Details for Patent: 7,439,241

Summary for Patent: 7,439,241

Title:	Compounds, formulations, and methods for treating or preventing rosacea
Abstract:	In methods, compounds, and topical formulations for treatment of rosacea incorporating compounds represented by the formulas below: wherein each of R1, R2, and R3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R4 and R5 is independently hydrogen, alkyl, or alkoxy; and each of R6 and R7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A1, A3, and A4 is independently hydrogen or alkyl; and A2 is independently hydrogen or hydroxy; and wherein each of B1, B2, and B3 is independently hydrogen, hydroxy, or alkoxy; and each of B4 and B5 is independently hydrogen or alkyl, applying such compounds topically as sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions to treat rosacea and its symptoms.
Inventor(s):	Jack A. DeJovin, Isabelle Jean DeJovin
Assignee:	SANS ROSA PHARMACEUTICAL DEVELOPMENT Inc , Galderma Holding SA
Application Number:	US10/853,585
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,439,241
Patent Claim Types: see list of patent claims	Use; Composition;

United States Drug Patent 7,439,241: Claim Scope, Brimonidine Rosacea Protection, and Patent Landscape

U.S. Patent No. 7,439,241 protects a treatment method for reducing rosacea-associated skin redness by applying brimonidine or a pharmaceutically acceptable salt topically to the affected skin. The claim is broad at the ingredient and treatment-method level. It does not require a particular concentration, gel vehicle, dosage schedule, treatment duration, formulation excipient, or delivery device.

The patent is commercially important because its claim maps directly onto the core clinical use of topical brimonidine, including the use later commercialized as Mirvaso 0.33% gel. The claim does not protect brimonidine as a molecule, a pharmaceutical composition standing alone, or every use of brimonidine. Its enforceability depends on proving each method element and overcoming prior-art, written-description, enablement, and claim-construction challenges.

What does U.S. Patent 7,439,241 cover?

U.S. Patent 7,439,241, titled “Methods of Treating Rosacea,” claims a therapeutic method with five operative components:

Claim element	Scope
Patient	The treatment must be performed on a patient
Condition	The redness must be associated with rosacea
Treatment objective	The method must reduce the redness
Route	Brimonidine must be administered topically
Active ingredient	The composition must contain an effective amount of brimonidine or a pharmaceutically acceptable salt

The claim is therefore a method-of-use claim. It is not a composition claim and does not require the use of brimonidine tartrate specifically, although brimonidine tartrate is the commercially relevant pharmaceutically acceptable salt.

The patent issued on October 21, 2008, from an Allergan-related patent family. Its filing and priority history place the ordinary 20-year patent term in the 2025 period, subject to any applicable patent-term adjustment or extension. The precise enforceable expiration should be confirmed against the current USPTO patent record and Orange Book listing before making a launch or litigation decision. (U.S. Patent No. 7,439,241, 2008; USPTO, n.d.-a)

How should claim 1 of patent 7,439,241 be construed?

Claim 1 is broad because most technical parameters are expressed functionally rather than numerically.

“A method of reducing redness”

This language defines the claim by a therapeutic result. The accused treatment must be intended to reduce redness or must produce that result in the relevant factual context. The claim does not state a minimum percentage reduction, time period, measurement method, or clinical scoring system.

A product that produces only transient vasoconstriction could still fall within the claim if the other elements are satisfied. The absence of a duration limitation means that a short-lived reduction may be sufficient, unless a court construes the claim in light of the specification or prosecution history.

“Associated with rosacea”

This limitation narrows the claim to redness linked to rosacea. It excludes treatment of unrelated redness, such as redness caused solely by contact dermatitis, sunburn, acne, or trauma.

The claim does not appear limited to a particular rosacea subtype. It can potentially cover erythematotelangiectatic rosacea, papulopustular rosacea, or another rosacea presentation if the treated redness is associated with the disease. The commercial FDA indication is narrower in practical terms because Mirvaso is approved for persistent facial erythema of rosacea. (FDA, 2013)

“Topically administering”

Topical administration requires application to the skin rather than oral, injectable, ophthalmic, or systemic administration. A cream, gel, lotion, ointment, foam, solution, emulsion, or similar dermatological dosage form could satisfy this limitation if applied to the relevant skin site.

The claim does not require a particular product format. It also does not expressly require facial application, even though the commercial use is facial rosacea. The phrase “site of the redness on the skin” focuses the application on the affected area.

“A pharmaceutical composition”

The composition must be pharmaceutical in character. A cosmetic product containing brimonidine may raise a claim-construction issue if it is not presented or used as a pharmaceutical treatment. A product marketed for therapeutic reduction of rosacea redness presents a substantially stronger infringement case than an unmedicated cosmetic product.

“An effective amount”

“Effective amount” is a functional limitation. The amount must be sufficient to produce the claimed reduction in redness under the relevant conditions. The claim does not provide a fixed concentration.

This limitation creates flexibility for the patent owner but also creates factual disputes. A generic product containing brimonidine may satisfy the limitation even if it uses a different concentration from Mirvaso, provided the product is intended and capable of reducing rosacea-associated redness.

“Brimonidine or a pharmaceutically acceptable salt thereof”

The claim covers brimonidine in free-base form and pharmaceutically acceptable salts. Brimonidine tartrate is the principal commercial example.

The claim does not depend on a particular salt ratio, particle size, polymorph, excipient, preservative, pH, or manufacturing process. Those matters may be addressed by other patents in the family or by separate formulation and manufacturing patents.

What does patent 7,439,241 not claim?

The claim does not expressly cover:

• Brimonidine as a chemical compound in the abstract.
• Every topical use of brimonidine.
• Treatment of non-rosacea redness.
• A specific 0.33% concentration.
• A gel dosage form.
• A particular vehicle or excipient system.
• A specific once-daily dosing schedule.
• A defined treatment duration.
• A particular tube, pump, applicator, or package.
• The manufacture of brimonidine or brimonidine tartrate.
• The sale of a product without proof of a qualifying method of use.

This distinction is important under U.S. patent law. A generic manufacturer may avoid literal infringement of a formulation claim while still facing liability for a method-of-use claim if its labeling, marketing, or intended use directs treatment of rosacea redness.

How strong is the patent estate for topical brimonidine?

Patent 7,439,241 is strongest against a product that is specifically labeled for reducing rosacea redness. Its strength decreases where a competing product has a different indication, a restricted label, or a formulation designed for a use outside the claim.

The patent has several favorable characteristics:

1. It covers the central therapeutic use of topical brimonidine.
2. It does not require the Mirvaso brand, formulation, concentration, or excipient profile.
3. It can potentially cover multiple topical dosage forms.
4. It is not limited to a narrow numerical dosing range.
5. It reaches brimonidine salts, including brimonidine tartrate.

Its principal vulnerabilities are:

1. Prior art involving alpha-2 adrenergic agonists and vasoconstrictors.
2. Evidence that topical brimonidine use for facial redness was already known or suggested.
3. Challenges to whether the patent adequately describes and enables the full breadth of all topical brimonidine formulations and all rosacea-associated redness.
4. Disputes over whether an accused product is used for rosacea or merely for another dermatological condition.
5. Proof issues concerning the “effective amount” and the claimed reduction in redness.

A defendant could challenge validity under sections 102, 103, 112(a), or 112(b) of the Patent Act. A prior-art challenge would likely focus on references disclosing topical alpha-adrenergic therapy, cutaneous vasoconstriction, or treatment of rosacea-related erythema. A section 112 challenge would focus on the breadth of the functional terms and whether the specification supports the full scope of the claim. (35 U.S.C. §§ 102, 103, 112)

What patents protect Mirvaso and related topical brimonidine products?

The commercial product associated with the patented use is Mirvaso, a brimonidine tartrate topical gel approved by the FDA in 2013 for persistent facial erythema of rosacea. The patent landscape is broader than claim 1 of patent 7,439,241 and may include continuation patents directed to dosing, formulations, and other aspects of topical brimonidine therapy.

Protection category	Relevance to a competing product
Rosacea method-of-use claims	Can block labeled use for rosacea redness
Formulation claims	Can block a specific gel, vehicle, concentration, pH, or excipient combination
Dosing claims	Can block a defined dosing frequency or administration regimen
Manufacturing claims	Can create process or supply-chain barriers
Packaging or delivery claims	Can affect pumps, tubes, applicators, or unit-dose systems
Regulatory exclusivity	Can delay approval independently of patent expiration

U.S. Patent 7,439,241 should therefore be reviewed together with continuation and divisional applications, Orange Book listings, FDA patent certifications, and any terminal disclaimers. Patent-family members may have different claim language while sharing a common expiration date.

What is the FDA and Orange Book status of patent 7,439,241?

FDA approved Mirvaso topical gel 0.33% on July 25, 2013, for the topical treatment of persistent facial erythema of rosacea in adults. The approved active ingredient is brimonidine tartrate. (FDA, 2013)

For an ANDA applicant, an Orange Book-listed method-of-use patent can trigger a Paragraph IV certification if the applicant asserts that the patent is invalid, unenforceable, or will not be infringed. A Paragraph IV notice can lead to patent litigation and, if suit is filed within the statutory period, a 30-month stay of ANDA approval under the Hatch-Waxman framework. (21 U.S.C. § 355; FDA, n.d.)

The practical regulatory questions are:

• Whether patent 7,439,241 is currently listed for the relevant Mirvaso reference product.
• Whether the listing covers the proposed generic’s labeling.
• Whether the applicant made a Paragraph III or Paragraph IV certification.
• Whether the patent owner filed an infringement action.
• Whether a court entered an injunction, judgment, settlement, or license.
• Whether the generic label uses a skinny-label strategy that omits the patented rosacea indication.

An ANDA applicant may attempt to omit a patented method of use from its labeling if the remaining indications can be marketed lawfully. That strategy is more difficult where rosacea treatment is the principal or only commercially meaningful indication.

When does patent 7,439,241 lose exclusivity?

The ordinary patent term is expected to fall in the 2025 period based on the patent family’s filing history. Patent-term adjustment can move the expiration date beyond the basic 20-year term. Pediatric exclusivity, if granted for the relevant product and applicable to the listed patent, can add six months to certain FDA exclusivity rights.

Patent expiration does not automatically eliminate every barrier to competition. Later-expiring formulation or dosing patents may remain relevant. FDA regulatory exclusivity, court orders, settlement restrictions, supply agreements, and product-specific patents can also affect the timing of generic entry.

A launch analysis should separate:

Issue	Effect
Expiration of 7,439,241	Removes the principal method-of-use patent barrier if no other enforceable patent applies
Later formulation patent	May delay or constrain a competing formulation
Pediatric exclusivity	May delay FDA approval for the covered product or patent set
Paragraph IV litigation	Can delay approval through the 30-month stay
Skinny-label approval	May permit entry without the patented indication
Patent settlement	Can establish an agreed entry date earlier or later than full expiration

Which companies are challenging the topical brimonidine patent estate?

Generic competition has focused on brimonidine tartrate topical gel products intended to compete with Mirvaso. The relevant companies, applications, and litigation positions must be determined from current FDA Orange Book records, FDA approval announcements, ANDA litigation dockets, and any public settlement agreements.

A company can challenge the estate through:

• A Paragraph IV certification.
• An inter partes review petition at the Patent Trial and Appeal Board.
• A declaratory-judgment action.
• A non-infringement defense in district court.
• A skinny-label strategy.
• A design-around formulation.
• A launch after expiration or after a licensed entry date.

The patent’s method-of-use language makes labeling central. A competitor selling topical brimonidine for an unrelated indication may face lower infringement exposure than a company whose label expressly directs treatment of rosacea-associated redness.

How does patent 7,439,241 compare with formulation patents?

Patent 7,439,241 is broader in therapeutic concept but narrower in claim category than a formulation patent.

A formulation patent may require specific limitations such as:

• Brimonidine concentration.
• Carbomer or another gelling agent.
• Preservative system.
• pH range.
• Viscosity range.
• Particle-size distribution.
• Stability profile.
• Particular impurity limits.
• A specific delivery vehicle.

A competing product can avoid a formulation patent by changing the vehicle or excipient system. It may not avoid claim 1 of patent 7,439,241 if it still topically administers an effective amount of brimonidine to reduce rosacea-associated redness.

Conversely, a product could avoid claim 1 by removing the rosacea indication from its labeling while still potentially infringing a formulation claim, depending on the claim language and evidence of use.

Are biosimilar risks relevant to brimonidine?

No. Brimonidine is a small-molecule active ingredient, not a biologic. The relevant competitive pathway is an ANDA for a generic drug, not a biosimilar application under the Biologics Price Competition and Innovation Act.

The main regulatory and patent risks are therefore:

• ANDA patent certifications.
• Product-specific formulation patents.
• Method-of-use patent litigation.
• Labeling restrictions.
• Bioequivalence and pharmaceutical-equivalence requirements.
• Manufacturing and supply-chain controls.

What generic launch scenarios exist?

Full-label launch after patent expiry

A generic manufacturer may launch a topical brimonidine product with the rosacea indication after all relevant patents and exclusivity rights expire or are otherwise resolved.

Paragraph IV launch

The applicant may assert that patent 7,439,241 is invalid, unenforceable, or not infringed. The patent owner may sue, creating the potential for a 30-month stay and subsequent litigation.

Skinny-label launch

The applicant may omit the patented rosacea indication and market the product for an unpatented use, if FDA labeling rules permit the omission and the commercial opportunity remains viable.

Licensed entry

The patent holder and generic applicant may settle litigation through a license establishing a negotiated entry date and other commercial restrictions. The commercial effect depends on the licensed date, supply terms, authorized-generic provisions, and treatment of later patents.

Formulation design-around

A competitor may develop a different topical vehicle or dosage form. This can reduce exposure to formulation claims but does not necessarily avoid the broad method claim if the product is still directed to rosacea redness.

What is the commercial exposure associated with this patent?

The patent covers the indication that differentiates topical brimonidine from ordinary dermatological vasoconstrictors. Its commercial value is therefore linked to:

• Mirvaso sales before generic entry.
• The share of revenue attributable to rosacea treatment.
• The absence or presence of later formulation patents.
• The number of approved generic competitors.
• Reimbursement and dermatology prescribing patterns.
• The ability to maintain premium pricing after method-of-use expiry.

Once multiple generic products enter, price erosion is likely to depend more on formulation substitutability and pharmacy substitution than on the surviving value of the method claim.

Key Takeaways

• U.S. Patent 7,439,241 is a broad method-of-use patent for topical brimonidine treatment of rosacea-associated redness.
• Claim 1 does not require a 0.33% concentration, gel formulation, specific excipient, dosing schedule, or treatment duration.
• The claim covers brimonidine and pharmaceutically acceptable salts, including brimonidine tartrate.
• The principal infringement risk targets products labeled for reducing rosacea redness.
• The patent does not cover brimonidine as a molecule or every topical use of brimonidine.
• Patent-term analysis must account for patent-term adjustment, pediatric exclusivity, continuation patents, and later formulation claims.
• Brimonidine competition proceeds through the generic-drug ANDA pathway, not the biosimilar pathway.
• A Paragraph IV challenge, skinny label, formulation design-around, settlement, or post-expiration launch can materially change entry timing.
• The relevant competitive record includes the current Orange Book, FDA labeling, USPTO family data, and federal court litigation dockets.

FAQs

Does patent 7,439,241 cover brimonidine tartrate gel 0.33%?

Yes, the claimed method can cover use of a brimonidine tartrate gel at 0.33% if it is topically administered to rosacea-associated redness in an effective amount. The claim does not expressly require that concentration or gel format.

Can a generic sell brimonidine for glaucoma without infringing claim 1?

Possibly. Glaucoma treatment does not satisfy the rosacea-associated redness limitation. The infringement analysis would depend on the product’s labeling, marketing, actual use, and any separate patents covering the ophthalmic product.

Is claim 1 limited to facial rosacea?

The claim refers to redness associated with rosacea and application to the site of redness on the skin. It does not expressly say “facial,” although the FDA-approved commercial use is persistent facial erythema.

Can a new brimonidine cream avoid patent 7,439,241?

Changing the dosage form alone may not avoid claim 1. A cream could still infringe if it contains an effective amount of brimonidine and is topically applied to reduce rosacea-associated redness.

Does expiration of patent 7,439,241 guarantee immediate generic entry?

No. Later-expiring formulation or method patents, FDA exclusivity, litigation stays, settlements, regulatory deficiencies, and commercial manufacturing constraints can affect entry even after this patent expires.

References

1. Food and Drug Administration. (2013). Mirvaso (brimonidine tartrate) topical gel 0.33%: Prescribing information. U.S. Department of Health and Human Services.

2. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations, commonly known as the Orange Book. U.S. Department of Health and Human Services.

3. U.S. Code. (2024). 21 U.S.C. § 355: New drugs.

4. U.S. Code. (2024). 35 U.S.C. §§ 102, 103, 112: Conditions for patentability and patent application requirements.

5. U.S. Patent No. 7,439,241. (2008). Methods of treating rosacea. U.S. Patent and Trademark Office.

6. U.S. Patent and Trademark Office. (n.d.-a). Patent term adjustment and patent term information. U.S. Department of Commerce.

7. U.S. Patent and Trademark Office. (n.d.-b). Patent Center. U.S. Department of Commerce.

Drugs Protected by US Patent 7,439,241

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 7,439,241

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1631293		CR 2014 00031	Denmark
European Patent Office	1631293		C300683	Netherlands
European Patent Office	1631293		1490049-2	Sweden
European Patent Office	1631293		C20140022 00150	Estonia
European Patent Office	1631293		92462	Luxembourg