United States Patent 12,564,593: Scope, Claim Strategy, and US Topography
US Drug Patent 12,564,593 claims a topical skin pharmaceutical oil-in-water emulsion defined by (i) a tightly bounded vehicle composition and (ii) a specific active ingredient salt: (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile phosphoric acid salt, expressed “on a free base basis.” The claim set is structured to lock down both the emulsion architecture and the exact formulation ranges, then carve narrower dependent fallbacks with particular excipient identities and optional preservative/chelant packages, plus a pH cap (≤3.6) in one dependent claim.
Claim numbers provided cover independent claim 1 and multiple dependents, plus separate independent compositions framed in claims 17 and 20. The scope is formulation-centric: the patent’s enforceable value is concentrated in the specific quantitative ranges and salt+carrier combination for topical use.
What is claimed: active + oil-in-water emulsion with defined excipient system?
What is the structural claim anchor (the “must-have” elements)?
Core requirements repeated across the independent claim set:
- Dosage form: “A pharmaceutical formulation for topical skin application”
- Emulsion type: “oil-in-water emulsion”
- Water content: 35%–65% by weight (claim 1) or 45%–55% (claim 17 and 20)
- Oil-phase excipient package: a defined mixture comprising:
- petrolatum + C16-18 fatty alcohols + mineral oil + triglyceride + silicone oil (quantified as a single combined mixture in claim 1)
- Emulsion stabilizer / fatty ester-tenside package: glyceryl fatty ester + sorbitan fatty ester within a defined range
- Polysaccharide thickener / rheology modifier: polysaccharide within a defined range
- Humectant pair: alkylene glycol + polyalkylene glycol within a defined range
- Active ingredient: the specified (R)-... phosphoric acid salt, present at 0.5%–1.5% by weight (free base basis) in the broad independent claim (claim 1), with the same parameter repeated in the later independent compositions as 0.5%–1%.
What is the quantitative footprint in claim 1?
Claim 1 defines the formulation by ranges (weight percent of total formulation):
| Component class (claim 1) |
Range in claim 1 (wt%) |
| Water |
35%–65% |
| Mixture of petrolatum + C16-18 fatty alcohols + mineral oil + triglyceride + silicone oil |
10%–40% |
| Mixture of glyceryl fatty ester + sorbitan fatty ester |
2%–6% |
| Polysaccharide |
0.05%–5% |
| Mixture of alkylene glycol + polyalkylene glycol |
10%–35% |
| Active (R-... phosphoric acid salt, free base basis) |
0.5%–1.5% |
Interpretation for scope: the patent’s broadest perimeter is not “any oil-in-water emulsion with this active.” It is an emulsion with a specific excipient architecture and bounded weight fractions for each architecture block.
Dependent claim locking: specificity on excipient identities and concentration windows
Which dependents narrow excipient identities?
Claims 2, 3, 7, 8, 12, 13 identify preferred excipient species inside the generic functional categories.
Claim 2 (a specific exemplifying set) pins:
- Petrolatum: white petrolatum
- C16-18 fatty alcohols: cetyl alcohol + stearyl alcohol
- Mineral oil: light mineral oil
- Triglyceride: medium chain triglycerides
- Silicone oil: dimethicone
- Glyceryl fatty ester: glyceryl stearate
- Sorbitan fatty ester: polysorbate 20
- Polysaccharide: xanthan gum
- Alkylene glycol: propylene glycol
- Polyalkylene glycol: polyethylene glycol
Claims 3 and 8 shift PEG specificity to lower molecular weight:
- Claim 3: polyethylene glycol 200
- Claim 8: glyceryl stearate SE and polyethylene glycol 200
Claims 12 and 13 likewise pick the same excipient roster as claim 2/3 variants but are bound to the narrower quantitative ranges of claim 11.
Which dependents narrow the composition ranges (not just the excipient names)?
Claim 6 narrows the overall range splits (still with the generic excipient categories):
- Water: 40%–60%
- Petrolatum/fatty alcohol/mineral oil/glyceride/silicone mixture: 17%–27%
- Glyceryl fatty ester + sorbitan fatty ester: 3%–5%
- Polysaccharide: 0.1%–2%
- Alkylene glycol + polyalkylene glycol mixture: 15%–30%
Claim 11 narrows further:
- Water: 45%–55%
- Petrolatum/fatty alcohol/mineral oil/glyceride/silicone mixture: 20%–27%
- Glyceryl fatty ester + sorbitan fatty ester: 3%–5%
- Polysaccharide: 0.3%–0.5%
- Alkylene glycol + polyalkylene glycol mixture: 20%–25%
These tighter dependent windows matter because they define enforceable fallbacks even if a challenger argues that the broader independent range is not met.
Preservative and chelant modules: what extra ingredients are allowed?
What do the dependents say about chelating agents and antimicrobials?
- Claim 4: adds:
- “a chelating agent component”
- and 0.05%–3% antimicrobial preservative component
- Claim 9: same concept tied to claim 7
- Claim 14: same concept tied to claim 12
- Claim 23: does not add chelant/preservative; it is active-range focused.
Which specific preservative exemplars are listed?
-
Claim 5 (tied to claim 3) adds:
- methyl paraben 0.1%
- propyl paraben 0.05%
- edetate disodium 0.05%
- phenoxyethanol 0.5%
-
Claim 10 adds the same quartet to claim 8
-
Claim 15 adds the same quartet to claim 13
-
Claim 18 adds the same quartet to claim 17
-
Claim 21 adds the same quartet to claim 20
Scope implication: the patent includes formulations with (and dependent fallbacks around) a specific preservative pattern, but those dependents are not described as mandatory in claim 1 or the later independent claims unless tied via the dependency.
pH constraint: when does acidity become part of claim scope?
What does the pH limitation do?
- Claim 23: “oil-in-water emulsion has a pH of not greater than 3.6.”
Scope implication: this is a further narrowing feature, not present in the main independent claim text provided. It can operate as a targeted enforcement hook for acidic emulsion competitors.
Separate independent compositions: claim 17 and claim 20 create “hard point” compositions
Claims 17 and 20 operate as independent formulations with fixed weight percentages (not just ranges). They reduce design-around flexibility by setting exact amounts for many excipient classes.
What is the exact composition in claim 17?
Claim 17 defines:
- Water: 45%–55%
- Petrolatum: 7%
- C16-18 fatty alcohols: 4.75%
- Mineral oil: 4%
- Glyceride: 5%
- Silicone oil: 1%
- Glyceryl fatty ester: 3%
- Sorbitan fatty ester: 1.25%
- Polysaccharide: 0.4%
- Alkylene glycol: 15%
- Polyalkylene glycol: 7%
- Active: 0.5%–1.5% (free base basis)
Claim 18 adds the preservative quartet (same amounts as claim 5).
Claim 19 re-confirms active range 0.5%–1% (free base basis).
What is the exact composition in claim 20?
Claim 20 defines:
- Water: 45%–55%
- White petrolatum: 7%
- Cetyl alcohol: 3%
- Stearyl alcohol: 1.75% (split is explicit)
- Light mineral oil: 4%
- Medium chain triglycerides: 5%
- Dimethicone: 1%
- Glyceryl stearate: 3%
- Polysorbate 20: 1.25%
- Xanthan gum: 0.4%
- Propylene glycol: 15%
- Polyethylene glycol: 7%
- Active: 0.05%–1.5% (free base basis) (note the lower lower-bound here differs from claim 1 and claim 17)
Claim 21 adds the preservative quartet.
Claim 22 ties the active to 0.5%–1% (free base basis) for this dependent path.
Active ingredient boundary: salt identity and percent range are the hinge
How does the active concentration vary across the claim set?
| Claim |
Active presence (wt%, free base basis) |
| 1 |
0.5%–1.5% |
| 16 |
0.5%–1% |
| 17 |
0.5%–1.5% |
| 19 |
0.5%–1% |
| 20 |
0.05%–1.5% |
| 22 |
0.5%–1% |
Scope implication: claim 20 expands the low end down to 0.05%. If a competitor uses the same salt and an oil-in-water emulsion meeting claim 20’s fixed excipient layout, the patent perimeter includes lower-dose formulations down to 0.05% (subject to the other fixed excipient amounts).
Practical infringement map: where competitors are most likely to land inside vs outside the claims
Most likely “inside” zones (highest risk for copycats)
- Same excipient architecture + same salt + overlapping ranges
- Oil-in-water emulsion
- Water between 35%–65% (or 45%–55% in claims 17/20)
- Petrolatum + C16-18 fatty alcohols + mineral oil + triglyceride + dimethicone in 10%–40% (claim 1)
- Xanthan gum at the claimed level
- Broad: 0.05%–5% (claim 1)
- Narrow: 0.3%–0.5% (claim 11)
- Fixed: 0.4% (claims 17 and 20)
- PEG/propylene glycol split and totals
- Broad: combined alkylene glycol + polyalkylene glycol 10%–35% (claim 1)
- Narrow: 20%–25% (claim 11)
- Fixed: propylene glycol 15% and PEG 7% (claims 17/20)
Most likely “outside” design-around levers
Because claim 1 is a block-range claim, competitors can try to avoid meeting all block bounds simultaneously:
- Alter water weight percent beyond the claimed range.
- Adjust the combined petrolatum/fatty alcohol/mineral oil/glyceride/silicone block outside 10%–40% (claim 1) or outside the narrower 17%–27% / 20%–27% (claims 6/11).
- Use a different polysaccharide or shift xanthan gum outside the claimed window.
- Change the PEG identity (claim dependents specify PEG and PEG200 in certain paths; claim 1 only requires “polyalkylene glycol,” so avoiding specific PEG may not avoid claim 1 but can avoid dependent claim scope).
- Shift the active salt outside 0.5%–1.5% (claim 1/17) or below 0.05% (claim 20). Note: claim 20 reaches down to 0.05%, which is a tougher low-dose boundary.
Patent landscape framing (US) grounded to the provided claim text
What can be concluded from the claim record you provided
- The patent’s enforceable hook is formula-defined topical emulsion with a defined salt and explicit quantitative excipient partitioning.
- The claim architecture includes:
- A broad independent (claim 1) with block-level ranges.
- Two additional independents (claims 17 and 20) with fixed composition points and specific excipient species.
- Dependent claim sets that:
- lock down excipient identities,
- tighten range splits,
- add preservative/chelating modules,
- cap pH to ≤3.6.
What cannot be concluded without the publication record
No additional US landscape statements can be made from the claim text alone (for example: grant date, priority chain, whether there are related continuations, whether other families cite it, or whether interferences or PTA exist). The scope below therefore focuses on claim-set topology and design-around logic rather than external citations.
Key Takeaways
- US 12,564,593 covers topical oil-in-water emulsion formulations using a specific (R)-... phosphoric acid salt, with enforceable boundaries tied to both excipient blocks and quantitative wt% ranges.
- Claim 1 is the broadest perimeter: it constrains the formulation by water (35%–65%), oil-phase block (10%–40%), fatty ester-tenside block (2%–6%), polysaccharide (0.05%–5%), and glycol pair (10%–35%), plus active 0.5%–1.5%.
- Claims 17 and 20 create fixed-point independent compositions with many excipients at exact wt% values and a notably broader active lower bound in claim 20 (0.05%–1.5%).
- Dependent claims add preservative/chelating modules, tighten excipient selection (xanthan gum, dimethicone, specific fatty esters), and impose a pH ≤3.6 limitation in claim 23.
- The highest-risk competitive space is formulations that match the salt identity and land within the xanthan gum level and glycol/emulsifier partitioning windows, particularly where emulsion pH is also ≤3.6.
FAQs
1) Does US 12,564,593 require xanthan gum?
Not in claim 1 as written; claim 1 requires a generic “polysaccharide” within 0.05%–5%. Xanthan gum is explicitly required in the dependent identity claims (e.g., claims 2, 7, 12, 13).
2) What is the active ingredient dose range in the broadest claim?
In claim 1, the salt is present at 0.5%–1.5% by weight (free base basis). A lower bound appears in claim 20 (down to 0.05%).
3) Are preservatives mandatory for infringement?
No. Preservatives are introduced via dependent claims (e.g., claims 5, 10, 15, 18, 21). The core claim 1 and the independent fixed compositions can be met without those dependents.
4) What is the significance of claim 23’s pH limitation?
Claim 23 requires the oil-in-water emulsion to have pH ≤3.6. It narrows scope to acidic formulations along the dependent claim path.
5) Which claim set is most useful for designing a generic or next-gen formulation around the patent?
Claims 17 and 20 are most restrictive because they fix many excipient concentrations and compositions. Claim 1 is more flexible by using block-level ranges, but it still imposes simultaneous constraints across multiple ingredient classes.
References
- United States Patent Application/Patent No. 12,564,593 (claims excerpt provided in prompt).
