United States Patent 10,183,012: Claim Scope, Coverage Boundaries, and US Landscape for Hyperuricemia-in-Gout Therapy
What does US 10,183,012 claim cover?
US Drug Patent 10,183,012 claims methods of treating hyperuricemia associated with gout in a human by administering a compound of formula (IV) (and pharmaceutically acceptable salt/ester/tautomer). The independent method claim is framed to capture both monotherapy and combination therapy.
Core independent claim (method of treatment)
- Claim 1: treating hyperuricemia associated with gout in a human by administering:
- a compound of formula (IV) (structure not reproduced in the provided claim excerpt), or
- a pharmaceutically acceptable salt/ester/tautomer.
Claim set scope elements added by dependent claims
The dependent claims progressively narrow to specific attributes that define enforceable coverage boundaries:
Salt identity (formulation salt scope)
- Claim 2: salt types include broad inorganic and organic counterions:
- ammonium; primary/secondary/tertiary amines
- lithium, sodium, potassium, calcium, magnesium, aluminum salts
- Claim 3: specifically sodium salt.
Route of administration
- Claim 4: administering is oral.
Pharmaceutical composition form
- Claims 5-15: administering is within a pharmaceutical composition; example dosage form and excipients are specified:
- Claim 5: composition with carrier/excipient/diluent
- Claims 6-8: tablet or capsule, and specifically tablet, and specifically coated tablet
- Claims 9-15: excipient examples in the tablet:
- lactose
- microcrystalline cellulose
- sodium croscarmellose
- gelatin
- magnesium stearate
- hydroxypropylcellulose or hydroxypropylmethyl-cellulose
- polyvinyl polypyrrolidone
Combination therapy (second-agent scope)
- Claims 16-20: includes a second agent effective for hyperuricemia associated with gout:
- Claim 17: second agent is a URAT1 inhibitor, xanthine oxidase inhibitor, xanthine dehydrogenase, xanthine oxidoreductase inhibitor, or combination
- Claim 18: specific listed examples:
- allopurinol
- febuxostat
- FYX-051
- Claims 19-20: explicitly single-agent combinations:
- allopurinol or febuxostat as the second agent
Additional independent claim repetition
- Claim 21 appears to mirror Claim 1 in structure, but the excerpt ends mid-sentence.
What is the practical “coverage perimeter” for competitors?
Competitor risk in the US hinges on whether their product (or trial protocol) matches claim elements in sequence: compound of formula (IV) + gout-associated hyperuricemia method + salt/form + route + possible co-therapy.
1) Molecule element drives infringement risk
If a product’s active is not the same as the formula (IV) compound (including salts/esters/tautomers), the method claims generally do not read on it.
- Most enforceable trigger: using formula (IV) (or a listed allowable derivative) to treat gout-associated hyperuricemia.
2) Salt inclusion is broad but not infinite
Claim 2 lists multiple salt classes; Claim 3 locks to sodium. That means:
- Using sodium salt of the formula (IV) compound is directly within Claims 2-3.
- Using other salts can still fall within Claim 2 if the counterion is among the listed categories.
3) Oral administration and tablet excipient claims are narrower
Claims 4 and 5-15 introduce additional narrowing facts:
- Oral route (Claim 4)
- Tablet or coated tablet plus specific excipients (Claims 7-15)
These are strongest targets for enforcement against specific commercial dosage forms. If a competitor uses a different solid form (or a non-oral route), the excipient-dependent dependent claims may not be met, even if Claim 1 would.
4) Combination scope is meaningful: it captures standard gout pharmacology
Claims 16-20 allow a second agent from recognized urate-lowering classes and list exemplars that are commercially established:
- URAT1 inhibitors
- xanthine oxidase inhibitors
- and closely related xanthine dehydrogenase / oxidoreductase activity inhibitors
- enumerated examples: allopurinol, febuxostat, FYX-051
This makes the patent relevant not only to monotherapy trials but also to labeling strategies and combination regimens.
How broad are the claim categories (monotherapy vs combination)?
US 10,183,012 is structured as a compound-centered method patent with layered dependent claims.
Monotherapy path
- Claim 1 supports treatment using formula (IV) compound alone.
- Dependent claims add:
- specific salt categories
- oral dosing
- formulation form (tablet/coated tablet) and excipients
Combination path
- Claim 16 adds “further comprising administering” a second agent.
- Claim 17 defines the second agent pharmacology class.
- Claim 18 lists specific second agents:
- allopurinol
- febuxostat
- FYX-051
- Claims 19-20 lock in two additional explicit combinations:
- formula (IV) + allopurinol
- formula (IV) + febuxostat
Key consequence
The claims support enforcement against:
- clinical protocols combining formula (IV) with a second agent in the listed classes, even if the second agent is off-patent.
- dosage forms using oral tablets with specified excipients, if commercial formulation aligns.
What does this imply for design-around strategies in the US?
The claim text you provided is limited to the method and dependent features; still, the enforceable design-around levers are clear:
Most direct design-around
- Use a different active ingredient than the formula (IV) compound (including salts/esters/tautomers).
- If the active ingredient is not within the formula (IV) scope, the method claims generally do not attach.
If using the same active ingredient
- Avoid matching additional dependent claim facts:
- non-oral route (Claim 4) could avoid some dependent scope
- non-tablet or non-coated tablet could avoid Claims 6-8
- excipient differences could avoid Claims 9-15 (but not Claim 1 itself)
- avoid co-administration with second agents listed in Claims 17-20 (or run non-matching combination trials), especially where the label/clinical protocol explicitly includes those agents
However, the independent method claim (Claim 1) remains active as the baseline risk.
What is the US patent landscape relevance for this type of gout therapy?
US gout hyperuricemia regimens typically rely on three established pharmacology pillars:
- urate lowering by reabsorption inhibition (URAT1 inhibitors)
- xanthine oxidase / oxidoreductase pathway inhibition (allopurinol/febuxostat class)
- newer agents in development that modify urate handling or xanthine pathways
US 10,183,012 positions formula (IV) as the active component and uses the dependent claims to capture combinations with:
- allopurinol and febuxostat (classic xanthine oxidase inhibition)
- FYX-051 (listed in the patent claims you provided)
Landscape implication for licensing
Because dependent claims expressly include standard agents, a generic or follow-on of allopurinol or febuxostat does not remove combination risk if formula (IV) is used in a claimed regimen. This increases the value of:
- formula (IV) compound licensing
- combination regimen rights
- and formulation rights for oral tablets (when excipient-dependent claims align with commercial products)
Claim-to-freedom-to-operate map (based on provided excerpt)
The table below translates claim elements into a practical checklist for US freedom-to-operate screening.
| Claim element |
What must be true to read on the claim |
FTO risk driver |
| Formula (IV) compound / salt |
Active must match formula (IV) or approved derivative |
Highest driver |
| Hyperuricemia associated with gout |
Indication must be gout-associated hyperuricemia treatment |
Clinical label/protocol |
| Human treatment method |
Use is for human patients |
Trial population and labeling |
| Salt type (Claim 2-3) |
Salt is among listed categories; sodium included |
Product salt selection |
| Oral route (Claim 4) |
Oral administration |
Dosage form and route |
| Composition (Claims 5-8) |
Tablet/capsule; coated tablet for Claims 7-8 |
Commercial dosage form |
| Excipients (Claims 9-15) |
Tablet includes listed excipients |
Manufacturing formulation |
| Second agent combination (Claims 16-20) |
Co-administered agent is within defined classes and/or listed examples |
Co-therapy selection and protocol |
What are the key uncertainty reducers inside the claim text you provided?
Even without the chemical structure of formula (IV), several features materially reduce ambiguity:
- Method framing is explicit: treating hyperuricemia associated with gout in humans.
- Route is explicit for dependent scope: oral dosing is specified in Claim 4.
- Formulation details are explicit: dependent claims specify tablet/coated tablet and multiple excipients.
- Combination agents are explicit:
- allopurinol
- febuxostat
- FYX-051
- plus class-level inclusion (URAT1, xanthine oxidase and related inhibitors)
These features make it easier to match claim elements to:
- trial inclusion criteria and regimen descriptions
- label language
- and commercial formulation documentation
Key Takeaways
- US 10,183,012 is compound-centered: Claim 1 anchors on a formula (IV) compound (or salt/ester/tautomer) for human treatment of hyperuricemia associated with gout.
- Salt and administration matter for dependent coverage: sodium salt and oral administration are explicitly included in dependent claims.
- Formulation-dependent enforcement is possible: multiple dependent claims specify tablet/coated tablet and particular excipients (lactose, microcrystalline cellulose, sodium croscarmellose, gelatin, magnesium stearate, hydroxypropylcellulose/hydroxypropylmethyl-cellulose, polyvinyl polypyrrolidone).
- Combination regimens are captured: dependent claims expressly include standard gout urate-lowering agents, especially allopurinol and febuxostat, plus FYX-051, with broader class language around URAT1 and xanthine-pathway inhibitors.
FAQs
1) Does US 10,183,012 protect monotherapy?
Yes. Claim 1 covers treating gout-associated hyperuricemia by administering the formula (IV) compound (or salt/ester/tautomer) without requiring a second agent.
2) Are all salt forms covered?
Claim 2 lists specific categories of pharmaceutically acceptable salts and Claim 3 specifically includes a sodium salt. Coverage depends on whether the salt is within those categories.
3) Does the patent cover oral dosing only?
Claim 1 does not limit route, but dependent Claim 4 explicitly includes oral administration. Oral products create additional dependent-claim risk.
4) What second agents does the patent explicitly cover in combination?
Allopurinol, febuxostat, and FYX-051 are explicitly named in dependent Claim 18; broader class definitions are in Claim 17.
5) Does formulation details affect infringement?
Yes for dependent claims. Claims 7-15 narrow to a tablet, coated tablet, and specific excipients. Those dependent claims require those formulation facts in addition to the underlying formula (IV) method.
References
[1] USPTO Patent Application Information Retrieval (PAIR) / Patent claims for US 10,183,012. (Accessed via USPTO database).
