EA022875B1 - Производные 4-(индазол-5-ил-амино)-2-фенилхиназолина - Google Patents
Производные 4-(индазол-5-ил-амино)-2-фенилхиназолина Download PDFInfo
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- EA022875B1 EA022875B1 EA200702048A EA200702048A EA022875B1 EA 022875 B1 EA022875 B1 EA 022875B1 EA 200702048 A EA200702048 A EA 200702048A EA 200702048 A EA200702048 A EA 200702048A EA 022875 B1 EA022875 B1 EA 022875B1
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- alkyl
- ylamino
- quinazolin
- indazol
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Abstract
Изобретение относится к ингибиторам ROCK1 и ROCK2 и способам модулирования фармакокинетических и/или фармакодинамических свойств таких соединений. Предложено соединение общей формулы (I)Также представлены способы ингибирования ROCK1 и/или ROCK2, применимые для лечения заболеваний.
Description
(57) Изобретение относится к ингибиторам КОСК1 и КОСК2 и способам модулирования фармакокинетических и/или фармакодинамических свойств таких соединений. Предложено соединение общей формулы (I)
022875 Β1
Claims (9)
- или его фармацевтически приемлемая соль, где К1 выбран из группы, состоящей из -О-(СН2)У-С(=О)-NΗ-(С1 -С6-алкил)-О-(С1 -С6алкил)группы,-Θ-(СН2)у-С(=Θ)-NΗ-(С1-С8алкил)группы,-Θ-(СН2)у-С(=Θ)-NΗ-(С1-С8алкил)-(С3-С7Циклоалкил)группы,-Θ-(СΗ2)у-С(=Θ)-NΗ-(С1-С6алкил)фенилгруппы,-Θ-(СН2)у-С(=Θ)-NΗ-пиридинилгруппы,-Θ-(СΗ2)у-С(=Θ)-NΗ2-группы,-NΗ-С(=О)фуранилгруппы,-N4 -С(=О) пиридинилгруппы,-NΗ-С(=О)пиперидинилгруппы,-NΗ-С(=Θ)-(СΗ2)у-морфолинилгруппы,-NΗ-С(=О)-(С1-С6алкил)-О-(С1-С6алкил)группы,-NΗ-С(=О)-(СН2)у-пирролидинилгруппы,-NΗ-С(=Θ) -(^^-N4-^1 -С8алкил)группы,-NΗ-С(=Θ)-(СН2)у-N-(С1 -С8алкил)(С1 -С6алкил)-О-(С -С6алкил)группы и -NΗ-С(=Θ)-(СН2)у-N(С1-С8алкил)2-группы, у имеет значение от 0 до 6;К2 является атомом водорода;К3 выбран из группы, состоящей из атома водорода, гидроксилгруппы и метоксигруппы;К4 выбран из группы, состоящей из атома водорода,-О-(СН2)с-^С1 -С8алкил)2-группы,-О-(С1 -С6алкил)-О-(С1 -С6алкил)группы,-О-(СН2)а-(С3-С7циклоалкил)группы,-О-(СН2)с-морфолинилгруппы,-О-(СН2)с-пирролидонилгруппы,-О-(СН2)с-пирролидинилгруппы, где пирролидинилгруппа, возможно, может замещаться -ОНгруппой и -ИК2-группой, К является С1-С6алкилгруппой,-О-(СН2)с-пиперидинилгруппы и-О-(СН2)с-пиперазинилгруппы, где пиперазинилгруппа, возможно, может замещаться С1С6алкилгруппой;а имеет значение от 0 до 6; с имеет значение от 2 до 6;К5 выбран из группы, состоящей из атома водорода,-(СН2)<^-С(=Θ)-NΗ-(С1-С8алкил)-(С3-С7циклоалкил)группы,-(СΗ2)<^-С(=Θ)-NΗ-(С1 -С8алкил)фенилгруппы и -(СН2)<^-С(=О)-NΗ-(С1 -С6алкил)-О-(С1 -С6алкил)группы, б имеет значение от 0 до 6;К6 выбран из группы, состоящей из атома водорода и С1 -С6алкилгруппы, η равен 0;т выбран из 0 и 1 и р выбран из 0 и 1.
- 2. Соединение, выбранное из группы, состоящей из2-(3-(4-(1Н-индазол-5-иламино)хиназолин-2-ил)фенокси)-^изопропилацетамида,2-(3-(4-(1Н-индазол-5-иламино)хиназолин-2-ил)фенокси)-^(2-метоксиэтил)ацетамида,2-(3-(4-(1Н-индазол-5-иламино)хиназолин-2-ил)фенокси)-^(пиридин-3-ил)ацетамида,- 106 0228752-(3-(4-(1Н-индазол-5-иламино)хиназолин-2-ил)фенокси)-^метилацетамида,2-(3-(4-(1Н-индазол-5-иламино)хиназолин-2-ил)фенокси)-^трет-бутилацетамида,2-(3-(4-(1Н-индазол-5-иламино)хиназолин-2-ил)фенокси)-^этилацетамида,2-(3-(4-(1Н-индазол-5-иламино)хиназолин-2-ил)фенокси)-^неопентилацетамида,
- 3 -(3 -(
- 4-(1Н-индазол-5-иламино)хиназолин-2-ил)фенил)-1,1 -диметилмочевины,N-(3 -(4-(1Н-индазол-5 -иламино)хиназолин-2-ил)фенил)-2-метоксиацетамида,N-(3 -(4-(1Н-индазол-5 -иламино)хиназолин-2-ил)фенил)-2-морфолинацетамида,N-(3 -(4-(1Н-индазол-5 -иламино)хиназолин-2-ил)фенил)пиперидин-4-карбоксамида, ^(3-(4-(1Н-индазол-5-иламино)-6-(2-метоксиэтокси)хиназолин-2-ил)фенил)бутирамида и 2-(3-(4-(1Н-индазол-5-иламино)хиназолин-2-ил)фенокси)ацетамида.3. Соединение, отвечающее структуре
- 5. Фармацевтическая композиция для ингибирования активности КЬо-киназы, включающая соединение по любому из пп. 1 -4 вместе с фармацевтически приемлемым носителем.
- 6. Применение соединения по любому из пп.1-4 в производстве медикамента для лечения рака, нейродегенерации, повреждения спинного мозга, эректильной дисфункции, атеросклероза, гипертонии, спазма мозговых сосудов, церебральной ишемии, рестеноза, астмы, глаукомы, остеопороза, фиброзного- 107 022875 заболевания или воспаления или для диализа почек.
- 7. Применение соединения по любому из пп.1-4 в производстве медикамента для лечения периферической нейродегенерации, центральной нейродегенерации, фиброзного заболевания печени или фиброзного заболевания почек.
- 8. Применение соединения по любому из пп.1-4 для ингибирования активности КЬо-киназы.
- 9. Применение по п.8, в котором КЬо-киназой является КОСК2.Фиг. 1- 108 022875Фиг. 2- 109 022875Фиг. 3- 110 022875- 111 022875Фиг. 6
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US66516505P | 2005-03-25 | 2005-03-25 | |
PCT/US2006/011271 WO2006105081A2 (en) | 2005-03-25 | 2006-03-27 | Pharmacokinetically improved compounds |
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EP (1) | EP1865958B1 (ru) |
JP (2) | JP2008534518A (ru) |
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