
Гейсбертус Франсискус Мария Верхейден
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Синтон Байофармасьютикалс Б. В.
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Claims (34)

1. Соединение формулы (I):
Figure 00000001
в которой Ат анти-HER2 представляет собой анти-HER2 антитело или фрагмент антитела,
n составляет 0-3,
m представляет собой среднее DAR (соотношение лекарственное средство/антитело) из 1 до 4,
R1 выбран из
Figure 00000002
y составляет 1-16, и
R2 выбран из
Figure 00000003
для применения в лечении человеческих солидных опухолей и гематологических злокачественных новообразований, экспрессирующих HER2.
2. Соединение для применения по п.1, при этом
Ат анти-HER2 представляет собой анти-HER2 антитело или фрагмент антитела,
n составляет 0-1,
m представляет собой среднее DAR от 1 до 4,
R1 выбран из
Figure 00000004
y составляет 1-16, и
R2 выбран из
Figure 00000005
3. Соединение для применения по п.1 или 2 формулы (II):
Figure 00000006
4. Соединение для применения по любому из пп.1-3, для применения в лечении человеческих солидных опухолей.
5. Соединение для применения по любому из пп.1-4, при этом экспрессирующая HER2 человеческая солидная опухоль представляет собой рак молочной железы, рак желудка, рак мочевого пузыря, рак яичников, рак легких, рак простаты, рак поджелудочной железы, колоректальный рак, плоскоклеточный рак головы и шеи или остеосаркому, и гематологическая злокачественная опухоль представляет собой острый лимфобластный лейкоз.
6. Соединение для применения по любому из пп.1-5, при этом экспрессирующая HER2 человеческая солидная опухоль представляет собой рак молочной железы или рак желудка.
7. Соединение для применения по любому из пп.1-6, при этом рак молочной железы является гормон-рецептор позитивным или негативным.
8. Соединение для применения по любому из пп.1-7, при этом человеческая солидная опухоль представляет собой HER2 IHC 2+ или 1+.
9. Соединение для применения по любому из пп.1-8, при этом человеческая солидная опухоль является HER2 FISH негативной.
10. Соединение для применения по любому из пп.1-9, при этом человеческая солидная опухоль представляет собой трижды негативный рак молочной железы.
11. Комбинация соединения для применения по любому из пп.1-10 с терапевтическим антителом и/или химиотерапевтическим агентом, для применения в лечении человеческих солидных опухолей и гематологических злокачественных опухолей, экспрессирующих HER2.
12. Комбинация для применения по п.11, для применения в лечении рака молочной железы, в частности трижды негативного рака молочной железы.
13. Комбинация для применения по п.11 или 12, при этом терапевтическое антитело представляет собой пертузумаб и химиотерапевтический агент представляет собой таксан, в частности доцетаксел или паклитаксел, или антрациклин, в частности доксорубицин, эпирубицин, даунорубицин или валрубицин.
14. Фармацевтическая композиция, содержащая соединение для применения по любому из пп.1-10 или комбинацию для применения по любому из пп.11-13 и одно или более фармацевтически приемлемых вспомогательных веществ.
15. Фармацевтическая композиция по п.14 в форме лиофилизированного порошка или замороженного раствора.
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NO3069735T3 (ru) 2018-08-11
JP6342517B2 (ja) 2018-06-13
WO2015104385A2 (en) 2015-07-16
PT2948184T (pt) 2016-07-08
US20190314513A1 (en) 2019-10-17
US20160008486A1 (en) 2016-01-14
AU2019264575B2 (en) 2020-10-29
KR102344354B1 (ko) 2021-12-28
ZA201604535B (en) 2018-11-28

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