The Chemical Formula for Atorvastatin, the Active Ingredient in Lipitor
This patent describes the chemical structure of a class of molecules designed to block the enzyme responsible for cholesterol production in the human body.
Patent Number
US 4681893
Status
Active
Filing Date
May 30, 1986
Grant Date
July 21, 1987
Expiration
~May 2006 (estimated)
Claims
10
Assignee
Warner Lambert Co LLC
Inventors
Bruce D. Roth
Citations
340 forward · 7 backward
What it covers
The patent claims a specific chemical structure—a pyrrole-based compound—that acts as an inhibitor of the enzyme HMG-CoA reductase. By blocking this enzyme, the compound prevents the liver from synthesizing cholesterol. The structure includes a lactone ring, which can open into a hydroxy acid form that is biologically active in the body. Claim 5 specifically identifies the chemical structure that would later become known as Atorvastatin.
What it doesn't cover
- —Does not cover naturally occurring cholesterol-lowering compounds found in plants or fungi.
- —Does not cover other classes of cholesterol-lowering drugs like fibrates or bile acid sequestrants.
- —Does not cover the specific manufacturing process or industrial synthesis route for the compound.
- —Does not cover the use of these compounds for treating conditions unrelated to cholesterol biosynthesis.
The clever bit
The inventor successfully utilized a pyrrole core to create a potent, synthetic inhibitor that mimics the transition state of the HMG-CoA reductase reaction, effectively tricking the enzyme into shutting down.
Why it matters
This patent is the foundation for Atorvastatin, marketed as Lipitor. It became one of the most commercially successful pharmaceutical products in history, fundamentally changing how doctors treat high cholesterol and cardiovascular disease.
Real-world examples
- 1.Lipitor (Atorvastatin)
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US 4681893 · 2026