[R-(R*R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, its lactone form and salts thereof

Abstract

[R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-((1-methylethyl)-3-phenyl-4-[(phenylamino)-carbonyl)]-1H-pyrrole-1-heptanoic acid or (2R-trans)-5-(4-fluoro-phenyl)-2-(1-methylethyl-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide; and pharmaceutically acceptable salts thereof.

1. [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)-carbonyl]-1H-pyrrole-1-heptanoic acid or (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide; or pharmaceutically acceptable salts thereof. 
     
     
       2. A compound of  claim 1  which is [R-(R*R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid. 
     
     
       3. A compound of  claim 1  which is (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide. 
     
     
       4. The monosodium salt of the compound of  claim 2 . 
     
     
       5. The monopotassium salt of the compound of  claim 2 . 
     
     
       6. The hemicalcium salt of the compound of  claim 2   [R-( R*,R* )]-   2   -(   4   - fluorophenyl )-β,δ- dihydroxy -   5   -(   1   - methylethyl )-   3   - phenyl -   4   -[( phenylamino )- carbonyl] -   1 H - pyrrole -   1   - heptanoic acid . 
     
     
       7. The N-methylglucamine salt of the compound of  claim 2 . 
     
     
       8. The hemimagnesium salt of the compound of  claim 2 . 
     
     
       9. The hemizinc salt of the compound of  claim 2 . 
     
     
       10. The 1-deoxy-1-(methylamino)-D-glucitol mixture with the compound of  claim 2 . 
     
     
       11. A pharmaceutical composition for treating hypercholesterolemia comprising a hypocholesterolemic effective amount of a compound of  claim 1  and a pharmaceutically acceptable carrier. 
     
     
       12. A method of inhibiting cholesterol synthesis in a human suffering from hypercholesterolemia comprising administering a compound of  claim 1  in unit dosage form. 
     
     
       13. A pharmaceutical composition for treating hypercholesterolemia comprising a hypocholesterolemic effective amount of the hemicalcium salt of [R-( R*,R* )]-   2   -(   4   - fluorophenyl )-β,δ- dihydroxy -   5   -(   1   - methylethyl )-   3   - phenyl -   4   -[( phenylamino )- carbonyl] -   1 H - pyrrole -   1   - heptanoic acid and a pharmaceutically acceptable carrier.   
     
     
       14. A method of inhibiting cholesterol synthesis in a human suffering from hypercholesterolemia comprising administering to said human the hemicalcium salt of [R-( R*,R* )]-   2   -(   4   - fluorophenyl )-β,δ- dihydroxy -   5   -(   1   - methylethyl )-   3   - phenyl -   4   -[( phenylamino )- carbonyl] -   1 H - pyrrole -   1   - heptanoic acid in unit dosage form.