| 摘要 |
Polycyclic salts of the formula A-XN+CH2-(Y)n-(CH2)p-(Z)q-L-(T)r-M I wherein A- is the anion of a strong organic or inorganic acid; XN+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R1, R2 and R3; n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15; Y is CH2, C(H,OH) or C(O); Z is O, S, CH2, C(O), NQ1, SO2, C(O)O, OC(O), C(O)N(Q1) or N(Q1)C(O); L is p-phenylene substituted by R4; and M is phenyl substituted by R5 and R6, T has one of the meanings given above, for Z or is C(CH3)2, C2H4, C(Q2)=C(Q3), C 3BOND C, CH2C(O), C(O)CH2, CH2O or OCH2, R1 is a group Ar, Ar-C1-4-alkyl, ArO or Arc(O), Ar is phenyl substituted by R7, R8 and R9; R2 and R3 individually are H, C1-4-alkyl, C1-4-alkoxy or C6H5, with the proviso that the N-atom in the 3-position of an imidazolium group XN+ is substituted by Ar, Ar-C1-4-alkyl or C1-4-alkyl, R4', R5, R6, R7, R8 and R9 individually are H, halogen, CF3, NO2, CN, C1-4-(alkyl, alkoxy, alkylthio or alkylsulphonyl), SO2N(R,Q), C(O)N(Q4, Q5), C(O)Q4, C(O)OQ4 or OC(O)Q4, R, Q, Q1+L, Q2 and Q3 individually are H or C1-4-alkyl, and Q4 and Q5 individually are C1-4-alkyl inhibit the intestinal resorption of cholesterol and of bile salts in the enterohepatic circulation. These salts containing a quaternary N-atom can be manufactured starting from corresponding amines.
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