SERIN / TREONIN KINASE INHIBITORS FOR TREATING OF HYPEROPLIFERATIVE DISEASES Russian patent published in 2018 - IPC C07D217/22 C07D401/12 C07D401/14 C07D405/12 C07D405/14 A61K31/4375 A61K31/472 A61K31/4725 A61P35/00 

Abstract RU 2644947 C2

FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely a heterocyclic compound of formula (I) or a stereo-isomer thereof or a pharmaceutically acceptable salt, where X is CH or N; Z is (i) NH(CH2)nCHR1Ar, where n is 0 or 1, or (ii) is 1-alkyl-4-aryl-pyrrolidin-3-ylamine, where alkyl is C1 alkyl, optionally substituted with a phenyl ring, and aryl is methoxy substituted phenyl; R1 is (a) hydrogen, (b) C1-C6 alkyl optionally substituted with a hydroxyl group, (c) from 4 to 5 member heterocycle containing 1 hetero atom selected from N, where the heterocycle is optionally substituted with one group selected from the group consisting of halogen, or (d) 5 member heteroaryl containing 1 or 2 hetero atoms selected from N, where heteroaryl is optionally substituted with one group selected from C1-6 alkyl; Ar is phenyl, pyridinyl or indolyl optionally substituted with from 1 to 2 groups independently selected from (a) C1-6 alkoxy, (b) halogen, (c) C1-6 halogenalkoxy, (d) cyano, (e) benzyl, (f) phenoxy, where said phenoxy is optionally substituted with halogen or C1-6 alkyl, (g) 4-methylpiperazin-1-yl or (h) heteroaryl selected from the group consisting of pyridinyl, pyrazinyl, pyrimidinyl and pyrazolyl, where said heteroaryl is optionally substituted with one C1-10 alkyl; R2 is selected from the group consisting of (a) C1-5 hydroxyalkyl, (b) C1-6 haloalkyl, (c) heterocyclyl, where said heterocyclyl is selected from the group consisting of tetrahydropyranyl, tetrahydrofuranyl, 2-oxa-bicyclo[2,2,1]heptan-5-yl and pyrrolidinyl, and where said heterocyclyl is optionally substituted with 1 group independently selected from the group consisting of halogen, C1-3 hydroxyalkyl or oxo, (d) heteroaryl, where said heteroaryl is selected from the group consisting of pyrazolyl and pyridinyl, and where said heteroaryl is optionally substituted with 1-2 C1-3 alkyl groups, (e) C3 cycloalkyl-C1-2 alkyl, where said C3 cycloalkyl-C1-2 alkyl is optionally substituted with hydroxyl. Invention is also relates to a pharmaceutical composition based on a compound of formula (I), method of ERK protein kinase activity inhibiting, method of a hyperproliferative disorder treating or severity reducing and the use of a compound of formula (I).

.

EFFECT: produced are new heterocyclic compounds, which are useful in hyperproliferative disorder treating.

29 cl, 3 tbl, 34 ex

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RU 2 644 947 C2

Authors

Blejk Dzhim

Chen Khojfen

Chikarelli Mark

Gaudino Dzhon

Gazzard Lyuis

Kintz Sem

Mor Pit

Robardzh Kirk

Shvarts Dzhejkob

Chzhou Ajkhe

Dates

2018-02-15Published

2013-08-27Filed