Phosphonamide ACAT inhibitors
AssigneeWarner-Lambert Company
InventorsWilliam Howard Roark, Bruce David Roth
Life of this patent
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Abstract
The present invention is directed to compounds useful for the regulation of cholesterol of Formula I, methods for using them and pharmaceutical compositions thereof, ##STR1## wherein Ar and Ar.sup.1 are each independently selected from unsubstituted or substituted phenyl which substituents are from 1-5 in number and are each independently selected from alkyl, alkoxy, hydroxy, halogen, nitro, trifluoromethyl, COOH, and COOalkyl; X is --NH--, --O--, --S--, or --(CH.sub.2).sub.0-4 --, and R is hydrogen, alkyl, or phenyl.
Claims7
Compounds of the formula (I) ##STR13## or a pharmaceutically acceptable salt thereof wherein:
- Ar and Ar.sup.1 are each independently selected from substituted phenyls which substituents are from 1-5 in number and at least one is at the ortho position and are each independently selected from alkyl, alkoxy, hydroxy, halogen, nitro, trifluoromethyl, COOH, and COOalkyl,
- X is --(CH.sub.2).sub.0-4 --;
- and
- R is hydrogen, alkyl, or phenyl.
A compound of formula I ##STR14## or a pharmaceutically acceptable salt thereof wherein Ar is phenyl substituted with 3 substituents each independently selected from isopropyl and chloride;
- Ar.sup.1 is phenyl substituted with 3 isopropyl substituents;
- and
- X is CH.sub.2.
A pharmaceutical composition for regulating plasma cholesterol concentration comprising an effective amount of a compound of formula I ##STR15## or a pharmaceutically acceptable salt thereof wherein:
- Ar and Ar.sup.1 are each independently selected from substituted phenyls which substituents are from 1-5 in number and are each independently selected from alkyl, alkoxy, hydroxy, halogen, nitro, trifluoromethyl, COOH, and COOalkyl;
- X is --(CH.sub.2).sub.0-4 --;
- and
- R is hydrogen, alkyl, or phenyl,
- and a pharmaceutically acceptable carrier.
A method of treating hypercholesterolemia comprising administering to a patient a therapeutically effective amount of a compound of formula I ##STR16## or a pharmaceutically acceptable salt thereof wherein:
- Ar and Ar.sup.1 are each independently selected from substituted phenyls which substituents are from 1-5 in number and are each independently selected from alkyl, alkoxy, hydroxy, halogen, nitro, trifluoromethyl, COOH, and COOalkyl;
- X is --(CH.sub.2).sub.0-4 --;
- and
- R is hydrogen, alkyl, or phenyl.
A method of treating atherosclerosis comprising administering to a patient a therapeutically effective amount of a compound of formula I ##STR17## or a pharmaceutically acceptable salt thereof wherein:
- Ar and Ar.sup.1 are each independently selected from substituted phenyls which substituents are from 1-5 in number and are each independently selected from alkyl, alkoxy hydroxy, halogen, nitro, trifluoromethyl, COOH, and COOalkyl;
- X is --(CH.sub.2).sub.0-4 --;
- and
- R is hydrogen, alkyl, or phenyl.
Dependencies are inferred from the claim text.