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DYETERED DIAMINOPYRIMIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH CONNECTIONS
专利权人:
LTD.;SUCHZHOU ZELGEN BIOFARMASYUTIKALS KO.
发明人:
LV Binkhua (CN),ЛВ Биньхуа (CN),LI Chenvej (CN),ЛИ Чэнвэй (CN),TSAO Benven (CN),ЦАО Бэньвэнь (CN),PAN Syujdun (CN),ПАН Сюйдун (CN),LV Binkhua,ЛВ Биньхуа,LI Chenvej,ЛИ Чэнвэй,TSAO Benven,ЦАО Бэньвэнь,PAN Syujdun,ПАН Сюйдун
申请号:
RU2015149767
公开号:
RU0002632907C2
申请日:
2014.04.22
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: pharmacology.SUBSTANCE: invention relates to novel deuterated diaminopyrimidines of the general formula (I) and their pharmaceutically acceptable salts. In the general formula (I) R1a, R1b, R1c, R2a, R2b, R2c, R3, R4, R6, R7, R9, R10, R11, R12, R13a, R13b, R13c, R14a, R14b, R14c, R15a, R15b, R15c, R16, R17a, R17b, R18a, R18b, R19a, R19b, R20a and R20b independently hydrogen or deuterium;R5 is hydrogen, deuterium or halogen, R8 Represents a halogen; Provided that at least four ofR1a, R1b, R1c, R2a, R2b, R2c, R3, R12, R13a, R13b, R13c, R14a, R14b, R14c, R19a, R19b, R20a or R20b are deuterium. The invention also relates to a process for the preparation of compounds of general formula (I) by reacting compoundA6 with compound XV and to intermediates A6 and XV. In this case, in compound A6 R10, R11, R12, R13a, R13b, R13c, R14a, R14b, R14c, R15a, R15b, R15c, R16, R17a, R17b, R18a, R18b, R19a, R19b, R20a or R20b are independently selected from deuterium or hydrogen and at least one of them is deuterium; In compoundXV R1a, R1b, R1c, R2a, R2b, R2c, R3, R4, R6, R7, R9 are independently selected from hydrogen or deuterium and at least one of them is deuterium; andR5 is hydrogen, deuterium or halogen; andR8 represents a halogen; X2 is selected from F, Cl, Br, I.EFFECT: compounds have ALK protein kinase inhibitory properties and can be used to treat or prevent cancer, impair cell proliferation, cardiovascular diseases, inflammation, infection, autoimmune diseases, organ transplantation, viral diseases, cardiovascular diseases or metabolic diseases.18 cl, 4 dwg, 1 tblНастоящее изобретение относится к новым дейтерированным диаминопиримидинам общей формулы (I) и их фармацевтически приемлемым солям. Соединения обладают свойствами ингибирования ALK протеинкиназ и могут быть использованы для лечения и/или предупреждения онкологических заболеваний, нарушения пролиферации клеток, сердечнососудистых заболеваний, воспаления, инфекции, аутоиммунных заболеваний, трансплантации органо
来源网站:
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http://www.ckcest.cn/home/

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