DYETERED DIAMINOPYRIMIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH CONNECTIONS Russian patent published in 2017 - IPC C07D401/12 A61K31/506 A61P35/00 A61P9/00 A61P29/00 A61P31/12 A61P37/02 A61P3/00 C07B59/00 

Abstract RU 2632907 C2

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 of R1a, 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 compound

A6 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 compound XV 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; and R5 is hydrogen, deuterium or halogen; and R8 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 tbl

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RU 2 632 907 C2

Authors

Lv Binkhua

Li Chenvej

Tsao Benven

Pan Syujdun

Dates

2017-10-11Published

2014-04-22Filed