RU2016132759A - Дуокармициновые adc, демонстрирующие улучшенную противоопухолевую активность in vivo - Google Patents
Дуокармициновые adc, демонстрирующие улучшенную противоопухолевую активность in vivo Download PDFInfo
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- 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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- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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Claims (34)
1. Соединение формулы (I):
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
y составляет 1-16, и
R2 выбран из
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
y составляет 1-16, и
R2 выбран из
3. Соединение для применения по п.1 или 2 формулы (II):
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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PCT/EP2015/050350 WO2015104385A2 (en) | 2014-01-10 | 2015-01-09 | Duocarmycin adcs showing improved in vivo antitumor activity |
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