Details for Patent: 9,095,609

Which drugs does patent 9,095,609 protect, and when does it expire?

Patent 9,095,609 protects TRYPTYR and is included in one NDA.

This patent has ten patent family members in four countries.

Summary for Patent: 9,095,609

Title:	Ophthalmic composition comprising ws-12 and methods to treat xerophthalmia
Abstract:	The invention relates to therapeutic compositions for the treatment of dry eye, more specifically to compositions comprising a TRPM8 receptor agonist ligand. Furthermore, the invention relates to therapeutic compositions for the treatment of epiphora, more specifically to compositions comprising a TRPM8 receptor antagonist.
Inventor(s):	Carlos Belmonte Martnez, Juana Gallar Martinez, Antonio Ferrer Montiel, Asia Fernández Carvajal, Félix Viana De La Iglesia
Assignee:	Consejo Superior de Investigaciones Cientificas CSIC , Universidad Miguel Hernandez de Elche UMH
Application Number:	US13/821,840
Patent Claim Types: see list of patent claims	Use; Composition;

Scope, claims, and US patent landscape for Drug Patent US 9,095,609

US 9,095,609 is directed to ophthalmic compositions and treatment methods for xerophthalmia that use WS-12 (2-isopropyl-5-methyl-cyclohexanecarboxylic acid (4-methoxyphenyl)-amide) in a defined dose range, with additional limitations covering TRPM8 agonist potency, non-cytotoxicity, dose regimens, and optional combination therapy (other TRPM8 agonists and standard xerophthalmia drugs), plus formulation components such as lubricants and vehicles.

At the claim level, the patent reads like a “stack” of three layers: 1) core active and indication (WS-12 + xerophthalmia + “not cytotoxic”), 2) mechanistic/potency framing (TRPM8 agonism with specified efficacy ratios), 3) productization constraints (dose and administration frequency; optional add-ons for synergistic or enhanced effect).

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What is the claim architecture in US 9,095,609?

The independent claim set is functionally two pillars: an apparatus-free composition claim (claim 1) and a method-of-treatment claim (claim 17), each followed by dependent claims that narrow scope around dosing, mechanism, formulation, and combination therapy.

Independent claims

• Claim 1 (composition)
  An ophthalmic composition comprising a therapeutically effective amount of WS-12, where WS-12 treats or reduces likelihood of xerophthalmia, and the amount of WS-12 is not cytotoxic.

• Claim 17 (method)
  A method to treat or reduce likelihood of xerophthalmia by administering a therapeutically effective amount of a composition comprising WS-12 to an individual with xerophthalmia.

Dependent claim groupings and what they add

1) Mechanism/potency

• Claims 2 and 18: WS-12 is a TRPM8 agonist with efficacy at least 50x, 100x, 1000x, or 2000x more than other members of the TRPM cation channel subfamily M (framed as relative to “the other channel of other members of TRPM”).

2) Dose amount and dosing-by-body-weight

• Claims 3-6: dose per dose ranges 0.0005 mg to 0.1 mg; with specific “about 0.0005 mg” fallback.
• Claims 5-6 and 21-22: dose per body weight ranges 0.007 micrograms/kg to 0.01 mg/kg (and specific “about 0.007 micrograms/kg”).

3) Dosing frequency

• Claims 7-8 and 23-24: variable number of times per day; specifically 1 to 4 times a day.

4) Multi-agonist approach

• Claims 9-10: composition comprises an additional TRPM8 agonist selected from: WS-3, WS-5, WS-11, WS-14, WS-23, WS-30, WS-148, menthol, or combinations.

5) Standard-of-care xerophthalmia add-on

• Claims 11-12: further comprises a drug useful for xerophthalmia selected from: corticoid, vitamin A, pilocarpine, hypromellone, carbomer, cyclosporine, or combinations.

6) Formulation components

• Claims 13-14: composition comprises a lubricant, with examples including glycerol, HPMC, hypromellose variants (as hydroxymethyl cellulose), carboxymethyl cellulose, PEG, PVA, hyaluronic acid, castor oil, mineral oil, etc.
• Claim 15: composition comprises a pharmaceutically acceptable vehicle.

7) Target population limitation

• Claim 16: subject is an animal subject (not a typical human-only carve-in, but it keeps non-human administration within scope).

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What is the technical scope of protection under claim 1?

Claim 1’s baseline is broad on several dimensions, but it contains key gating limitations that define infringement and non-infringement boundaries.

Core gating limitations

• Therapeutic effective amount of WS-12
  The patent ties treatment effect to WS-12 presence, not to any particular excipient chemistry.

• Ophthalmic composition
  The composition is formulated for eye administration (no further device or dosage form constraints are stated in your claim text, but it implies standard ophthalmic formulation forms).

• Indication tie-in
  WS-12 treats or reduces likelihood of xerophthalmia.

• Non-cytotoxicity constraint

  • “wherein the amount of WS-12 is not cytotoxic.”
  • This is a claim limitation that can be outcome-determinative for a design-around. It also implies the patent relies on supporting data that WS-12 in the claimed amounts is not harmful to ocular cells.

Implicit product scope boundaries

• Claim 1 does not specify a dosage form, but downstream dependent claims narrow dose and dosing frequency.
• Claim 1 does not require a specific lubricant or vehicle, but dependent claims 13-15 add options and may matter for narrower claim coverage.
• Claim 1 does not require TRPM8 mechanism, but claims 2 and 18 do. That means:
  • A product using WS-12 for xerophthalmia without proving “TRPM8 agonist efficacy ratios” could still fall under claim 1 depending on how “not cytotoxic” and “therapeutically effective” are established.
  • A competing product that changes mechanism or shows different channel selectivity may still be exposed on claim 1, but safer positions arise if it can avoid the WS-12/xerophthalmia/non-cytotoxic composition constraints.

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How does the TRPM8 “efficacy ratio” language change scope?

Claims 2 and 18 inject a mechanistic constraint: WS-12 acts as a TRPM8 agonist with efficacy at least 50x, 100x, 1000x, or 2000x more than “the other channel of other members” of TRP subfamily M.

Practical effect

This language can be used in at least two ways in enforcement and defense:

• Enforcement leverage: it provides a measurable pharmacology hook to argue WS-12 is uniquely TRPM8 selective and achieves efficacy relative to other TRPM targets. This matters if an accused product argues it is not acting at TRPM8 or that it is non-selective.
• Defense leverage: if an accused product uses WS-12 but has a different pharmacology profile, it can attempt to narrow to claim 1 (composition) rather than claim 2/18 (mechanism). The claim text you provided makes claim 2/18 dependent, not independent, so the risk can be compartmentalized.

Drafting consequence

Because the efficacy thresholds are expressed as selectable tiers (at least 50x, 100x, 1000x, or 2000x), a factual record that shows efficacy is above any one of these tiers can support the limitation depending on how the court evaluates the construction. As drafted, the claim language is structured to accommodate multiple tiers.

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Where are the numerical “design-around” points: dose and body-weight ranges

The patent uses two dosing frameworks: 1) Dose per administration (mg per dose) 2) Dose per body weight (micrograms/kg to mg/kg)

Dose per dose (mg)

• Claim 3: 0.0005 mg to 0.1 mg
• Claim 4: about 0.0005 mg (single-point fallback)
• Claim 3-4 can capture both titration schedules and low-dose regimens if they land within the numeric window.

Dose per body weight

• Claim 5: 0.007 micrograms/kg to 0.01 mg/kg
• Claim 6: about 0.007 micrograms/kg

Key scope implication

A product outside these numeric windows can potentially avoid claims 3-6 and 19-22, but it may remain exposed under broader claim 1 and 17 if “therapeutically effective amount” is satisfied and non-cytotoxicity is met. Still, in practice, dosing is often the first place competitors look because numerical ranges give clear infringement boundaries.

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Administration frequency: 1 to 4 times/day and variable dosing

• Claim 7 / 23: variable number of times a day
• Claim 8 / 24: 1 to 4 times a day

This gives the patent a structured claim window. If an accused product is dosed more frequently than 4 times/day, claim 8/24 might be avoided, but claim 7/23 may still capture it because those are not limited to 1-4 (they allow variable frequency). Conversely, very infrequent regimens may avoid both if they do not qualify as “variable number of times a day” in claim construction, but most ocular dosing schedules will be treated as “times per day.”

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How do dependent claims expand the “combination” landscape?

Additional TRPM8 agonist (Claims 9-10)

• The patent permits inclusion of another TRPM8 agonist selected from:
  • WS-3, WS-5, WS-11, WS-14, WS-23, WS-30, WS-148, menthol
  • or combinations

This matters for competitive portfolios because many ocular therapeutics use menthol derivatives or cooling agents, but this claim is TRPM8-oriented and ties to xerophthalmia treatment in combination with WS-12.

Standard xerophthalmia drugs (Claims 11-12)

• Additional xerophthalmia drug selected from:
  • corticoid, vitamin A, pilocarpine, hypromellone, carbomer, cyclosporine
  • or combinations

This creates potential overlap with multiple classes in the dry eye/xerophthalmia ecosystem:

• anti-inflammatory (corticoid)
• secretagogue/salivatory pathway (pilocarpine)
• anti-inflammatory immunomodulator (cyclosporine)
• tear film / viscosity agents (hypromellone, carbomer)
• epithelial maintenance (vitamin A)

If a competitor’s WS-12 ocular product uses one or more of these agents, claims 11-12 may become relevant, even if the WS-12 dosing aligns and non-cytotoxicity is addressed.

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Formulation and vehicle scope: lubricants as dependent claim “hooks”

• Claim 13-14 (lubricants) lists common ophthalmic excipients:
  • glycerol, hypromellone, hydroxymethyl cellulose, carboxymethyl cellulose
  • PEG, PVA, hyaluronic acid
  • castor oil, mineral oil
  • plus combinations
• Claim 15 (vehicle) is broad: “pharmaceutically acceptable vehicle.”

This suggests the patent is not limited to a special chemical delivery system. For infringement, WS-12 content and xerophthalmia therapeutic use matter more than lubricant selection unless the competitor wants to reduce exposure to narrower dependent claims.

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Potential infringement pathways by claim type

A WS-12 ophthalmic product that treats xerophthalmia

• Strong exposure to claim 1 and claim 17 if it meets:
  • WS-12 is present at therapeutically effective (and non-cytotoxic) levels
  • formulation is ophthalmic
  • the product is used for xerophthalmia treatment or reduction of likelihood

A WS-12 product with TRPM8 selectivity claims or data

• Exposure increases to claim 2/18 if WS-12 is validated as TRPM8 agonist with the specified efficacy ratios.

A dosing-limited WS-12 regimen

• Exposure to dose-dependent claims 3-6 and 19-22 if dosing matches those numeric ranges.

A WS-12 regimen combined with other TRPM8 agonists

• Exposure to claims 9-10 if additional TRPM8 agonists are included (including menthol).

A WS-12 regimen combined with standard dry eye/xerophthalmia drugs

• Exposure to claims 11-12 if the combination includes any listed class members.

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US patent landscape: what matters around US 9,095,609

Because US 9,095,609 is an ophthalmic-use and composition patent anchored on WS-12, the relevant landscape for R&D planning typically clusters into four zones of risk and opportunity:

1) WS-12 composition and dosing follow-on patents

• Competitors often attempt to file around by:
  • changing dose form
  • using different dose ranges
  • using different co-actives
• The presence of broad claim 1/17 plus dependent dosing and combination claims means follow-ons may still face partial overlap.

2) TRPM8 agonist family patents

• The claims explicitly name WS series (WS-3, WS-5, WS-11, etc.) and menthol as additional TRPM8 agonists.
• This narrows freedom for competitors who also want TRPM8 “cooling” agonists to accompany WS-12.

3) Xerophthalmia/dry eye combination therapy patents

• Cyclosporine, corticoids, pilocarpine, hypromellone, carbomer, and vitamin A are standard.
• The patent’s combination claims suggest it targets regimens that mix WS-12 with those standard therapies.
• Even if competitors have separate patents for dry eye combinations, overlap depends on whether WS-12 is involved.

4) Formulation and vehicle patents

• The lubricant list is conventional; the patent is likely not overly dependent on novel formulation.
• That raises the chance that competitors can still formulate WS-12 into conventional vehicles, but their legal freedom depends on whether those formulations land within the numeric and non-cytotoxic limitations.

Bottom line for landscape mapping: if a competitor’s pipeline uses WS-12 specifically for xerophthalmia, the exposure is high against the “core” claims (1 and 17) regardless of lubricant and vehicle choices. Freedom mainly comes from:

• avoiding WS-12 entirely,
• using WS-12 but failing “not cytotoxic” or “therapeutically effective” in the claimed use context,
• moving dosing outside the dependent numeric ranges while accepting that claim 1/17 may still capture therapeutically effective use.

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Key Takeaways

• US 9,095,609 protects WS-12 ophthalmic compositions and xerophthalmia treatment methods with a core constraint of non-cytotoxic WS-12 at a therapeutically effective amount (claims 1 and 17).
• The patent expands scope with TRPM8 agonist efficacy ratios (claims 2 and 18) and multiple dosing windows (claims 3-6 and 19-22) plus dose frequency limits (claims 7-8 and 23-24).
• Dependent claims add legal risk if WS-12 is paired with other TRPM8 agonists (claims 9-10, including menthol and WS compounds) or with standard xerophthalmia drugs (claims 11-12, including corticoid, vitamin A, pilocarpine, hypromellone, carbomer, cyclosporine).
• Formulation breadth is strong: common lubricants and vehicles are contemplated (claims 13-15), so competitive differentiation based solely on excipients is unlikely to avoid exposure.

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FAQs

1) What is the scope of protection’s “center of gravity” in US 9,095,609?

Claim 1 (composition) and claim 17 (method) because they cover ophthalmic WS-12 for xerophthalmia with a “not cytotoxic” limitation, and do not require a specific lubricant or combination co-therapy.

2) Does the patent require TRPM8 selectivity to be infringed?

Not for the core claims 1 and 17. TRPM8 selectivity thresholds appear in dependent claims 2 and 18.

3) Can a different lubricant avoid infringement?

Changing lubricants may avoid dependent claims 13-14, but it does not generally avoid claim 1/17 because claim 1 does not require a particular lubricant or vehicle.

4) What combinations are explicitly inside the claim set?

Additional TRPM8 agonists listed in claims 9-10 (including menthol), and xerophthalmia drugs listed in claims 11-12 (including corticoid, vitamin A, pilocarpine, hypromellone, carbomer, cyclosporine).

5) Where are the most obvious numerical design-around points?

The dependent dosing windows in claims 3-6 and 19-22 and the frequency limitation in claims 8 and 24.

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References

[1] Claims text provided by user for US 9,095,609 (WS-12 ophthalmic composition and xerophthalmia treatment).

Drugs Protected by US Patent 9,095,609

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Alcon Labs Inc	TRYPTYR	acoltremon	SOLUTION/DROPS;OPHTHALMIC	217370-001	May 28, 2025		RX	Yes	Yes			Y			TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)

International Family Members for US Patent 9,095,609

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2614860
European Patent Office	4268814
Spain	2377785