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RU2348627C2 - Ингибиторы тирозинкиназ - Google Patents

Ингибиторы тирозинкиназ Download PDF

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RU2348627C2
RU2348627C2 RU2005102917/04A RU2005102917A RU2348627C2 RU 2348627 C2 RU2348627 C2 RU 2348627C2 RU 2005102917/04 A RU2005102917/04 A RU 2005102917/04A RU 2005102917 A RU2005102917 A RU 2005102917A RU 2348627 C2 RU2348627 C2 RU 2348627C2
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Вернер БРАЙТЕНШТАЙН (CH)
Вернер Брайтенштайн
Паскаль ФЮРЕ (FR)
Паскаль Фюре
Сандра ДЖЕЙКОБ (FR)
Сандра ДЖЕЙКОБ
Пол Уилль м МАНЛИ (CH)
Пол Уилльям МАНЛИ
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Abstract

Изобретение относится к новым соединениям формулы (I) или фармацевтически приемлемой соли такого соединения, которые обладают свойствами ингибитора протеинкиназы. Соединения могут найти применение для лечения опухолевых заболеваний, в частности лейкемии. В соединении формулы I
Figure 00000084
R1 представляет собой водород; R2 представляет собой фенил, замещенный трифторметилом и необязательно другим заместителем, выбранным из группы, состоящей из гидрокси-низшего алкила, низшего алкиламино, гидрокси-низшего алкиламино, динизшего алкиламино, 1H-имидазолила, низший алкил-1H-имидазолила, карбамоила, низшего алкилкарбамоила, пирролидино, пиперидино, пиперазино, низшего алкилпиперазино, морфолино, низшего алкокси, трифтор-низшего алкокси, фенила, пиридила и галогенила; R4 представляет собой метил; где префикс «низший» обозначает радикал, имеющий включительно до 7 атомов углерода. Изобретение также относится к фармацевтической композиции и способу лечения, а также к применению соединений изобретения для получения фармацевтической композиции. 3 з. и 6 н.п. ф-лы.

Description

Текст описания приведен в факсимильном виде.
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Claims (11)

1. Соединение формулы I
Figure 00000079

где R1 представляет собой водород;
R2 представляет собой фенил, замещенный трифторметилом и необязательно другим заместителем, выбранным из группы, состоящей из гидрокси-низшего алкила, низшего алкиламино, гидрокси-низшего алкиламино, динизшего алкиламино, 1H-имидазолила, низший алкил-1H-имидазолила, карбамоила, низшего алкилкарбамоила, пирролидино, пиперидино, пиперазино, низшего алкилпиперазино, морфолино, низшего алкокси, трифтор-низшего алкокси, фенила, пиридила и галогенила;
R4 представляет собой метил;
где префикс «низший» обозначает радикал, имеющий включительно до 7 атомов углерода,
или фармацевтически приемлемая соль такого соединения.
2. Соединение формулы I по п.1, где
R1 представляет собой водород;
R2 представляет собой фенил, замещенный 3-трифторметилом и необязательно другим заместителем, выбранным из группы, состоящей из 1-гидрокси-1-метилэтила, метиламино, этиламино, 2-гидрокси-1-пропиламино, 2-гидрокси-2-пропиламино, диэтиламино, 1H-имидазолила, 2- и 4-метил-1Н-имидазолила, карбамоила, метилкарбамоила, пирролидино, пиперидино, пиперазино, 4-метилпиперазино, морфолино, метокси, трифторметокси, 2,2,2-трифторэтокси, фенила, 2-, 3- и 4-пиридила, хлора и фтора;
R4 представляет собой метил;
или фармацевтически приемлемая соль такого соединения.
3. Соединение формулы I по п.1, где R1 представляет собой водород;
R2 представляет собой 3-(1-гидрокси-1-метилэтил)-5-(трифторметил)фенил;
R4 представляет собой метил;
или фармацевтически приемлемая соль такого соединения.
4. Соединение формулы I по п.1, являющееся
4-метил-3-[[4-(3-пиридинил)-2-пиримидинил]амино]-N-[5-(4-метил-1Н-имидазол-1-ил)-3-(трифторметил)фенил]бензамидом
или фармацевтически приемлемой солью такого соединения.
5. Соединение формулы
Figure 00000080

где R4 представляет собой метил.
6. Способ получения соединения формулы I по п.1
Figure 00000081

где символы R1, R2 и R4 являются такими, как определено в п.1, характеризующийся тем, что соединение формулы II
Figure 00000082

где R4 является таким, как определено для соединения формулы I, или его производное, где карбоксигруппа -СООН находится в активированной форме, подвергают реакции с амином формулы III
Figure 00000083

где R1 и R2 являются такими, как определено для соединения формулы I, необязательно в присутствии дегидрирующего агента и инертного основания и необязательно в присутствии инертного растворителя;
где указанные выше исходные соединения II и III могут также присутствовать с защищенными функциональными группами, при необходимости, и любую защитную группу в защищенном производном соединения формулы I удаляют.
7. Фармацевтическая композиция для лечения заболевания, которое связано с ингибированием активности протеинкиназы, включающем в качестве активного ингредиента соединение формулы I по любому одному из пп.1-4 или его или фармацевтически приемлемую соль вместе с фармацевтически приемлемым носителем.
8. Способ лечения заболевания, которое связано с ингибированием активности протеинкиназы, который включает введение соединения формулы I по любому одному из пп.1-4 или его фармацевтически приемлемой соли.
9. Применение соединения формулы I по любому одному из пп.1-4 или его фармацевтически приемлемой соли для получения фармацевтической композиции для лечения заболевания, которое связано с ингибированием активности протеинкиназы.
Приоритет по пунктам:
05.07.2002 по пп.1-3, 5-8;
20.12.2002 по пп.4, 9.
RU2005102917/04A 2002-07-05 2003-07-04 Ингибиторы тирозинкиназ RU2348627C2 (ru)

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