AMINOPYRIMIDINE KINASE INHIBITORS Russian patent published in 2017 - IPC C07D417/06 C07D417/14 C07D471/04 C07D487/04 A61K31/4427 A61K31/506 A61P35/00 

Abstract RU 2636589 C2

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound of formula 2 ,

wherein independently for each case R1 is hydrogen; each R2 and R3 is independently selected from the group consisting of hydrogen; (C1-C6)alkyl, optionally substituted with OH; heteroaryl containing 6 atoms in the ring, 1 atom of which is N, and the remaining ones are C atoms (pyridine); heterocyclyl containing 5 or 6 ring atoms, 1 atom of which is N and the remaining ones are C atoms (piperidine or pyrrolidine) optionally substituted by a group selected from methyl, phenyl, pyridinylmethyl, quinolinylmethyl, pyridinylmethyl, piperidinylmethyl or azetidinylmethyl; aryl (C1-C6)alkyl, wherein aryl contains 6 ring atoms, optionally substituted amino or CH2NH2, where (C1-C6)alkyl is optionally substitutedby OH; heteroaryl (C1-C6)alkyl, wherein heteroaryl contains 5 to 9 ring atoms, of which 1 to 2 are heteroatoms selected from N and S, and the remaining atoms are C atoms (indole, pyridine, thiophene, benzimidazole, pyrazole), wherein heteroaryl is optionally is replaced by ethyl; heterocycle (C1-C6)alkyl, wherein the heterocycle contains 6 ring atoms, 1 atom of which is N and the remaining ones are C atoms (piperidine) optionally substituted by methyl; and - [C(R4)2]p-R5, or R2 and R3 are joined together to form an optionally substituted heterocyclic ring containing 5-10 atoms, of which 1 to 2 are heteroatoms selected from N and O, and the remaining ones are C atoms; R20 is selected from the group consisting of hydrogen; heterocyclyl containing 6 ring atoms, 1 atom of which is a heteroatom selected from N, and the remaining atoms are C atoms (piperidinyl); halogen (C1-C6)alkyl; trifluoromethyl; fluorine (C1-C6)alkyl; -O-[C(R4)2]p-R5; -OR16, where R16 is methyl; and amino, which is -N(R50)(R51), where each R50 and R51 is independently hydrogen, (C1-C6)alkyl, optionally substituted by methoxy, or - (CH2)m-R61, where R61 is an aryl containing 6 ring atoms, and m is an integer from 1 to 8. The invention also relates to specific compounds as defined in the claims. The compounds of the invention are for cancer treatment or effect on apoptosis, by administration of a therapeutically effective amount of a compound to a mammal in need thereof.

EFFECT: aminopyrimidine compounds for cancer treatment.

24 cl, 30 tbl, 251 ex, 53 dwg

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RU 2 636 589 C2

Authors

Baldino Karmen M.

Kaserta Dzhastin L.

Li Chi-Seng

Najsvondzher Robert B.

Flanders Ivonn L.

Dyuma Stefan A.

Dates

2017-11-24Published

2010-12-23Filed