Details for Patent: 6,245,819

Summary for Patent: 6,245,819

Title:	Method for the treatment of vaginal dryness and sexual dysfunction in women during or after the menopause
Abstract:	This invention concerns a method for the treatment of vaginal dryness or sexual dysfunction in women during or after the menopause, said method comprising administering to the woman an effective amount of the compound (deaminohydroxy)toremifene or a pharmaceutically acceptable salt or ester thereof, or a metabolite thereof.
Inventor(s):	Kaija Halonen, Lauri Kangas, Michael W. DeGregorio
Assignee:	QuatRx Pharmaceuticals Co
Application Number:	US09/625,199
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,245,819
Patent Claim Types: see list of patent claims	Use; Delivery;

United States Patent 6,245,819 Scope, Claim Analysis, and Patent Landscape for (Deaminohydroxy)toremifene in Vaginal Dryness and Menopause-Related Sexual Dysfunction

Executive summary: US 6,245,819 claims a method-of-treatment for vaginal dryness and/or sexual dysfunction in women during or after menopause using (deaminohydroxy)toremifene (or pharmaceutically acceptable salt/ester/metabolite). The independent claim is limited by (i) a defined patient population (women during/after menopause), (ii) a defined condition (vaginal dryness or sexual dysfunction), and (iii) administration of the active compound. Dependent claims narrow with dose ranges (25–100 mg; 30–90 mg) and administration routes (oral or transdermal). The patent’s practical enforceability hinges on whether accused products prescribe or otherwise induce use that falls within these elements, including dose and route.

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What is US Patent 6,245,819 and what does it claim?

Direct answer: US 6,245,819 is a US method-of-treatment patent for menopausal women with vaginal dryness and/or sexual dysfunction, using (deaminohydroxy)toremifene (including pharmaceutically acceptable salts, esters, and metabolites) administered at specified oral/transdermal dose ranges.

Core claim structure

• Claim 1 (independent):
  A method for treating vaginal dryness or sexual dysfunction in women during or after menopause, comprising administering an effective amount of (deaminohydroxy)toremifene (or salt/ester/metabolite).
• Claims 2–3 (dose narrowing):
  • Claim 2: daily dose 25 to 100 mg
  • Claim 3: daily dose 30 to 90 mg
• Claims 4–6 (route narrowing):
  • Claim 4: administered orally or transdermally
  • Claim 5: 25 to 100 mg with oral/transdermal
  • Claim 6: 30 to 90 mg with oral/transdermal

Claim 1: scoping implications

Claim 1 is broad in that it is not restricted to:

• a specific formulation type (other than salt/ester/metabolite),
• a specific schedule beyond “effective amount,”
• a specific severity grading,
• a specific endpoint measurement.

Its key limiting features are the patient subgroup and indication:

• “women during or after the menopause”
• “vaginal dryness or sexual dysfunction”

From an infringement standpoint, those limitations matter for induced infringement and for claim construction. If an accused use targets non-menopausal populations, other indications, or uses not directed to vaginal dryness/sexual dysfunction, the claim elements are not met.

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How broad is claim 1 for (deaminohydroxy)toremifene treatment of vaginal dryness and sexual dysfunction?

Direct answer: Claim 1 is indication-anchored and population-anchored while being compound-anchored and otherwise flexible on formulation and regimen details.

Meaning of “administering to the woman an effective amount”

• “Effective amount” is typically construed as a therapeutically effective dose to treat the stated condition. This can leave room for argument based on clinical endpoints.
• Claim 1 does not define an exact mg/day, so it can capture a wide dosing spectrum unless constrained by specification or prosecution history.

“vaginal dryness or sexual dysfunction” breadth

This phrase can be read as:

• two alternative therapeutic targets (“vaginal dryness” OR “sexual dysfunction”), either of which qualifies, and/or
• overlapping symptom complexes that together satisfy “sexual dysfunction.”

That breadth increases the risk that clinical messaging or labeling that ties the compound to either symptom cluster could be argued to fall within Claim 1.

“during or after menopause”

This is also a meaningful limiter:

• It can include peri-menopause (“during”) and post-menopause (“after”).
• It likely excludes pre-menopausal populations unless a court interprets “during” broadly enough to capture early transition states.

“(deaminohydroxy)toremifene or … salt/ester … metabolite thereof”

This expands scope beyond the parent compound to:

• salt and ester forms,
• metabolites.

From a landscape perspective, this affects both:

• design-around (form of drug may still be captured), and
• metabolite argumentation (systemic metabolites that are present at therapeutic exposure could be alleged to qualify as “metabolite thereof,” depending on claim construction).

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What do the dose claims (25–100 mg and 30–90 mg) cover and how do they constrain infringement?

Direct answer: Claims 2 and 3 restrict treatment to daily dosing windows that are commonly actionable in prescribing, labeling, and “use instructions” for oral or transdermal products.

Dose constraint details

• Claim 2: 25 to 100 mg daily dose
• Claim 3: 30 to 90 mg daily dose

Practical enforceability

• If an accused product is marketed with dosing instructions wholly outside those ranges, infringement of Claims 2 and 3 is less likely.
• If dosing instructions fall within the ranges, infringement risk increases.
• If labeling allows dose titration that overlaps the claimed window, the risk persists unless the practical induced-use avoids the specific range.

Intersection with route claims

Claims 5 and 6 lock together dose and route:

• Claim 5: 25–100 mg, oral or transdermal
• Claim 6: 30–90 mg, oral or transdermal

So an accused regimen outside the claimed route could avoid the narrower claims, while still potentially implicating Claim 1 depending on whether oral or transdermal use is within the alleged act of infringement.

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How do the oral or transdermal route limitations affect the patent’s scope?

Direct answer: The dependent route language confines Claims 4–6 to oral or transdermal administration.

Key implication

• If an accused product delivers the active compound via a route other than oral or transdermal (eg, intravaginal), the dependent claims likely do not read on that route.
• Claim 1 itself does not specify a route, so route arguments may reduce dependent-claim risk but may not eliminate risk under Claim 1 if the court finds administration was “administering” within the meaning of Claim 1 and the accused conduct includes oral/transdermal use.

Given the text you provided, Claim 1 is not limited to route. That keeps Claim 1 broader than the dependent claims.

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What patent estate does US 6,245,819 sit in, and how to map likely related protection areas?

Direct answer: Based on the claim theme, the landscape for this patent family typically clusters around:

1. use claims for menopausal vaginal dryness/sexual dysfunction,
2. dose and route dependent variations, and
3. compound-related claims covering (deaminohydroxy)toremifene, salts/esters, and potentially metabolites.

Expected adjacent claim categories in related filings

Even without a family list here, these are the usual “nearby” protection zones that track with a use claim of this type:

1. Compound claims

   • Direct coverage of (deaminohydroxy)toremifene chemical entity
   • Salt/ester forms
   • Possibly polymorphs or solvates (if disclosed)

2. Method-of-use claims

   • Menopausal vaginal dryness
   • Sexual dysfunction endpoints
   • Variants by population subgroup (peri- vs post-menopause)
   • Variants by clinical stage or severity

3. Route/formulation dependent claims

   • Oral and transdermal dosage forms
   • Dose windows
   • Alternative scheduling (daily dosing vs titration) if separately claimed

4. Metabolite-related coverage

   • Claims that explicitly include metabolites often sit alongside definitions in the specification.

How to think about claim coverage for a competitor

A competitor trying to avoid this patent would typically consider:

• different indication (not vaginal dryness or sexual dysfunction),
• different patient population (not during/after menopause),
• different active agent (not (deaminohydroxy)toremifene or its salts/esters/metabolites),
• different dose range (outside 25–100 mg and/or 30–90 mg),
• different route (not oral/transdermal).

But because Claim 1 is not limited to route or a particular dose window, the most robust design-around is usually through active choice and indication rather than dosing or route.

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What other US patents are likely to be “blocking” around this use claim?

Direct answer: For a use-based patent tied to a specific active and indication, blocking patents in the broader landscape typically include:

• an earlier compound patent on the same active and derivatives, and/or
• later formulation patents (oral or transdermal dosage forms) and
• continuation/divisional patents with refined patient subpopulations, dosing schedules, or endpoints.

Landscape mapping framework

When analyzing enforcement and entry risk, treat US 6,245,819 as one layer in a stack:

• Layer 1: active compound entity claims (if present)
• Layer 2: salts/esters or prodrug-like variants
• Layer 3: method-of-use claims like this one (indication anchored)
• Layer 4: formulation/delivery claims (dose release characteristics, patches, oral matrices)
• Layer 5: regulatory/labeling induced-use exposure

If only the method-of-use claim exists and the compound entity is unprotected, a competitor can sometimes seek non-infringing use or pursue labeling carve-outs. If the compound entity remains protected, the competitor’s freedom to operate depends on both chemical and use coverage.

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What “claim construction” issues are likely to matter for infringement of US 6,245,819?

Direct answer: The highest-impact construction issues are:

• the scope of “vaginal dryness or sexual dysfunction,”
• the meaning of “during or after menopause,”
• the scope of “(deaminohydroxy)toremifene … metabolite thereof,” and
• whether an accused regimen is “administering… an effective amount” within the therapeutic intent.

Indication scope

• If an accused label or promotional materials support treatment of “genitourinary syndrome” or “dyspareunia” without linking to “vaginal dryness or sexual dysfunction,” the defense may argue non-literal correspondence. Courts may still evaluate whether the therapeutic claims effectively cover the same symptoms, but claim element matching is central.

Metabolite scope

“Metabolite thereof” can be construed narrowly (specific metabolite structures) or broadly (any systemic metabolic product). The breadth affects design-around and whether a prodrug/metabolic route could still land within the claim language.

Effective amount

If an accused regimen uses doses that overlap partially, litigation often becomes a factual dispute about therapeutic effect and intended use.

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How strong is the enforceability of US 6,245,819 based on the claim set you provided?

Direct answer: The claim set is enforceable against therapeutic use that:

• matches the menopausal indication (vaginal dryness or sexual dysfunction),
• uses (deaminohydroxy)toremifene (or salts/esters/metabolites),
• and, for the narrower claims, matches dosing and route (oral/transdermal).

Its enforceability is likely strongest when the accused product’s labeling includes:

• a menopausal indication consistent with “during or after menopause,” and
• prescribed or recommended dosing within 25–100 mg/day or 30–90 mg/day, and
• administration instructions that are oral or transdermal.

If labeling avoids those exact elements, enforceability shifts toward a doctrine-of-equivalents or induced-use theory rather than straightforward literal infringement.

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What generic entry risks exist if a product is accused to practice the claimed method?

Direct answer: The key entry risk is not “generic chemical identity” alone; it is whether the generic’s label and prescribing practice induce the claimed menopausal use with the same active and within the claimed dosing and route parameters.

Risk scenarios by claim layer

• Claim 1 risk (highest breadth):
  Any oral/transdermal or other route practice that targets menopausal vaginal dryness/sexual dysfunction using (deaminohydroxy)toremifene (or salt/ester/metabolite) and “effective amount.”
• Claim 2–3 risk (dose-triggered):
  Generic dosing in the 25–100 mg/day or 30–90 mg/day ranges elevates exposure.
• Claim 4–6 risk (route-triggered):
  Oral or transdermal instructions elevate exposure; other routes reduce dependent-claim risk.

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Key takeaways

• US 6,245,819 is an indication-anchored method patent for menopause-related vaginal dryness and sexual dysfunction using (deaminohydroxy)toremifene (and salts/esters/metabolites).
• Claim 1 is broad on regimen details and does not specify route or mg/day limits, making it the principal enforcement hook.
• Dependent claims narrow by daily dose (25–100 mg; 30–90 mg) and route (oral or transdermal), which are the main design-around levers but only meaningfully shield against the narrower claims.
• From a freedom-to-operate standpoint, the strongest entry barriers usually come from the stack of protections around the active compound and use/labeling alignment, not only from the method claim alone.

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FAQs

1. Does US 6,245,819 cover intravaginal delivery if it treats vaginal dryness in menopausal women?
2. What dosing facts matter most for avoiding infringement of the 25–100 mg and 30–90 mg claims?
3. Can a salt or ester form of (deaminohydroxy)toremifene fall within the claim even if the parent compound is not administered?
4. How does “metabolite thereof” change exposure for prodrugs or reformulated analogs?
5. What labeling language would most directly create induced-use risk for generic entry?

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References

1. United States Patent and Trademark Office. (n.d.). US 6,245,819. USPTO Patent Full-Text and Image Database.

Drugs Protected by US Patent 6,245,819

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 6,245,819

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	300289
Australia	2001258449
Australia	5844901