Details for Patent: 7,026,337

Summary for Patent: 7,026,337

Title:	Antimycotic gel having high active compound release
Abstract:	A pharmaceutical preparation comprising a hydrophilic gel-forming agent, water and a compound of the formula I is suitable for the treatment and prophylaxis of dermatomycoses.
Inventor(s):	Manfred Bohn, Karl Theodor Kraemer, Astrid Markus
Assignee:	Medicis Pharmaceutical Corp
Application Number:	US10/690,597
Patent Claim Types: see list of patent claims	Use; Composition;

Scope and Patent Landscape for US Drug Patent 7,026,337 (Dermatomycoses/Fungal Foot Gel Methods)
US Patent 7,026,337 centers on dermatophyte and related dermatomycoses treatment or prophylaxis using a topical gel with a limited “consisting essentially of” active: a pyridone compound of formula (I) (or physiologically tolerable salts), formulated with hydrophilic gel-forming agents plus spreading agents, and expressly requiring the composition is substantially free of additional active components. The claim set is method-focused (treatment/prophylaxis) and tightly productizes the formulation: the active identity is narrowed further in dependent claims to specific substituted pyridones.

---

What does US 7,026,337 claim for dermatomycoses gel treatment in the US?

Claim 1: What is the core protected invention?

Featured snippet answer: Claim 1 protects a method of treating or prophylaxis of dermatomycoses by administering a topical hydrophilic gel containing (i) hydrophilic gel-forming agent(s), (ii) spreading agent(s), and (iii) an active component that “consists essentially of” at least one compound of formula (I) (or physiologically tolerable salts), with R1-R3 = H or C1-C4 alkyl and R4 = saturated C6-C9 hydrocarbon radical, and the gel is substantially free of additional active components.

Structured parsing of Claim 1 limitations

1. Indication / use

   • “Method of treatment or prophylaxis of dermatomycoses”
   • Scope includes both therapeutic and preventive administration.

2. Dosage form / administration medium

   • “Composition is a gel composition”
   • Implies topical gel administration (not oral, not lotion/cream unless a cream gels qualifies, but claim requires “gel composition”).

3. Formulation system

   • at least one hydrophilic gel-forming agent
   • at least one spreading agent
   • These two excipients are mandatory categories.

4. Active component limitation

   • Active component “consists essentially of” at least one compound chosen from:
     • compound of formula (I)
     • and physiologically tolerable salts
   • “Consists essentially of” is a major narrowing phrase:
     • It permits minor components not materially affecting basic and novel characteristics.
     • It blocks adding other antifungal actives as “additional active components.”
     • It still allows formulation excipients.

5. “Substantially free of any additional active components”

   • This is an express negative limitation.
   • It is aimed at combination antifungal strategies (including pairing with additional actives) that could otherwise fall under “consisting essentially of.”

6. Chemical structure boundaries

   • R1, R2, R3: each is hydrogen or a C1-C4 alkyl
   • R4: saturated hydrocarbon radical with C6-C9
   • The claim therefore captures a family of pyridone derivatives within that substitution pattern.

Claim 2–3: How do dependent claims narrow the active?

Both dependent claims preserve the Claim 1 formulation architecture and negative active restriction, while narrowing the active identity to specific pyridones.

• Claim 2 (specific active family member)

  • Active consists essentially of:
    • 1-hydroxy-4-methyl-6-cyclohexyl-2(1H)pyridone
    • one or more physiologically tolerable salts
    • or mixtures

• Claim 3 (alternative specific active family member)

  • Active consists essentially of:
    • 1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)-2(1H)pyridone
    • one or more salts
    • or mixtures

Practical effect: Claim 2 and Claim 3 convert the formula-(I) genus into two specific embodiments with tighter infringement hooks for products using those exact substitution patterns.

Claims 4–5: What changes for fungus of the foot (athlete’s foot)?

• Claim 4 protects a method for “fungus of the foot” using a gel with hydrophilic gel-former(s), spreading agent(s), and active consisting essentially of 1-hydroxy-4-methyl-6-cyclohexyl-2(1H)pyridone, with the same “substantially free” limitation.

• Claim 5 protects the same but with active consisting essentially of 1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)-2(1H)pyridone.

Important scope difference between dermatomycoses vs fungus of the foot:
Dermatomycoses is broader (skin fungal infections generally). Fungus of the foot is narrower (tinea pedis). The patent includes both categories, creating two use-tailored claim paths.

---

What is the claim “consists essentially of” impact for infringement and design-around?

How “consisting essentially of” constrains active inclusion

“Consists essentially of” typically means:

• The active component is limited to the recited compound(s) and permitted salts.
• Other actives cannot be present if they would materially change the basic and novel characteristics.
• It is paired here with “substantially free of any additional active components,” strengthening exclusion.

Design-around pressure points

• Adding another antifungal active (even if the pyridone remains) risks falling outside the “substantially free” and/or outside “consists essentially of.”
• Switching from a gel to another topical form could avoid “gel composition” if not a true gel.
• Changing excipient categories (e.g., eliminating a hydrophilic gel-forming agent or a spreading agent as claimed) also risks non-infringement.

“Substantially free” is a practical litigation hinge

“Substantially free” is a flexible threshold. In disputes, expert evidence often focuses on:

• actual formulation composition,
• whether added active(s) are present in meaningful amounts,
• and whether they would materially affect performance.

For a competitor, the high-risk zone is intentional combination antifungal products.

---

What patents likely cover the same pyridone antifungal family as US 7,026,337?

US 7,026,337 is a formulation-plus-method patent built around a distinct chemical series: substituted 1-hydroxy-4-methyl-2(1H)pyridones with bulky hydrophobic group at the 6-position (cyclohexyl or branched aliphatic). The landscape typically splits into three overlapping blocks:

1. Core chemistry patents (compound claims to the pyridone series, salts, and possibly process claims)
2. Formulation patents (gels, creams, vehicles, polymer systems, spreading agents, tolerability)
3. Use patents (methods for dermatomycoses, tinea pedis, prophylaxis vs treatment, dosing regimes)

Given US 7,026,337’s structure, it functions primarily as a use/formulation enforcement patent rather than the broadest chemistry coverage.

Landscape inference by claim architecture

• If US 7,026,337 issues as a US patent, earlier or parallel applications usually exist for:
  • the same pyridone compounds of formula (I)
  • preparation of those compounds and salts
  • antifungal use concepts
• The “consists essentially of” and negative active restriction often appear when the patentee expects competition from combination products and wants to keep exclusivity for single-active antifungal delivery in gel form.

---

Which product formats are most vulnerable under US 7,026,337’s gel-method claims?

High infringement likelihood

Products that match most of the following:

• Topical gel format
• Uses a hydrophilic gel-forming agent system
• Contains a spreading agent
• Uses one of the protected actives (formula (I) series), especially:
  • 1-hydroxy-4-methyl-6-cyclohexyl-2(1H)pyridone
  • or 1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)-2(1H)pyridone
• Contains little or no other antifungal actives
• Targets dermatomycoses and/or tinea pedis

Lower infringement likelihood (common workarounds)

• Creams/ointments/lotions that are not properly categorized as “gel composition”
• Formulations that materially include additional active antifungal agents (combination therapy)
• Substitution outside R1-R3 (not H or C1-C4 alkyl) or R4 not C6-C9 saturated hydrocarbon

---

When does US 7,026,337 expire for US exclusivity timing and generic risk?

No expiry date, patent term adjustment (PTA), or filing chronology is provided in the prompt. Without those, a complete and accurate exclusivity timeline cannot be produced.

---

What is the Orange Book status for US 7,026,337 and what does it mean for generic entry?

No FDA NDA/ANDA/BLA identifiers, listed drug, or Orange Book listing status is provided in the prompt. Without that mapping, a correct Orange Book status statement cannot be produced.

---

What Paragraph IV risks exist for US 7,026,337?

US 7,026,337 is a method-of-treatment claim tied to a topical gel. Paragraph IV certification typically applies to an ANDA referencing an NDA drug product with listed patents. However, the prompt does not provide:

• the drug product,
• the Orange Book listing,
• or the patent listing linkage.

A complete and accurate Paragraph IV risk assessment cannot be produced from the provided information alone.

---

How strong is the patent estate coverage of this pyridone antifungal gel approach?

Strength drivers

• Narrow “active consists essentially of” ties enforceability to specific chemistry and single-active delivery strategy.
• Formulation specificity (hydrophilic gel-forming agent + spreading agent) reduces the number of non-infringing gel products.
• Negative limitation (“substantially free of any additional active components”) blocks combination antifungals.

Main vulnerability points

• If the accused product’s vehicle is not a “gel composition” under claim construction, infringement weakens.
• If the accused active is outside the formula (I) boundaries (R4 C6-C9 saturated hydrocarbon, and R1-R3 H or C1-C4 alkyl), infringement weakens.
• If the accused formulation intentionally includes other active antifungal agents at levels that are not “substantially free,” infringement weakens.

---

Litigation and settlement landscape: what patent disputes affect US 7,026,337?

No litigation docket numbers, enforcement parties, or settlements are provided in the prompt. A correct litigation status cannot be produced.

---

Regional scope: does US 7,026,337 cover outside the US?

US patents are territorially limited to the United States unless there are related foreign filings (not provided). No foreign family data is provided, so a multi-jurisdiction landscape cannot be completed.

---

Key takeaways

• US 7,026,337 claims topical gel methods for dermatomycoses and fungus of the foot, requiring a formulation with hydrophilic gel-forming agent(s) and spreading agent(s).
• The protected active is limited by “consists essentially of” to formula (I) pyridones (or physiologically tolerable salts) with defined substitution constraints (R1-R3 = H or C1-C4 alkyl; R4 = saturated C6-C9 hydrocarbon).
• Dependent claims narrow enforcement further to two specific pyridones:
  • 1-hydroxy-4-methyl-6-cyclohexyl-2(1H)pyridone
  • 1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)-2(1H)pyridone
• The gel must be substantially free of additional active components, making combination antifungal gel strategies the primary design-around risk zone.

---

FAQs

1) Does US 7,026,337 require prophylaxis or only treatment?

Both. The claims cover “treatment or prophylaxis” for dermatomycoses (and separately for fungus of the foot).

2) What excipients are mandatory under the claims?

At least one hydrophilic gel-forming agent and at least one spreading agent.

3) Can a product include another antifungal alongside the protected pyridone?

The composition must be “substantially free of any additional active components,” and the active component “consists essentially of” the formula (I) compound(s) and salts, which collectively restrict adding additional actives.

4) Are athlete’s foot claims broader or narrower than dermatomycoses claims?

Narrower. “Fungus of the foot” is a subset of dermatomycoses.

5) What structural features of the active are essential?

R1-R3 must be H or C1-C4 alkyl, and R4 must be a saturated hydrocarbon radical with 6 to 9 carbons.

---

References (APA)

1. United States Patent 7,026,337. (n.d.). Method of treatment or prophylaxis of dermatomycoses comprising administering a gel composition containing specified pyridone compounds.

Drugs Protected by US Patent 7,026,337

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

Foreign Priority and PCT Information for Patent: 7,026,337

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Germany	196 39 816	Sep 27, 1996

International Family Members for US Patent 7,026,337

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	008858
Austria	216882
Australia	4703797
Australia	718837
Bulgaria	103262
Bulgaria	63864