PYRIMIDINE DERIVATIVES AS BTK INHIBITORS AND USE THEREOF Russian patent published in 2021 - IPC C07D403/12 C07D401/12 C07D471/04 C07D471/10 C07D413/12 C07D409/12 C07D487/04 C07D239/48 A61K31/506 A61P25/28 A61P19/02 A61P17/02 A61P7/00 

Abstract RU 2743040 C2

FIELD: pharmaceutics.

SUBSTANCE: invention relates to the compound of a formula I-b or a pharmaceutically acceptable salt thereof having the properties of an inhibitor of the activity of CE, pharmaceutical composition on the basis thereof, a method for inhibiting the activity of CE, and a method for treating a disease, mediated by BTK, a method for producing compound of formula I-b. In the general formula I-b R1 selected from ; R2 represents hydrogen; or R1 and R2, taken together with the atom to which they are connected, form a 5-6 member heterocyclic ring containing 1 nitrogen and 0 other heteroatoms; or an 8-10 member condensed or spiral bicyclic heterocyclic ring containing 1 nitrogen and 1 other heteroatom of nitrogen; where the ring formed by R1 and R2 is replaced R4 represents hydrogen; each R5 independently is C1-6 alkyl substituted by (2-hydroxyisopropyl)phenyl, tert-butylphenyl or -NH-phenyl-Cl; phenyl substituted by tert-butyl, cyclopropyl, hydroxypropyl or -N(CH3)2; or a 5-member monocyclic heteroaril ring containing 2 heteroatoms independently selected from nitrogen and oxygen substituted by phenyl or tert-butyl; and m equals 0 or 1.

EFFECT: invention enables treating diseases, mediated by BTK.

10 cl, 21 ex, 1 tbl

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RU 2 743 040 C2

Authors

Qiu, Hui

Caldwell, Richard D.

Liu-Bujalski, Lesley

Dates

2021-02-12Published

2016-07-08Filed