RU2500680C2 - Новые замещенные пиридин-2-оны и пиридазин-3-оны - Google Patents

Новые замещенные пиридин-2-оны и пиридазин-3-оны Download PDF

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RU2500680C2
RU2500680C2 RU2011101774/04A RU2011101774A RU2500680C2 RU 2500680 C2 RU2500680 C2 RU 2500680C2 RU 2011101774/04 A RU2011101774/04 A RU 2011101774/04A RU 2011101774 A RU2011101774 A RU 2011101774A RU 2500680 C2 RU2500680 C2 RU 2500680C2
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Нолан Джеймс ДЬЮДНИ
Рама К. КОНДРУ
Брэдли Э. ЛО
Янь ЛОУ
Джоэл Макинтош
Тимоти Д. Оуэнс
Майкл СОТ
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Abstract

Изобретение относится к новым производным пиридин-2-онов и пиридазин-3-онов, обладающим ингибирующей активностью в отношении Btk-киназы. В формулах I-IV:
Figure 00000082
Figure 00000083
Figure 00000084
Figure 00000085
R обозначает -R1-R2-R3 или -R2-R3; R1 обозначает гетероарил, содержащий в кольце 6 атомов, включая один гетероатом N; R2 обозначает -C(=O), -C(=O)N(R2'), где R2' обозначает H; R3 обозначает R4; где R4 - низший алкил, гетероциклоалкил, (низший алкил)гетероциклоалкил или гетероциклоалкил(низший алкил), где гетероциклоалкил содержит в кольце 6 атомов, включая два гетероатома, выбранных из N и O; и где R4 может быть замещен одним или более заместителем, выбранным из низшего алкила, оксогруппы и низшей алкоксигруппы; X обозначает CH или N; Y1 обозначает низший алкил; n и m равны 0; значения радикалов Y2, Y4 приведены в формуле изобретения. Изобретение также относится к фармацевтической композиции, содержащей указанные соединения. 2 н. и 4 з.п. ф-лы, 2 табл., 42 пр.

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Claims (6)

1. Соединение формулы I, II, III или IV:
Figure 00000082
Figure 00000083

Figure 00000084
Figure 00000085

в которой:
R обозначает -R1-R2-R3 или -R2-R3; где
R1 обозначает гетероарил, содержащий в кольце 6 атомов, включая один гетероатом N;
R2 обозначает -C(=O), -C(=O)N(R2'), где R2' обозначает H;
R3 обозначает R4; где R4 обозначает низший алкил, гетероциклоалкил, (низший алкил)гетероциклоалкил или гетероциклоалкил(низший алкил), где гетероциклоалкил содержит в кольце 6 атомов, включая два гетероатома, выбранных из N и O; и где R4 может быть замещен одним или более заместителем, выбранным из низшего алкила, оксогруппы и низшей алкоксигруппы;
X обозначает СН или N;
Y1 обозначает низший алкил;
Y2 обозначает Y2b; где Y2b обозначает низший алкил, необязательно замещенный одним Y2b'; и Y2b' обозначает гидроксигруппу;
n равен 0;
m равен 0;
Y4 обозначает Y4a, Y4b, Y4c или Y4d; где
Y4a обозначает галоген;
Y4b обозначает низший алкил, необязательно содержащий один заместитель, выбранный из гидроксигруппы;
Y4c обозначает низший циклоалкил; и
Y4d обозначает аминогруппу, необязательно замещенную одним или более низшим алкилом;
или его фармацевтически приемлемая соль.
2. Соединение по п.1, в котором Y1 обозначает метил.
3. Соединение по п.1, в котором X обозначает CH.
4. Соединение по п.1, в котором Y2 обозначает метил или гидроксиметил.
5. Соединение по п.1, в котором R обозначает -R1-R2-R3; где R1 обозначает пиридил; R2 обозначает -C(=O); R3 обозначает R4; и R4 обозначает морфолин или пиперазин.
6. Фармацевтическая композиция, обладающая ингибирующей активностью в отношении Btk-киназы, включающая соединение по любому из пп.1-5 в терапевтически эффективном количестве в смеси по меньшей мере с одним фармацевтически приемлемым носителем, инертным наполнителем или разбавителем.
RU2011101774/04A 2008-06-24 2009-06-15 Новые замещенные пиридин-2-оны и пиридазин-3-оны RU2500680C2 (ru)

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