| 摘要 |
Pyrimidine-4,6-dicarboxylic acid 4-benzylamide 6-(substituted alkyl)-amide compounds (I) are new. Pyrimidine derivatives of formula (I) (including all stereoisomeric forms and their mixtures in any ratio) and their salts are new. R1 = H or alkyl; R2 = alkyl, substituted by 1-3 groups R2a; R2a = aryloxyalkyl; -R-N(R8)-COO-alkyl; -CONR9R10; aryl substituted by 1-3 groups R2b; -CO-NR8-R-Ar'; -CO-NR8-R-Het'; -NH-Ar'; or -NH-Het'; R = direct bond or alkylene; R8 - R10 = H or alkyl; or NR9R10 = 5-7 membered saturated ring, optionally containing 1 or 2 additional O, S, NH or N(alkyl) heteroatom(s); R2b = -CH2COOR8, -R-CONR9R10, -R-CONHCN, -O-R-CO-NR9R10, -S(O)y-alkylene-COOR8, -S(O)z-alkylene-CONR9R10, -R-CO-NR8-R-NR9R10, -CO-NR8-R-Het, -CO-NR8-R-Ar, -R-NR9R10, -(CH2)y-NR8-CO-Alk, -(CH2)x-NR8-CO-R-Ar, -(CH2)x-NR8-CO-R-Het, -(CH2)x-NR8-CO-O-Alk, -(CH2)x-NR8-CO-O-R-Ar, -(CH2)x-NR8-CO-O-R-Het, -(CH2)x-NR8-CO-R-NR11R12, -(CH2)x-NR8-SO2-R-Ar, -(CH2)x-NR8-SO2-R-Het, -(CH2)x-NR8-SO2-NR8-Alk, -(CH2)x-NR8-SO2-NR8-R-Ar, -(CH2)x-NR8-SO2-NR8-R-Het, -(CH2)x-NR8-CO-NR8-SO2-R13, -SO2-NR8-R-Ar, -R'-SO2-NR8-R-Het, -SO2-NR8-R-Alk, -SO2-R-Ar, -SO2-R-Het, -O-Het or -Het; Het = saturated or unsaturated, mono- or bicyclic, 3-10 membered heterocyclic ring system, containing 1-3 of N, O and/or S as heteroatom(s)and os by 1-3 groups Q; Q = halo, CN, NO2, OH, NH2, alkoxycarbonyl, COOH, alkyl (os by 1-3 halo) or alkoxy (os by 1-3 halo); y = 1 or 2; z = 0-2; Ar = aryl (os by 1-3 groups Q); Alk = alkyl (os by 1-3 groups Q); x = 0-4; Alk' = alkyl; R11, R12 = H, alkyl, -R-Ar, -R-Het, alkylcarbonyl, -CO-R-aryl, -CO-R-Het, alkylsulfonyl, -SO2-R-aryl or -SO2-R-Het; R13 = alkyl, aryl or arylalkyl; Ar' = aryl (os by 1-3 of R2b or Q); Het'' = as for Het, but where the optional substituents include R2b as well as Q; R3 - R7 = H, halo, alkyl (os by 1-3 halo), alkoxy (os by 1-3 halo) or alkylthio; or R4 + R5 or R5 + R6 = group completing a 5- or 6-membered saturated or aromatic ring, optionally containing 1 or 2 N, O and/or S heteroatom(s) and os by 1 or 2 halo; unless specified otherwise alkyl or alkylene moieties have 1-6C and aryl moieties 6-14C. An Independent claim is included for the preparation of (I).
|
