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US 5,494,918 AGranted
Multicyclic tertiary amine polyaromatic squalene syntase inhibitors
AssigneeRhone-Poulenc Rorer Pharmaceuticals Inc.
InventorsKent Neuenschwander, Dilip Amin, Anthony C. Scotese, Robert L. Morris
Life of this patent
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Abstract
This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
Claims11
A compound of the formula ##STR135## where:
- Ar I is a substituted or unsubstituted phenylene or naphthylene and where the substituents may be located at any appropriate position of the ring system and are described by R;
- Ar II is a substituted or unsubstituted benzoxazolyl and where the substituents may be located at any appropriate position of the ring system and are described by R;
- A is ##STR136## B is CR'R', O or a bond;
- D is CR'R', R'C.dbd.CR', C.tbd.C, C.dbd.CHR' or a bond;
- R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are independently hydrogen or (CH.sub.2).sub.x --X where x is 0-5 and X is hydrogen, alkyl, alkenyl, aralkyl, hydroxy, alkoxy, aralkoxy, aryloxy, acyloxy, aryl, halo, amino, mono- and di-alkylamino or acylamino;
- R' is hydrogen, alkyl or aralkyl;
- R is hydrogen, alkyl, aralkyl, hydroxy, alkoxy, aralkoxy, acyloxy, halo, haloalkyl, amino, mono- and di-amino or acylamino;
- and
- a, b, d and e are 0-4;
- or
- a pharmaceutically acceptable salt thereof.
8 more elements
Dependencies are inferred from the claim text.