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How a Cholesterol-Lowering Drug Molecule Was Patented

This patent protects the specific chemical structure of a molecule designed to lower cholesterol, including its various salt forms and its use in medicine.

Granted 1993ExpiredExpired 2011Owned by Warner Lambert Co LLCInvented by Bruce D. Roth

Original patent title: “[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

Plain-English explanation by SahiLast reviewed · June 15, 2026

This patent protects the specific chemical structure of a molecule designed to lower cholesterol, including its various salt forms and its use in medicine. Granted to Warner Lambert Co LLC in 1993 with 13 claims and 519 forward citations.

Key facts

Patent numberUS 5273995
StatusExpired
FieldBiotech & Medicine
AssigneeWarner Lambert Co LLC
InventorBruce D. Roth
Filed1991
Granted1993
Claims13
Times cited519
LitigationNone on record
Value · $113K$360KModest

Coverage

What does this patent actually cover?

This patent specifically claimsclaimsThe numbered statements at the end of a patent that legally define what the inventor owns.Read more → a complex organic molecule, identified by its chemical name and structure, that is designed to treat high cholesterol. It covers the molecule itself, including its acid and lactone forms, as well as various pharmaceutically acceptable salts like sodium, potassium, calcium, and magnesium salts. ClaimclaimA numbered sentence at the end of a patent that legally defines what the inventor owns. The most important section.Read more → 11 describes a pharmaceutical composition containing this molecule for treating hypercholesterolemia (high cholesterol). Claim 12 outlines a method for treating high cholesterol in humans by administering this molecule.

The gap

What does this patent NOT cover?

  • Does not cover other types of cholesterol-lowering drugs that do not use this specific chemical structure.
  • Does not cover the synthesis process or manufacturing methods for the molecule.
  • Does not cover the use of the molecule for treating conditions other than hypercholesterolemia.
  • Does not cover the molecule if it is not in a pharmaceutically acceptable salt form.
  • Does not cover the molecule if it is not in the specific stereochemical configuration claimed.

These exclusions are unique to PatentBrief — derived from the actual claim language, not patent-office boilerplate.

What made this novel

The noveltynoveltyThe requirement that an invention be different from anything publicly known before its priority date.Read more → lies in the precise chemical architecture of the molecule, which was found to be highly effective at inhibiting cholesterol synthesis. This specific structure, including its stereochemistry, was the key to its potent therapeutic effect.

[R-(R*R*)]-2-(4-fluorophenyl)-…(Primary claim)pharmaceuticalbiotech

Schematic visualization of the patent's claim structure. Hand-drawn diagrams in progress for each landmark patent.

Where you've seen this

Real-world examples

01

Atorvastatin (Lipitor)

Why it matters

The bigger picture

This patent is significant because it covers a key molecule that became the active ingredient in a widely used cholesterol-lowering drug. The drug, known as atorvastatin (marketed as Lipitor), became one of the best-selling pharmaceuticals of all time, profoundly impacting the treatment of cardiovascular disease.

Filed

February 26, 1991

Granted

December 28, 1993

Market context

Who's building on this

Companies in this space

Pfizer, the company that developed and marketed Lipitor, was the primary beneficiary of this patent. Following its expiration, numerous generic pharmaceutical companies now manufacture and sell generic versions of atorvastatin.

Market impact

This patent protected a blockbuster drug that dominated the hypercholesterolemia market for years. Its commercial success led to massive revenue for the assigneeassigneeThe entity that owns the patent — usually the inventor's employer or a company.Read more → and significantly influenced the pharmaceutical industry's focus on statin drugs for cardiovascular health. The patent's expiration led to a surge in generic competition, drastically lowering the cost of atorvastatin.

Claim 1 — Plain English

What this patent covers

This patent specifically claims a complex organic molecule, identified by its chemical name and structure, that is designed to treat high cholesterol. It covers the molecule itself, including its acid and lactone forms, as well as various pharmaceutically acceptable salts like sodium, potassium, calcium, and magnesium salts. Claim 11 describes a pharmaceutical composition containing this molecule for treating hypercholesterolemia (high cholesterol). Claim 12 outlines a method for treating high cholesterol in humans by administering this molecule.

The clever bit

The novelty lies in the precise chemical architecture of the molecule, which was found to be highly effective at inhibiting cholesterol synthesis. This specific structure, including its stereochemistry, was the key to its potent therapeutic effect.

What it does not cover

  • Does not cover other types of cholesterol-lowering drugs that do not use this specific chemical structure.
  • Does not cover the synthesis process or manufacturing methods for the molecule.
  • Does not cover the use of the molecule for treating conditions other than hypercholesterolemia.
  • Does not cover the molecule if it is not in a pharmaceutically acceptable salt form.
  • Does not cover the molecule if it is not in the specific stereochemical configuration claimed.

Patent timeline

Filing

Application submitted to the patent office

Publication

Application published, typically 18 months after filing

Grant

Patent officially issued

PatentBrief Score

Impact Score

Moderate

Citation count

40/40

Highly cited

Claim breadth

9/20

Moderate scope

Recency

0/20

Older than 20 years

Assignee scale

0/20

Independent or smaller assigneeassigneeThe entity that owns the patent — usually the inventor's employer or a company.Read more →

PatentBrief Impact Score — based on citation count, claim breadth, recency, and assignee scale. Not a legal assessment.

Heuristic Value Estimate

What this patent might be worth

Modest

$113K$360K

Midpoint $225K · expired or expiring · industry ×3.0

Adjust inputs →

Heuristic only — blends forward/backward citation counts, claim scope, time remaining, litigation history, and CPC-derived industry baseline. Real valuations need a professional appraisal.

The original legal language

Original claims

13 claims as filed with the patent office.

Concepts involved

ClaimPrior artNon-obviousnessNoveltySpecificationAssigneePatent term

Citations

Patent lineage

Cites earlier patents

1

earlier patents this invention cites as foundations

View prior art →

Cited by later patents

519

later patents that build on this invention

View patents →

Cite this patent

Roth, B. D. (1993). How a Cholesterol-Lowering Drug Molecule Was Patented (U.S. Patent No. 5,273,995). U.S. Patent and Trademark Office. https://patentbrief.org/patent/us/5273995/viagra-sildenafil

Auto-generated from the patent record. Double-check author order and the issue date against the official USPTO document before submitting.

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Common Questions

Frequently Asked Questions

What does How a Cholesterol-Lowering Drug Molecule Was Patented cover?

This patent protects the specific chemical structure of a molecule designed to lower cholesterol, including its various salt forms and its use in medicine.

Who owns patent US 5273995?

Warner Lambert Co LLC owns this patent, granted in 1993.

When does this patent expire?

This patent has expired and is now in the public domain — anyone can use the invention freely.

What is patent US 5273995 cited by?

This patent has been cited by 519 later patents that build on its ideas.

What problem does this patent solve?

This patent is significant because it covers a key molecule that became the active ingredient in a widely used cholesterol-lowering drug. The drug, known as atorvastatin (marketed as Lipitor), became one of the best-selling pharmaceuticals of all time, profoundly impacting the treatment of cardiovascular disease.

What does this patent NOT cover?

Does not cover other types of cholesterol-lowering drugs that do not use this specific chemical structure.

Same assignee

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US 4681893·1987

The Chemical Formula for Atorvastatin, the Active Ingredient in Lipitor

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Last reviewed: June 15, 2026 · PatentBrief is not a law firm and this is not legal advice.