PYRIMIDINE DERIVATIVES

FIELD: chemistry. ^ SUBSTANCE: invention relates to novel compounds having inhibitory effect on focal adhesion kinase (FAK) and/or anaplastic lymphoma kinase (ALK) of formula (I) ^ , where R0 denotes hydrogen; R1 is a saturated 6-member monocyclic or 10-member bicyclic heterocycle containing 1 or 2...

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Hauptverfasser: MIJAKI TAKAKHIRO, REZEL' IOGANNES, KAVAKHARA EHJDZHI
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: chemistry. ^ SUBSTANCE: invention relates to novel compounds having inhibitory effect on focal adhesion kinase (FAK) and/or anaplastic lymphoma kinase (ALK) of formula (I) ^ , where R0 denotes hydrogen; R1 is a saturated 6-member monocyclic or 10-member bicyclic heterocycle containing 1 or 2 heteroatoms independently selected from nitrogen and oxygen, which can be substituted with piperidinyl, (C1-C7)alkylpiperidinyl, hydroxy, (C1-C7)alkyl, piperazinyl, (C1-C7)alkylpiperazinyl; R2 and R3 together with the carbon or nitrogen atom to which they are bonded form a 5- or 6-member heterocycle containing one heteroatom selected from a nitrogen atom which is substituted with (C1-C7)alkyl and/or oxo- group, R4 is hydrogen; R5 is a halide; R6 is hydrogen; R7 is hydrogen; R8 is hydrogen; halide, (C1-C7)alkoxy; carbamoyl which is unsubstituted or substituted with (C1-C7)alkyl; (C1-C7)alkoxy(C1-C7)alkoxy; 5- or 6-member heterocycle containing one or two heteroatoms independently selected from nitrogen or oxygen, and is unsubstituted or substituted with a substitute independently selected from hydroxy, (C1-C7)alkyl, mono- or di(C1-C7)alkylamino, 6-member heterocycle containing one or two nitrogen ring atoms which are unsubstituted or substituted with (C1-C7)alkyl; 5- or 6-member heterocycle(C1-C7)alkoxy containing one nitrogen ring atom which is unsubstituted or substituted with (C1-C7)alkyl; R9 is hydrogen; R10 is hydrogen, halide or (C1-C7)alkoxy; or their pharmaceutically acceptable salts. The invention also relates to a pharmaceutical composition and use of formula (I) compounds. ^ EFFECT: obtaining novel compounds with inhibitory effect on focal adhesion kinase (FAK) and/or anaplastic lymphoma kinase (ALK), having formula (I) . ^ 7 cl, 155 ex Изобретение относится к новым соединениям, обладающим ингибирующей активностью в отношении киназы фокальных контактов (FAK) и/или киназы клеток анапластической лимфомы (ALK) формулы (I) ! ! где R0 означает водород; R1 означает насыщенный 6-членный моноциклический или 10-членный бициклический гетероцикл, включающий 1 или 2 гетероатома, независимо выбранных из азота и кислорода, который может быть замещен пиперидинилом, (С1-С7)алкилпиперидинилом, гидрокси, (С1-С7)алкилом, пиперазинилом, (С1-С7)алкилпиперазинилом; R2 и R3 образуют вместе с углеродом и азотом, с которыми они соединены, 5- или 6-членный гетероцикл, включающий один гетероатом, выбранный из атома азота, который является замещенным (С1-С7)алкилом и/или оксогруп