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RU2013126112A - СОЛЬ (СОЛИ) ДИМЕТИЛАМИДА 7-ЦИКЛОПЕНТИЛ-2-(5-ПИПЕРАЗИН-1-ИЛ-ПИРИДИН-2-ИЛАМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-6-КАРБОНОВОЙ КИСЛОТЫ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ - Google Patents

СОЛЬ (СОЛИ) ДИМЕТИЛАМИДА 7-ЦИКЛОПЕНТИЛ-2-(5-ПИПЕРАЗИН-1-ИЛ-ПИРИДИН-2-ИЛАМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-6-КАРБОНОВОЙ КИСЛОТЫ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ Download PDF

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RU2013126112A
RU2013126112A RU2013126112/04A RU2013126112A RU2013126112A RU 2013126112 A RU2013126112 A RU 2013126112A RU 2013126112/04 A RU2013126112/04 A RU 2013126112/04A RU 2013126112 A RU2013126112 A RU 2013126112A RU 2013126112 A RU2013126112 A RU 2013126112A
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Джон Винсент КАЛЬЕННИ
Гуан-Пэй ЧЭНЬ
Баоцин ГУН
Прасад Котесвара КАПА
Вишал Саксена
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Новартис Аг
Астекс Терапьютикс Лтд
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Abstract

1. Сукцинатная соль диметиламида 7-циклопентил-2-(5-пиперазин-1-ил-пиридин-2-иламино)-7H-пирроло[2,3-d]пиримидин-6-карбоновой кислоты.2. Соль по п. 1, представленная формулой (II):3. Соль по п. 1 в негидратной форме.4. Соль по п. 1 в гидратной форме.5. Фармацевтическая композиция, содержащая:(a) терапевтически эффективное количество соли по любому из пп. 1-4; и(b) по меньшей мере один фармацевтически приемлемый носитель, разбавитель, растворитель или эксципиент.6. Способ лечения заболевания, которое ослабляется ингибированием активности циклинзависимых киназ, включающий стадию введения пациенту, нуждающемуся в таком лечении, терапевтически эффективного количества соли по любому из пп. 1-4.7. Способ получения соединения формулы (I), включающий:(1) взаимодействиеис получениеми(2) преобразованиев.8. Способ по п. 7, в котором стадию (1) осуществляют в присутствии Pd(OAc), BINAP и CsCO.9. Способ по п. 7, в котором стадию (2) осуществляют в присутствии водного раствора HCl и толуола.10. Способ по п. 7, в которомдополнительно преобразуют в.11. Способ по п. 10, в котором преобразование происходит в присутствии IPA и12. Способ получения соединения формулы (III):,включающий преобразование13. Способ по п. 12, в котором преобразованиепроисходит в присутствии MnO, NaCN,и ТГФ.14. Способ по п. 12, в которомполучают из15. Способ получения соединения формулы (III):включающий:(1) взаимодействиеис получением(2) преобразованиес получением(3) преобразованиес получениеми(4) преобразованиес получением16. Способ получения соединения формулы (IV):,включающий:(1) взаимодействиесс получением(2) преобразованиес получениеми(3) преобразованиес получением17. Способ по п. 16, в котором реакция происходит в присутстви

Claims (18)

1. Сукцинатная соль диметиламида 7-циклопентил-2-(5-пиперазин-1-ил-пиридин-2-иламино)-7H-пирроло[2,3-d]пиримидин-6-карбоновой кислоты.
2. Соль по п. 1, представленная формулой (II):
Figure 00000001
3. Соль по п. 1 в негидратной форме.
4. Соль по п. 1 в гидратной форме.
5. Фармацевтическая композиция, содержащая:
(a) терапевтически эффективное количество соли по любому из пп. 1-4; и
(b) по меньшей мере один фармацевтически приемлемый носитель, разбавитель, растворитель или эксципиент.
6. Способ лечения заболевания, которое ослабляется ингибированием активности циклинзависимых киназ, включающий стадию введения пациенту, нуждающемуся в таком лечении, терапевтически эффективного количества соли по любому из пп. 1-4.
7. Способ получения соединения формулы (I), включающий:
(1) взаимодействие
Figure 00000002
и
Figure 00000003
с получением
Figure 00000004
и
(2) преобразование
Figure 00000005
в
Figure 00000006
.
8. Способ по п. 7, в котором стадию (1) осуществляют в присутствии Pd(OAc)2, BINAP и Cs2CO3.
9. Способ по п. 7, в котором стадию (2) осуществляют в присутствии водного раствора HCl и толуола.
10. Способ по п. 7, в котором
Figure 00000007
дополнительно преобразуют в
Figure 00000008
.
11. Способ по п. 10, в котором преобразование происходит в присутствии IPA и
Figure 00000009
12. Способ получения соединения формулы (III):
Figure 00000010
,
включающий преобразование
Figure 00000011
13. Способ по п. 12, в котором преобразование
Figure 00000012
происходит в присутствии MnO2, NaCN,
Figure 00000013
и ТГФ.
14. Способ по п. 12, в котором
Figure 00000014
получают из
Figure 00000015
15. Способ получения соединения формулы (III):
Figure 00000016
включающий:
(1) взаимодействие
Figure 00000017
и
Figure 00000018
с получением
Figure 00000019
(2) преобразование
Figure 00000020
с получением
Figure 00000021
(3) преобразование
Figure 00000022
с получением
Figure 00000023
и
(4) преобразование
Figure 00000024
с получением
Figure 00000025
16. Способ получения соединения формулы (IV):
Figure 00000026
,
включающий:
(1) взаимодействие
Figure 00000027
с
Figure 00000028
с получением
Figure 00000029
(2) преобразование
Figure 00000030
с получением
Figure 00000031
и
(3) преобразование
Figure 00000032
с получением
Figure 00000033
17. Способ по п. 16, в котором реакция происходит в присутствии n-BuOH.
18. Способ получения соединения формулы (IV):
Figure 00000034
включающий:
(1) взаимодействие
Figure 00000035
с
Figure 00000036
с получением
Figure 00000037
и
(2) последующее преобразование
Figure 00000038
с получением
Figure 00000039
RU2013126112A 2010-11-10 2011-11-09 СОЛЬ (СОЛИ) ДИМЕТИЛАМИДА 7-ЦИКЛОПЕНТИЛ-2-(5-ПИПЕРАЗИН-1-ИЛ-ПИРИДИН-2-ИЛАМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-6-КАРБОНОВОЙ КИСЛОТЫ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ RU2631243C2 (ru)

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UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
US20120115878A1 (en) 2010-11-10 2012-05-10 John Vincent Calienni Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof
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