Phenyl-pyrimidinium, thiazolium or imidazolium salts and use in inhibiting intestinal resorption of cholesterol and bile salts

摘要

Polycyclic salts of the formula ##EQU1## wherein A.sup.- is the anion of a strong organic or inorganic acid;PPXN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R. sup. 1, R.sup.2 and R.sup.3 ;PPn, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;PP Y is CH. sub.2, C(H,OH) or C(O);PPZ is O, S, CH.sub.2, C(O), NQ. sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O); P PL is p-phenylene substituted by R.sup.4 ; andP PM is phenyl substituted by R.sup.5 and R.sup.6,PP T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C. sub.2 H.sub. 4, C(Q.sup.2)C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O) CH.sub.2, CH. sub.2 O or OCH.sub.2,PPR.sup.1 is a group Ar, Ar--C.sub.1- 4 -alkyl, ArO or Arc(O),PPAr is phenyl substituted by R. sup.7, R.sup.8 and R.sup.9 ;PPR.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C. sub.6 H.sub. 5,PPwith the proviso that the N-atom in the 3-position of an imidazolium group XN.sup.+ is substituted by Ar, Ar-C. sub.1-4 -alkyl or C.sub.1-4 -alkyl,PPR.sup.4 ', R.sup.5, R.sup.6, R.sup. 7, R.sup.8 and R.sup.9 individually are H, halogen, CF. sub.3, NO.sub.2, CN, C.sub.1-4 -(alkyl, alkoxy, alkylthio or alkylsulphonyl), SO.sub.2 N(R, Q), C(O)N(Q.sup.4, Q.sup.5), C(O)Q.sup.4, C(O)OQ.sup.4 or OC(O)Q.sup.4, PPR, Q, Q.sup.1 Q.sup.2 and Q.sup.3 individually are H or C.sub.1-4 -alkyl, andPPQ. sup.4 and Q.sup.5 individually are C.sub.1-4 -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.