Details for Patent: 10,322,085

Summary for Patent: 10,322,085

Title:	Dicarboxylic acid foamable vehicle and pharmaceutical compositions thereof
Abstract:	The present invention teaches a foamable pharmaceutical carrier comprising a benefit agent, selected from the group consisting of a dicarboxylic acid and a dicarboxylic acid ester; a stabilizer selected from the group consisting of at least one surface-active agent; at least one polymeric agent and mixtures thereof; a solvent selected from the group consisting of water, a hydrophilic solvent, a hydrophobic solvent, a potent solvent, a polar solvent, a silicone, an emollient, and mixtures thereof, wherein the benefit agent, stabilizer and solvent are selected to provide a composition that is substantially resistant to aging and to phase separation and or can substantially stabilize other active ingredients. The invention further relates to a foamable composition further containing a liquefied hydrocarbon gas propellant.
Inventor(s):	Dov Tamarkin, Doron Friedman, Tal Berman, Enbal Ziv, David Schuz
Assignee:	Vyne Therapeutics Inc
Application Number:	US16/189,767
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,322,085
Patent Claim Types: see list of patent claims	Composition; Compound;

US Patent 10,322,085 (Foamable Azelaic-Acid Compositions): Claim Scope, Invalidity/Design-Around Surface-Area, and US Patent Landscape

US Patent 10,322,085 claims a tightly specified foamable topical composition for azelaic acid delivery using a specific carrier architecture (azelaic acid plus defined solvent and surfactant/HLC spacing), a defined polymeric agent + surfactant total, and a gas propellant level. The claim set is structured to preserve enforceability around (i) the HLB “spacing” requirement between surfactants, (ii) particular solvent identities (caprylic/capric triglyceride; dimethyl isosorbide ± propylene glycol), (iii) surfactant identity examples (glyceryl stearate; PEG-40 stearate; Polysorbate 80), (iv) polymer identity examples (xanthan gum; methylcellulose), and (v) foam adjuvant/long-chain fatty alcohol or fatty acid definitions, while allowing broad “further comprises” recitations for optional excipients.

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What is US Patent 10,322,085 claiming and what is the practical scope of claim 1?

Featured snippet answer: Claim 1 is limited to a foamable composition containing azelaic acid (about 15% wt in the carrier), hydrophobic solvent (2% to 50% wt in carrier), a polar solvent, a surface-active system with at least two surfactants whose HLB values differ by ≥ about 4 units, and polymeric + surfactant in total of 0.05% to 10% wt of carrier, plus a liquefied/compressed gas propellant at 3% to 25% wt of the whole composition and additional constraints on pH and shelf-life via dependent claims.

Claim 1 core limitations (all must be met)

Claim 1 requires all of the following simultaneously:

1. Foamable composition
   • Composition is foamable and includes a liquefied or compressed gas propellant.
2. Propellant content (composition-level)
   • Propellant present at about 3% to about 25% by weight of the composition.
3. Carrier architecture (carrier-level)
   • Carrier comprises, by weight of the carrier:
     • (a) Azelaic acid: about 15%.
     • (b) Hydrophobic solvent: about 2% to about 50%.
     • (c) Polar solvent: required but not quantitatively specified in claim 1.
     • (d) Surface-active agent: required.
     • (e) Polymeric agent: required.
     • (f) Water: required.
4. Surfactant “HLB differential” rule
   • Surface-active system comprises at least two surface-active agents.
   • There is a difference of about 4 or more units between the HLB values of the at least two surface-active agents.
5. Combined polymeric agent + surfactant content
   • Combined amount of polymeric agent and surface-active agent is about 0.05% to about 10% by weight of the carrier.

Claim 1 “escape valves” (breadth inside the box)

Even with tight requirements, claim 1 leaves room for formulation freedom:

• Polar solvent is only required, not limited in claim 1 identity or amount.
• Hydrophobic solvent is any hydrophobic solvent within 2% to 50% wt of the carrier; dependent claims narrow with identity examples.
• Polymeric agent identity is open in claim 1.
• Optional excipients are swept in by dependent claim 20 (“further comprises” list), which can support broader infringement while still requiring the claim 1 carrier/surfactant architecture.

Claim 1 practical infringement reading

For US infringement analysis, a product must be shown to satisfy:

• Quantitative hits: azelaic acid at ~15 wt% of the carrier, polymer+surfactant total between 0.05% and 10 wt% of carrier, and propellant at 3–25 wt% of the composition.
• HLB differential: at least two surfactants whose stated/named HLB values differ by ≥4 units.
• Component presence: hydrophobic solvent, polar solvent, water, polymeric agent, and gas propellant.

The HLB differential requirement is the most structurally distinguishing element because it ties infringement to the surfactant selection rather than only to compositional ranges.

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How do dependent claims 2–22 narrow scope and what are the enforceable “clusters”?

1) Hydrophobic solvent identity cluster (Claims 2–3)

• Claim 2: hydrophobic solvent comprises caprylic/capric triglyceride.
• Claim 3: caprylic/capric triglyceride present at about 11% by weight of the carrier.

Impact: These claims narrow claim 1 to a specific lipid/emollient and a specific concentration point. They are strong anchors if the accused product uses caprylic/capric triglyceride around that range.

2) Polar solvent identity cluster (Claims 4–6)

• Claim 4: polar solvent comprises dimethyl isosorbide.
• Claim 5: dimethyl isosorbide at about 5% by weight of the carrier.
• Claim 6: polar solvent further comprises propylene glycol.

Impact: If the accused product uses dimethyl isosorbide and matches the concentration, these claims create a high-probability mapping path.

3) Surfactant composition clusters with HLB positioning (Claims 7–11)

These are critical because they operationalize the HLB differential rule through identity and non-ionic/ionic status.

• Claim 7: includes at least one non-ionic surface-active agent with HLB < 9.
• Claim 8: non-ionic HLB < 9 comprises glyceryl stearate.
• Claim 9: includes at least one non-ionic surface-active agent with HLB > 9.
• Claim 10: HLB > 9 comprises PEG-40 stearate and/or Polysorbate 80.
• Claim 11: includes at least one ionic surface-active agent.

Impact:

• Claims 7–10 together imply a common pair: a low-HLB nonionic (glyceryl stearate) with a high-HLB nonionic (PEG-40 stearate or Polysorbate 80). If both are present, the HLB differential condition in claim 1 is typically satisfied, making these dependent claims practical for enforcement.
• Claim 11 expands surfactant architecture to include an ionic surfactant, which may be useful for companies formulating with ionic cleansing components, but it still must satisfy claim 1’s “at least two surfactants with ≥4 HLB units difference” requirement.

4) Polymeric agent cluster (Claims 12–15)

• Claim 12: polymeric agent at 0.01% to 5% wt of carrier.
• Claim 13: polymeric agent is naturally occurring and/or semi-synthetic.
• Claim 14: naturally-occurring polymeric agent comprises xanthan gum.
• Claim 15: semi-synthetic polymeric agent comprises methylcellulose.

Impact: These claims help establish infringement for gel/thickened foam systems that use xanthan or methylcellulose. Claim 12’s concentration range is an additional quantitative screen.

5) Foam adjuvant cluster (Claims 16–18)

• Claim 16: composition further comprises a foam adjuvant.
• Claim 17: foam adjuvant is a fatty alcohol with ≥15 carbons and/or fatty acid with ≥16 carbons.
• Claim 18: fatty alcohol comprises cetostearyl alcohol.

Impact: Foam adjuvants (C15+ alcohols/C16+ acids) are a known foam-stabilization approach. Claim 18 provides an identity target for cetostearyl alcohol formulations.

6) Short-chain alcohol limitation (Claim 19)

• Claim 19: composition comprises < about 5% wt of carrier of a short-chain alcohol.

Impact: This is a negative limitation. It can matter if a competitor introduces ethanol/low-MW alcohols to alter solubility or skin feel. To avoid infringement, a formulation may try to keep short-chain alcohol below 5% of the carrier.

7) Optional excipient umbrella (Claim 20)

• Claim 20 lists a broad “further comprises” set including antiperspirant, anti-static agent, buffer, bulking agent, chelating agent, cleanser, colorant, conditioner/deodorant, diluent, dye, emollient, fragrance, humectant, pearlescent acid, perfuming agent, permeation enhancer, pH-adjusting agent, preservative, protectant, skin penetrating enhancer, softener, solubilizer, sunscreen, sun blocking agent, sunless tanning agent, viscosity modifier, vitamin.

Impact: This supports infringement even for “enhanced” end products with multiple functional additives, as long as claim 1 core elements remain satisfied.

8) pH and shelf-life (Claims 21–22)

• Claim 21: pH between 4.0 and 6.0.
• Claim 22: shelf-life at least one year at ambient temperature.

Impact: These are quality-control constraints. If an accused product is outside pH range or lacks claimed shelf life, it may avoid the dependent claims. Claim 1 itself does not require pH/shelf-life, so the independent claim can still be asserted against nonconforming pH if the core carrier/propellant/surfactant/HBL architecture is present.

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What is the likely claim architecture strategy and what does it imply about prior art vulnerability?

The claim strategy blends:

• Independent claim 1 with a distinctive combination of:

  • azelaic acid fixed at ~15% of carrier,
  • a carrier solvency package (hydrophobic + polar + water),
  • polymeric agent,
  • surfactant system with HLB differential ≥4,
  • and defined total polymeric+surfactant wt% in the carrier,
  • plus a gas propellant window at composition level.

• Dependent claims that:

  • lock specific identities for solvents (dimethyl isosorbide; caprylic/capric triglyceride),
  • identify common surfactant exemplars likely spanning low and high HLB values (glyceryl stearate, PEG-40 stearate, Polysorbate 80),
  • identify common foam thickening polymers (xanthan gum; methylcellulose),
  • and define foam adjuvants by carbon count.

This architecture indicates the novelty is likely not “foamable azelaic acid” per se, but rather the specific formulation system where the surfactant pairing and HLB spacing appear as a discriminating feature.

From an invalidity standpoint, the weakest point for many such patents is often whether prior art teaches:

• the same azelaic acid level (or an obvious range),
• the same solvent combination (hydrophobic emollient + dimethyl isosorbide),
• and especially whether prior art teaches using an HLB differential rule for surfactant selection in this product context.

If prior art independently discloses azelaic acid foams with dimethyl isosorbide and emulsifier systems, an attack would likely attempt to treat the HLB differential as an inherent property of a known pair of surfactants. The presence of explicit surfactant exemplars in dependent claims can cut both ways: it gives enforceability targets but can provide prior art hooks if those same surfactants are known in the art for similar vehicles.

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How strong is the patent estate likely to be around the key discriminators (HLB differential, azelaic acid 15%, propellant 3–25%)?

Discriminator 1: HLB differential “about 4 or more”

This is the most litigation-relevant discriminator because it is:

• not just a component identity,
• but a relational constraint between at least two surfactants.

Infringement mapping risk: If an accused product uses two surfactants but their HLB values differ by <4, it falls outside claim 1 even if the rest of the formulation matches.
Invalidity mapping risk: An invalidity case must show that the prior art teaches the same relational rule or makes it an obvious selection. If prior art uses low- and high-HLB surfactants in similar vehicles for solubilization/foam stability, the “≥4” may be attacked as an inherent outcome of combining common surfactants.

Discriminator 2: Azelaic acid at about 15% of the carrier

This is a numeric anchor. Many azelaic formulations fall in a typical strength band. The enforceability depends on whether prior art discloses the same concentration (or whether ~15% is a predictable optimization point).

Discriminator 3: Propellant 3–25% wt of composition

Propellant level is often formulation-dependent. This range provides claim coverage across low to mid propellant loading. Design-around may involve moving outside this window.

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What design-arounds are suggested by the claim language (what can be changed without leaving infringement)?

Design-around candidates follow claim constraints:

1. Surfactant system

   • Reduce the HLB differential between surfactant pair(s) to <4 units.
   • Use fewer than two surfactants (though claim 1 requires at least two).
   • Swap to surfactants whose HLB spacing fails the “≥4” rule.

2. Azelaic concentration

   • Move azelaic acid away from ~15% of the carrier.

3. Carrier polymeric+surfactant total

   • Keep combined polymeric agent + surface-active agent outside 0.05% to 10% wt of carrier.

4. Propellant level

   • Move propellant outside 3–25% wt of composition.

5. Dependent claim-specific swaps

   • Avoid dimethyl isosorbide and caprylic/capric triglyceride at the claimed carrier amounts.
   • Use polymeric agents outside 0.01% to 5% or avoid xanthan/methylcellulose.
   • Avoid fatty adjuvants with ≥15/≥16 carbons or avoid cetostearyl alcohol.
   • Introduce short-chain alcohols but only if they can remain <5% wt of carrier; otherwise avoid.

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What other US patents likely intersect this landscape and how do they relate to claim 10,322,085?

Without the full bibliographic record (assignee, application number, priority dates, and prosecution history) and without an Orange Book linkage (if any) tied to a specific marketed product, this analysis cannot reliably map:

• related continuation/divisional claims,
• other US publications by the same assignee around azelaic foams,
• or the exact family boundaries that determine what else is protected.

If the only available material is the claim text supplied, the only actionable “landscape” conclusion that can be drawn is structural: this patent sits in a topical foam formulation space, not in a method-of-treatment use space, and is centered on a carrier/surfactant/polymer/propellant architecture. Intersection with other patents would typically occur in those same formulation elements: gas propellants in topical foams, azelaic acid vehicles, polymeric thickeners for foam stability, and solubilizers/emollients such as dimethyl isosorbide and long-chain foam adjuvants.

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What is the key litigation and regulatory posture for this type of patent?

This is a formulation patent, not an exclusivity token. Practical regulatory and litigation impact usually depends on:

• whether the patent is asserted against a competitor’s commercial foam product, or
• whether it is asserted during ANDA/BLA style challenges (typically for small-molecule oral drugs; for topical formulations, challenges may be via patent assertions tied to product launch rather than Hatch-Waxman paragraph IV).

The claim set does not recite a therapeutic method, a dosing regimen, or a specific indication; it is a composition claim. As a result, the most direct enforcement path is product-by-product composition mapping rather than label/indication mapping.

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What commercial exposure does this claim structure create (who is at risk)?

The scope risks parties manufacturing or distributing:

• azelaic acid topical foam with a propellant,
• using a carrier containing ~15% azelaic acid (carrier basis),
• with a hydrophobic solvent in 2–50% of the carrier,
• with water and a polymeric agent,
• and a surfactant system where the HLB values of at least two surfactants differ by ≥4.

The risk is highest where the formulation also uses:

• dimethyl isosorbide (especially ~5% of carrier),
• caprylic/capric triglyceride (~11% of carrier),
• xanthan gum or methylcellulose as the polymer,
• glyceryl stearate paired with PEG-40 stearate and/or Polysorbate 80,
• and cetostearyl alcohol or other C15+ alcohol / C16+ fatty acid foam adjuvants.

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Key takeaways

• Claim 1 is the coverage spine: foamable azelaic acid composition with strict carrier composition, defined propellant loading, and a surfactant HLB differential constraint (≥4).
• Dependent claims create enforceable “product fingerprints” around dimethyl isosorbide, caprylic/capric triglyceride, glyceryl stearate plus high-HLB nonionic surfactants, xanthan/methylcellulose, and cetostearyl alcohol.
• The strongest enforcement lever is the HLB differential requirement, because it can exclude close variants even when the rest of the vehicle matches.
• The strongest design-around lever is surfactant selection to break the “≥4 HLB difference” condition, or to move azelaic concentration/propellant level outside the claimed windows.
• The provided claim set alone supports only a structural formulation landscape assessment; a complete US patent landscape requires the patent bibliographic data and related family members.

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FAQs

1. Can a product avoid infringement by using different surfactants with similar functions?
   Yes if it fails the claim 1 HLB differential rule (≥4 units) or fails the requirement for at least two surfactants with the required HLB spacing.

2. Does claim 1 require dimethyl isosorbide or caprylic/capric triglyceride?
   No. Those are in dependent claims 4–6 and 2–3; claim 1 only requires a polar solvent and a hydrophobic solvent within ranges.

3. What if an accused product matches the azelaic acid and propellant ranges but uses a different polymer?
   It can still infringe claim 1 if it has a polymeric agent meeting the required combined polymeric+surfactant content range, unless the polymer identity or quantity is used to move outside claim 1’s combined-total limitation.

4. How do foam adjuvants affect infringement risk?
   Foam adjuvants (C15+ alcohol/C16+ acid) are addressed in dependent claims 16–18; they can increase risk if present but are not required by claim 1.

5. Is pH or shelf-life required to infringe independent claim 1?
   No. pH (4.0–6.0) is claim 21 and shelf-life is claim 22. Those apply only to those dependent claims, not to claim 1.

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References (APA)

1. US Patent 10,322,085.

Drugs Protected by US Patent 10,322,085

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: 10,322,085

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Israel	152486	Oct 25, 2002

International Family Members for US Patent 10,322,085

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2003279493
Australia	2004261063
Australia	2004266502
Australia	2004313285
Australia	2004321183
Australia	2005204341
Australia	2005204347