SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR Russian patent published in 2018 - IPC C07D401/04 C07D401/14 A61K31/444 A61K31/506 A61K31/496 A61K31/4545 A61K31/5377 A61P35/00 

Abstract RU 2671212 C2

FIELD: chemistry.

SUBSTANCE: invention relates to 2-aminopyridine derivatives of Formula (I) and Formula (III) (I) (III), where A1 is selected from the group consisting of a hydrogen atom and -O-(CHR1)-A4; R1 is selected unsubstituted methyl and methyl having 1–3 halogen atoms as substituents; A4 is phenyl optionally having one or more R4 as substituents; R4 is selected from the group consisting of a halogen atom, an unsubstituted C1-6 alkyl and C1-6 alkyl substituted with halogen atom (s); A2 is selected from the group consisting of phenyl, pyridinyl and pyrimidinyl, optionally substituted with one or more substituents selected from halo and -OC1-6 alkyl, in which each hydrogen atom C1-6 alkyl moiety is optionally substituted with hydroxy or heteroalicyclic; A5 is a heteroalicyclyl which optionally has one or more substituents selected from the group consisting of =O, unsubstituted C1-6 alkyl, heteroalicyclyl, wherein heteroalicyclyl is optionally further substituted with a substituent(s) selected from the group consisting of C1-6 alkyl, =O, -OH, -COOH, -CN, a halogen atom, -NH(C1-6 alkyl) and -N(C1-6 alkyl)2, and C1-6 alkyl substituted with heteroalicyclic; A3 is selected from the group consisting of a hydrogen atom, a heteroaryl having as a substituent a phenyl, and heteroaryl ethynyl having as a substituent heteroarylalkyl, wherein each phenyl and heteroaryl optionally have one or more substituents selected from the group consisting of a halogen atom, C1-6 alkyl optionally having a halogen atom as substituents; provided that A1 and A3 At the same time they are not hydrogen atoms and one of A1 and A3 must be a hydrogen atom; and when A1 is -O-(CHR1)-A4 and R1 is methyl, A2 has, as substituents, at least one -OC1-6 alkyl, where C1-6 the alkyl moiety is optionally substituted with hydrogen or heteroalicyclic; and pharmaceutically acceptable salts thereof having an inhibitory activity against protein kinase.

EFFECT: substituted 2-aminopyridine protein kinase inhibitor.

32 cl, 5 tbl, 56 ex

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RU 2 671 212 C2

Authors

Syao Denmin

Syuj Sinkhe

Lyu Sitsze

Khu Yuandun

Yuj Khunkhao

Lyu Chzhi Khua

Pen Yun

Sun Inkhuj

Lo Khun

Kun Fanshen

Khan Yunsin

Sun Tszyan

Dates

2018-10-30Published

2014-01-27Filed