SERIN / TREONIN KINASE INHIBITORS FOR TREATING OF HYPEROPLIFERATIVE DISEASES

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(CH)CHRAr, where n is 0 or 1, or (ii) is 1-alkyl-4-aryl-pyrrolidin-3-ylamine...

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Hauptverfasser: GAZZARD Lyuis, SHVARTS Dzhejkob, CHEN Khojfen, BLEJK Dzhim, CHZHOU Ajkhe, ROBARDZH Kirk, MOR Pit, KINTZ Sem, CHIKARELLI Mark, GAUDINO Dzhon
Format: Patent
Sprache:eng ; rus
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Zusammenfassung: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(CH)CHRAr, where n is 0 or 1, or (ii) is 1-alkyl-4-aryl-pyrrolidin-3-ylamine, where alkyl is Calkyl, optionally substituted with a phenyl ring, and aryl is methoxy substituted phenyl; Ris (a) hydrogen, (b) C-Calkyl 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 Calkyl; Ar is phenyl, pyridinyl or indolyl optionally substituted with from 1 to 2 groups independently selected from (a) Calkoxy, (b) halogen, (c) Chalogenalkoxy, (d) cyano, (e) benzyl, (f) phenoxy, where said phenoxy is optionally substituted with halogen or Calkyl, (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 Calkyl; Ris selected from the group consisting of (a) Chydroxyalkyl, (b) Chaloalkyl, (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, Chydroxyalkyl 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 Calkyl groups, (e) Ccycloalkyl-Calkyl, where said Ccycloalkyl-Calkyl 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 Изобретение относится к области органической химии, а именно к гетероциклическому соединению формулы (I) или к его стереоизомеру или фармацевтически приемлемой