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Claims for Patent: 5,385,929

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Claims for Patent: 5,385,929

Title: [(Hydroxyphenylamino) carbonyl] pyrroles
Abstract:2-(4-Fluorophenyl)-.beta.,.delta.-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[( hydroxyphenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, and their lactone forms, and salts and solyates thereof, inhibit cholesterol biosynthesis, and thus are useful in treating hypercholesterolemia.
Inventor(s): Bjorge; Susan M. (Ann Arbor, MI), Black; Ann E. (Tecumseh, MI), Roth; Bruce D. (Ann Arbor, MI), Woolf; Thomas (Dexter, MI)
Assignee: Warner-Lambert Company (Morris Plains, NJ)
Application Number:08/238,120
Patent Claims: 1. A compound of the formula ##STR17## where R.sup.1 is hydrogen or a hydroxy protecting group and solyates thereof or the open chain form of the formula ##STR18## and the pharmaceutically acceptable salts and solyates thereof.

2. A compound of claim 1 wherein R.sup.1 is benzyl.

3. A compound of claim 1 wherein R.sup.1 is hydrogen.

4. A compound of claim 3 which is ##STR19##

5. The compound of claim 4 which is (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N-(4-hydroxyphenyl)-4-phen yl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carbo xamide.

6. The compound of claim 4 which is (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N-(3-hydroxyphenyl)-4-phen yl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carbo xamide.

7. The compound of claim 4 which is (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N-(2-hydroxyphenyl)-4-phen yl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carbo xamide.

8. A compound of claim 3 which is ##STR20## or a pharmaceutically acceptable salt thereof.

9. The compound of claim 8 which is [3R,5R]-2-(4-fluorophenyl)-.beta.,.delta.-dihydroxy-5-(1-methylethyl)-3-ph enyl-4-[(4-hydroxyphenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, sodium salt.

10. The compound of claim 8 which is [3R,5R]-2-fluorophenyl-.beta.,.delta.-dihydroxy-5-1-methylethyl-3-phenyl-4 -[(3-hydroxyphenylamine)carboxyl]-1H-pyrrole-1-heptanoic acid, sodium salt.

11. The compound of claim 8 which is [3R,5R]-2-fluorophenyl-.beta.,.delta.-dihydroxy-5-(1-methylethyl)-3-phenyl -4-[(2-hydroxyphenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, sodium salt.

12. A pharmaceutical formulation comprising a compound of claim 1 together with a pharmaceutically acceptable carrier.

13. A formulation of claim 12 wherein the active ingredient is a compound in which R.sup.1 is hydrogen.

14. A formulation of claim 13 wherein the active ingredient is a compound of the formula ##STR21##

15. A formulation of claim 13 wherein the active ingredient is a compound of the formula ##STR22## or a pharmaceutically acceptable salt thereof.

16. A method of inhibiting cholesterol synthesis in an animal comprising administering a compound of claim 1.

17. The method of claim 16 employing a compound wherein R.sup.1 is hydrogen.

18. A method of treating a mammal suffering from conditions of hypercholesterolemia by administering a compound of claim 1 wherein R.sup.1 is hydrogen.
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