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RU2445312C2 - ПРОИЗВОДНЫЕ 2-МЕТИЛМОРФОЛИН ПИРИДО-, ПИРАЗО- И ПИРИМИДО-ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ mTOR - Google Patents

ПРОИЗВОДНЫЕ 2-МЕТИЛМОРФОЛИН ПИРИДО-, ПИРАЗО- И ПИРИМИДО-ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ mTOR Download PDF

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RU2445312C2
RU2445312C2 RU2009110261/04A RU2009110261A RU2445312C2 RU 2445312 C2 RU2445312 C2 RU 2445312C2 RU 2009110261/04 A RU2009110261/04 A RU 2009110261/04A RU 2009110261 A RU2009110261 A RU 2009110261A RU 2445312 C2 RU2445312 C2 RU 2445312C2
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Хитер Мэри Эллен ДАГГАН (GB)
Хитер Мэри Эллен ДАГГАН
Фредерик Жорж Мари ЛЕРУ (GB)
Фредерик Жорж Мари Леру
Карин МАЛАГУ (GB)
Карин МАЛАГУ
Нилл Морриссон Барр МАРТИН (GB)
Нилл Морриссон Барр МАРТИН
Кейт Аллан МЕНИР (GB)
Кейт Аллан МЕНИР
Грейм Камерон Марри СМИТ (GB)
Грейм Камерон Марри Смит
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Abstract

Настоящее изобретение относится к соединениям общей формулы (I)
Figure 00000223
или его фармацевтически приемлемым солям, которые действуют в качестве ингибиторов mTOR. Также заявляется получение фармацевтической композиции, содержащей терапевтически эффективное количество соединения формулы (I) и фармацевтически приемлемый носитель или разбавитель, а также заявляется применение соединения формулы (I) или его фармацевтически приемлемой соли для приготовления лекарственного средства предназначенного для получения противоракового действия. 4 н. и 7 з.п. ф-лы, 25 пр.

Description

Текст описания приведен в факсимильном виде.
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Figure 00000169
Figure 00000170

Claims (11)

1. Соединение формулы I
Figure 00000171

или его фармацевтически приемлемая соль,
где X5 и X6 представляют собой СН;
X8 представляет собой N;
R7 выбирают из
Figure 00000172
Figure 00000173
Figure 00000174

Figure 00000175
Figure 00000176
Figure 00000177
Figure 00000178

Figure 00000179
Figure 00000180
Figure 00000181
Figure 00000182

Figure 00000183
Figure 00000184
Figure 00000185

Figure 00000186
Figure 00000187
Figure 00000188

Figure 00000189
и
Figure 00000190

и R2 представляет собой
Figure 00000191
или
Figure 00000192
или
Figure 00000193

или
Figure 00000194
или
Figure 00000195
2. Соединение по п.1, где соединение формулы I представляет собой соединение формулы Ia или Ib
Figure 00000196
Figure 00000197

или их фармацевтически приемлемую соль,
где X5 и X6 представляют собой СН, X8 представляет собой N, а остальные представляют собой СН;
R7 выбирают из
Figure 00000198
Figure 00000199
Figure 00000200

Figure 00000175
Figure 00000201
Figure 00000202
Figure 00000203

Figure 00000204
Figure 00000205
Figure 00000206
Figure 00000207

Figure 00000208
Figure 00000209
Figure 00000210

Figure 00000211
Figure 00000212
Figure 00000213

Figure 00000214
и
Figure 00000215

и R2 представляет собой
Figure 00000191
или
Figure 00000192
или
Figure 00000193

или
Figure 00000194
или
Figure 00000195
3. Соединение по п.1, где соединение формулы I представляет собой соединение формулы Ia
Figure 00000196

или его фармацевтически приемлемую соль
где X5 и X6 представляют собой СН, X8 представляет собой N, R7 выбирают из
Figure 00000198
Figure 00000199
Figure 00000200

Figure 00000175
Figure 00000201
Figure 00000202
Figure 00000203

Figure 00000204
Figure 00000205
Figure 00000206
Figure 00000207

Figure 00000208
Figure 00000209
Figure 00000210

Figure 00000211
Figure 00000212
Figure 00000213

Figure 00000214
и
Figure 00000215

и R2 представляет собой
Figure 00000216
или
Figure 00000217
или
Figure 00000218

или
Figure 00000219
или
Figure 00000220
4. Соединение по п.1, которое представляет собой
Figure 00000221

или его фармацевтически приемлемую соль.
5. Соединение по п.1, которое представляет собой
Figure 00000221
.
6. Соединение по п.1, которое представляет собой
Figure 00000222

или его фармацевтически приемлемую соль.
7. Соединение по п.1, которое представляет собой
Figure 00000222
8. Фармацевтическая композиция, обладающая активностью ингибитора mTOR, содержащая терапевтически эффективное количество соединения по п.1 и фармацевтически приемлемый носитель или разбавитель.
9. Соединение по п.1 или его фармацевтически приемлемая соль, обладающее активностью ингибитора mTOR.
10. Применение соединения по п.1 или его фармацевтически приемлемой соли для приготовления лекарственного средства, предназначенного для получения ингибирующего действия в отношении mTOR.
11. Применение соединения по п.1 или его фармацевтически приемлемой соли для приготовления лекарственного средства, предназначенного для получения противоракового действия.
RU2009110261/04A 2006-08-23 2007-08-21 ПРОИЗВОДНЫЕ 2-МЕТИЛМОРФОЛИН ПИРИДО-, ПИРАЗО- И ПИРИМИДО-ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ mTOR RU2445312C2 (ru)

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