FUKS Tomas (DE),ФУКС Томас (DE),EMDE Ulrikh (DE),ЭМДЕ Ульрих (DE),BUKHSHTALLER Khans-Peter (DE),БУХШТАЛЛЕР Ханс-Петер (DE),MEDERSKI Verner (DE),МЕДЕРСКИ Вернер (DE)
申请号：
RU2015153094
公开号：
RU0002701193C2
申请日:
2014.05.08
申请国别(地区):
RU
年份:
2019
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention relates to a novel compound of formula (I), a physiologically acceptable salt thereof and/or a stereoisomer having the properties of DNA-dependent protein kinase (DNA-PC). In formula (I),X is CH, CF, S or N, Y is CH, S or N, Z is C or N, , if Z = C, then forms a double bond together with a simple bond, or is absent, if Z = N, n is equal to 1 or 2, where if n = 1, then X = S, and if n = 2, then both X = CH, or X, bonded to the pyrimidine ring, is CF, and X, which is not bonded to the pyrimidine ring, is CH, or one X is CH, and the other X is N； m is equal to 1 or 2, where if m = 1, then Y = S, and if m = 2, then both Y = CH, or one Y is CH, and other Y is N； R1, R2, R3, R4 independently of each other are H, Hal, CN, OH, CONH2, CONH (LA) or LA； R5 is H, Hal, CN or C≡CH； Cyc is phenyl which can be unsubstituted or mono- or disubstituted independently by R6, or is Het1； Het1 is a mono- or bicyclic 5–10-member heterocycle having 1–3 N, 0 and/or S atoms, or 1–4 N atoms, which can be unsubstituted or mono-, di- or tri-substituted independently by R6, or can be monosubstituted with Het2； R6 is Hal, LA, oxo, CN or NH2； LA is a straight or branched alkyl having 1–5 C atoms, which can be saturated or partially unsaturated, in which 1–3 H atoms can be replaced by Hal, and/or one H atom can be replaced with CN or Het2, and/or one or two CH2 groups can be replaced by O, NH, N (CH3) or CO； Het2 is 3–5-member aliphatic homo- or heterocycle having 0, 1, 2 or 3 N, 0 and/or S atoms which is unsubstituted； Hal is F, Cl, Br or I； where value H covers 1H and deuterium. Method of producing a compound of formula (I) and/or a physiologically acceptable salt and/or stereoisomer thereof involves the following steps: (a) reacting a compound of formula (V), ,in which LG is a common leaving group, such as Hal, and R5, X, n and Z have values given in cl. 1, with a compound of formula (IV), in which A is a boronic acid or a boronic acid ester, and R1, R2, R3,
