BRUTON'S TYROSINE KINASE INHIBITORS Russian patent published in 2018 - IPC C07D401/14 C07D403/06 A61K31/4155 A61K31/4439 A61K31/4184 A61K31/5377 A61P11/06 A61P29/00 A61P35/00 A61P37/00 

Abstract RU 2653500 C2

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula (I) or to pharmaceutically acceptable salts thereof. In general formula (I), R1 is lower alkyl, phenyl optionally substituted with one or more R1', cycloalkyl or pyridyl; each R1' is independently a lower alkyl, halogen, -C(=O)NH2 or cyano; R2 is absent or is halogen, lower alkoxy, hydroxy or lower alkyl; R3 is absent or is halogen, lower alkoxy, hydroxy or lower alkyl; R4 is absent or is morpholinyl-lower alkylenyl; X is CH or N; and Y is CH or N. Compounds of formula (I) inhibit Btk (Bruton's tyrosine kinase). Compounds of formula (I) are useful for modulating the activity of Btk and treating diseases associated with excessive Btk activity. Compounds are useful in the treatment of cancer, autoimmune and inflammatory diseases caused by aberrant B-cell activation. (I).

EFFECT: invention also relates to pharmaceutical compositions containing compounds of formula (I) and at least one carrier, diluent or excipient.

25 cl, 2 tbl, 20 ex

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RU 2 653 500 C2

Authors

Dominik Romir

Kon Norman

Lou Yan

Lopez-Tapia Fransisko Khaver

So Sun-Sau

Dates

2018-05-10Published

2014-12-10Filed