FIELD: medicine; pharmaceuticals.
SUBSTANCE: invention relates to a method for inhibiting RET, comprising administering to a patient a compound represented by formula (I)
,
where A is pyrazolyl, substituted with n-number of substitutes R1; R1 is halogen, cyano, C1-C6 alkyl, unsubstituted or substituted with at least one substitute selected from a group consisting of halogen and C1-C6 alkoxy, C3-C7 cycloalkyl, unsubstituted or substituted with at least one substitute selected from a group consisting of C1-C6 alkyl and halogen, C6 aromatic hydrocarbon substituted with at least one substitute selected from a group consisting of C1-C6 alkyl and halogen; or C4 monocyclic unsaturated heterocyclic group containing 1 heteroatom selected from oxygen and sulfur, which is unsubstituted or substituted with at least one substitute selected from a group consisting of C1-C6 alkyl and halogen; R2 is C1-C10 alkyl unsubstituted or substituted with at least one substitute selected from a group consisting of halogen, C1-C6 alkoxy, C3-C7 cycloalkyl, which can be substituted with C1-C4 alkyl, phenyl, one C4 monocyclic unsaturated heterocyclic group containing 1 heteroatom selected from oxygen and sulfur, C3-C7 cycloalkyl, unsubstituted or substituted with at least one substituent 1–2 times, selected from a group consisting of C1-C6 alkyl, halogen, C1-C6 haloalkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, unsubstituted or substituted with halogen, C4-C12 bonded cycloalkyl, unsubstituted or substituted 1–3 times with C1-C6 alkyl or C3-C10 monocyclic or bicyclic saturated or unsaturated heterocyclic group, containing 1–3 identical or different heteroatoms selected from nitrogen, oxygen and sulfur, which is unsubstituted or substituted with C1-C6 alkyl; X is N or CR3, where R3 is hydrogen, halogen, cyano, C1-C6 alkyl, unsubstituted or substituted C1-C6 alkoxy, C2-C6 alkynyl substituted with at least one substitute selected from a group consisting of C1-C6 alkyl, which can be substituted with hydroxy, C1-C6 alkoxy, pyridinyl, C3-C6 cycloalkyl, which can be substituted with hydroxy, N-C1-C6 alkylpyrazolyl, N-C1-C6 alkyl imidazolyl, morpholinyl, tetrahydropyranyl and imidazo(1,2-b)pyridazinyl, C1-C6 alkoxy, unsubstituted or substituted with tetrahydrofuran, n is an integer ranging from 0 to 3.
EFFECT: disclosed are a condensed pyrimidine compound or salt thereof.
36 cl, 4 dwg, 19 tbl, 90 ex
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Authors
Dates
2020-08-11—Published
2016-09-07—Filed