RU2017107089A - Производные пирролидинона в качестве ингибиторов метар-2 - Google Patents

Производные пирролидинона в качестве ингибиторов метар-2 Download PDF

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RU2017107089A
RU2017107089A RU2017107089A RU2017107089A RU2017107089A RU 2017107089 A RU2017107089 A RU 2017107089A RU 2017107089 A RU2017107089 A RU 2017107089A RU 2017107089 A RU2017107089 A RU 2017107089A RU 2017107089 A RU2017107089 A RU 2017107089A
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inhibitor
group
tautomers
stereoisomers
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RU2017107089A
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RU2694624C2 (ru
RU2017107089A3 (ru
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Тимо Генрих
Франк Ценке
Феликс РОДИХ
Маня Фризе-Хамим
Диане ХАН
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Мерк Патент Гмбх
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Claims (34)

1. Соединения, выбранные из группы
Figure 00000001
Figure 00000002
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
Figure 00000011
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000015
Figure 00000016
Figure 00000017
Figure 00000018
и их фармацевтически применимые соли, таутомеры и стереоизомеры, включая их смеси во всех отношениях.
2. Соединения по п. 1, выбранные из группы, включающей
Figure 00000019
Figure 00000020
Figure 00000021
и их фармацевтически применимые соли, таутомеры и стереоизомеры, включая их смеси во всех отношениях.
3. Соединения по п. 1, выбранные из группы, включающей
Figure 00000022
Figure 00000023
и их фармацевтически применимые соли, таутомеры и стереоизомеры, включая их смеси во всех отношениях.
4. Лекарственные средства, содержащие по меньшей мере одно соединение по п. 1 и/или его фармацевтически применимые соли, таутомеры и стереоизомеры, включая их смеси во всех отношениях, и необязательно наполнители и/или вспомогательные средства.
5. Соединения по п. 1, их фармацевтически применимые соли, таутомеры и стереоизомеры, включая их смеси во всех отношениях, для применения в лечении опухолевых новообразований, метастаз опухолей, пролиферативных заболеваний мезангиальных клеток, гемангиомы, пролиферативной ретинопатии, ревматоидного артрита, атеросклеротической неоваскуляризация, псориаза, глазной неоваскуляризации, остеопороза, диабетов и ожирения, лимфолейкоза, лимфомы, малярии и гипертрофии предстательной железы.
6. Соединения по п. 5, причем опухолевое заболевание выбирают из группы, включающей новообразования чешуйчатого эпителия, мочевого пузыря, желудка, почек, головы и шеи, пищевода, шейки матки, щитовидной железы, кишечника, печени, головного мозга, предстательной железы, мочеполовых путей, лимфатической системы, желудка, гортани, легкого, кожи, моноцитарного лейкоза, аденокарциномы легкого, немелкоклеточной карциномы легких, рака поджелудочной железы, глиобластомы, рака молочной железы, острой миелоцитарной лейкемии, хронической миелоцитарной лейкемии, острого лимфобластного лейкоза, хронического лимфолейкоза, лимфомы Ходжкина, неходжкинской лимфомы.
7. Соединения по п. 1 и/или их фармацевтически приемлемые соли для применения в лечении опухолевых новообразований, причем терапевтически эффективное количество соединения по п. 1 вводят в комбинации с соединением из группы, включающей 1) модулятор эстрогеновых рецепторов, 2) модулятор андрогенных рецепторов, 3) модулятор ретиноидных рецепторов, 4) цитотоксическое средство, 5) антипролиферативное средство, 6) ингибитор пренил-протеин-трансферазы, 7) ингибитор HMG-CoA редуктазы, 8) ингибитор ВИЧ-протеазы, 9) ингибитор обратной транскриптазы и 10) другие ингибиторы ангиогенеза.
8. Соединения по п. 1 и/или фармацевтически приемлемые соли для применения в лечении опухолевых новообразований, причем терапевтически эффективное количество соединения по п. 1 вводят в комбинации с лучевой терапией и соединением из группы, включающей 1) модулятор эстрогеновых рецепторов, 2) модулятор андрогенных рецепторов, 3) модулятор ретиноидных рецепторов, 4) цитотоксическое средство, 5) антипролиферативное средство, 6) ингибитор пренил-протеин-трансферазы, 7) ингибитор HMG-CoA редуктазы, 8) ингибитор ВИЧ-протеазы, 9) ингибитор обратной транскриптазы и 10) другие ингибиторы ангиогенеза.
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