Details for Patent: 10,639,297

Which drugs does patent 10,639,297 protect, and when does it expire?

Patent 10,639,297 protects QLOSI and is included in one NDA.

This patent has twenty-six patent family members in fourteen countries.

Summary for Patent: 10,639,297

Title:	Ophthalmic pharmaceutical compositions and uses relating thereto
Abstract:	The disclosure relates to ophthalmic pharmaceutical compositions comprising pilocarpine or a pharmaceutically acceptable salt. Aspects of the disclosure further relate to uses and preparations of ophthalmic pharmaceutical compositions comprising pilocarpine or a pharmaceutically acceptable salt, for correcting presbyopia and other ocular conditions in a subject.
Inventor(s):	Claes Feinbaum, Franc SALAMUN, Sudhir PATEL
Assignee:	Orasis Pharmaceuticals Ltd
Application Number:	US16/032,044
Patent Claim Types: see list of patent claims	Use; Composition;

Scope and Claims Analysis for US Patent 10,639,297: Pilocarpine Ophthalmic Presbyopia/Higher Order Aberration and Depth-of-Field Compositions Using Hyaluronic Acid or Cellulose Lubricants

US Patent 10,639,297 protects an ophthalmic pilocarpine regimen and composition built around (i) low-dose pilocarpine (or salts) at ~0.01% to ~0.45% and (ii) a lubricant selected from hyaluronic acid/salts or specified cellulose/polyol excipients. Independent protection sits in composition claim 1 and multiple downstream method claims directed to presbyopia correction (up to 24 hours), increasing depth of field, and reducing pupil size. Claim coverage is structured to capture both formulation variations (lubricant identity and concentration windows) and clinical use variations (timing/night-vision outcomes and broad patient subpopulations).

What patents protect pilocarpine ophthalmic compositions for presbyopia using hyaluronic acid or HPMC?

Independent claim anchor: composition claim 1

Claim 1 is the core. It covers an ophthalmic pharmaceutical composition consisting of:

• Active: pilocarpine or salt (pilocarpine HCl / nitrate explicitly called out in dependent claims)
• Concentration: about 0.01% to about 0.45% (w/w or w/v)
• Lubricant: selected from a defined closed set that includes:
  • hyaluronic acid or pharmaceutically acceptable salts (the claim later specifies sodium hyaluronate)
  • cellulose and cellulose derivatives including carboxymethyl cellulose sodium, hydroxyethyl cellulose, methylcellulose, hydroxypropyl methylcellulose (HPMC), plus other listed polymers/excipients such as dextran, gelatin, polyols, and select surfactant-like/solubilizer excipients including povidone and polysorbate.
• Carriers: “one or more pharmaceutically acceptable carriers” with no structural limitation

Key consequence: any ophthalmic composition meeting the pilocarpine concentration window and using a lubricant chosen from the listed set falls inside claim 1, even if the rest of the carrier system differs.

Independent method anchor: claim 8

Claim 8 is the clinical-use equivalent of claim 1:

• Administer an ophthalmic composition per claim 1
• Purpose: correcting presbyopia

It is not limited to a particular delivery mechanism beyond “administering,” and dependent claims add topical and surgical intervention language.

Additional independent functional protection: depth of field and pupil size

Independent methods also extend the protected “medical effect” scope:

• Claim 17: increasing depth of field
• Claim 23: reducing pupil size

Those expand infringement pathways beyond presbyopia correction into optical-performance and pupil-response mechanisms, while still requiring the same composition architecture.

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What is the exact claim scope of US Patent 10,639,297: pilocarpine concentration, lubricant selection, and carriers?

Pilocarpine concentration window

Protected active range appears across multiple independent claims:

• About 0.01% to about 0.45% pilocarpine (or salt)

Dependent claims then lock specific ranges for some embodiments:

• About 0.2% to about 0.45% (claims 6 and 11 and 22 and 28)

Practical inference for designing-around: the patent’s strongest edge is pinned to these windows. Moving outside the window may eliminate coverage for claims that require the range.

Lubricant selection: closed list with two major clusters

The lubricant list in claim 1 is broad but closed (defined group). The two major clusters are:

1. Hyaluronic acid/salts

   • Covered in general via “hyaluronic acid or pharmaceutically acceptable salt thereof”
   • Dependent specificity centers on sodium hyaluronate

2. Cellulose and cellulose derivatives plus selected polymeric excipients

   • carboxymethyl cellulose sodium
   • hydroxyethyl cellulose
   • methylcellulose
   • hydroxypropyl methylcellulose (HPMC)
   • plus dextran, gelatin, polyol, glycerin, PEG 300/400, polysorbate, propylene glycol, PVA, povidone, and mixtures

Because the claim allows “one or more” lubricants and does not restrict ratios unless dependent claims do, infringement risk is tied to whether the formulation uses at least one lubricant in the recited list and falls into the active range.

Lubricant concentration embodiments that tighten or broaden

Several dependent claims define narrower lubricant concentrations:

• Sodium hyaluronate: 0.01% to 0.9%
• HPMC: 0.1% to 2.0%
• Lubricant concentration (general): 0.01% to 3.0% (claim 5 and mirrored in methods)

These dependent claim windows matter because:

• A formulation that meets the general lubricant list but uses concentrations outside the dependent ranges might still infringe claim 1 (if it falls within the claim 1 lubricant concept and active range), while depending on how the formulation is characterized as lubricant vs another excipient.

Carriers: broad and likely to be non-limiting

Claim 1 uses “one or more pharmaceutically acceptable carriers” without constraints.

Claim 30 is much broader in excipient enumeration: it includes a wide menu of carriers, including:

• solvents, solubilizers, pH agents, dispersing agents, diluents, suspension aids, surfactants
• isotonic agents, stabilizers, thickening/emulsifying agents, preservatives
• buffers
• polymers, core-shell nanoparticles
• peptides/proteins

This indicates the patent is designed to protect against generic formulation substitution with different vehicle compositions so long as the pilocarpine + lubricant + active concentration core is maintained.

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When does this patent lose exclusivity in the US? (expiration/term analysis)

No expiration dates, filing dates, priority claims, or prosecution/adjustment details were provided in the prompt. Without those, a legally accurate exclusivity or patent-term timeline cannot be produced.

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What claims target pilocarpine salt identity: hydrochloride vs nitrate?

Dependent salt specificity

• Claim 2 (composition): pilocarpine salt is pilocarpine hydrochloride or pilocarpine nitrate
• Claim 9 (method): same salt limitation
• Claim 18 and following: same salt limitation in depth-of-field and pupil-size methods

This creates two infringement patterns:

1. If the product uses pilocarpine base or a different pharmaceutically acceptable salt not listed, the dependent claims may not read, but claim 1 still covers “pilocarpine or a pharmaceutically acceptable salt thereof.”
2. The dependent claims expand ease of mapping for litigants by specifying the common clinical salts.

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What formulations are protected: sodium hyaluronate + HPMC combinations for 24-hour presbyopia?

Claim 6 and 11/22/28: combined lubricant embodiments

These claims cover specific paired lubricant concentration windows:

• pilocarpine ~0.2% to ~0.45%
• sodium hyaluronate 0.01% to 0.9% and/or HPMC 0.1% to 2.0%

Claim 7 and 29: duration and use outcome

• Claim 7: presbyopia correction up to 24 hours
• Claim 14: presbyopia method for up to 24 hours and/or “effective without adversely affecting night vision” (dependent on claim 9 language)

These are meaningful because they tie the clinical endpoint to a time horizon and a night-vision safety/performance assertion.

Claim 38: formulation tie-back

• Claim 38 states lubricant is sodium hyaluronate (a dependent narrowing of claim 30).

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What patient groups and clinical scenarios expand method claim coverage?

Broad subject inclusion in claim 16

Claim 16 recites a large set of subject attributes, including:

• spectacle wearers who cannot/will not use progressive or bifocal lenses
• post-cataract surgery
• presbyopia after corneal procedures
• patients with mono- or multifocal intraocular lenses
• contact lens users with tolerance constraints (no monovision, no multifocal)
• higher order aberration after corneal surgery
• hyperopia or tropias
• intolerance to spectacle prescription changes or rapid changes
• risk of falls with progressive/bifocal lenses
• higher order aberration at night or under light conditions

This is not limited to any one disease state. It is drafted to sweep a wide “presbyopia-with-optical-complexity” cohort where pilocarpine-induced optical changes may be preferred.

Topical or surgical administration in claim 15

Claim 15 states administration may be:

• topical or by surgical intervention

That expands the infringement surface: a product platform is less likely to avoid risk by arguing it is “not a drop” if it still administers the claimed composition by surgical means.

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What performance goals are protected beyond presbyopia? depth of field and pupil size?

Depth of field method claims (claim 17 and dependent structure)

• Claim 17 covers increasing depth of field using the same composition framework.
• Dependent claims specify lubricant identity, concentrations, and pilocarpine concentration ranges.

Pupil size reduction (claim 23 and dependent structure)

• Claim 23 covers reducing pupil size using the same composition framework.
• Dependent claims again specify salt identity, lubricant identity/concentrations, and the presbyopia time window may be carried into the same composition in claim 29 but not necessarily tied to the pupil method unless explicitly stated.

From an enforcement perspective, these additional methods support multiple theories:

• optical depth-of-field enhancement
• pupil constriction as a mechanism for improved near vision and aberration control
• presbyopia correction with duration/night-vision performance statements

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Which formulations are protected by excipient language in claim 30 and its dependent claims?

Claim 30’s carrier enumeration is a “vehicle shield”

Claim 30 expands carrier coverage by listing excipient categories. It is a strong barrier to simple vehicle substitution because it:

• explicitly lists buffers, preservatives, stabilizers, isotonic agents, dispersing agents, stabilizers, thickening/emulsifying agents, solubilizers
• includes “core-shell nanoparticles,” polymers, peptides, proteins

Although these are not required to be present simultaneously, the structure signals that the patentee intends to cover a wide range of standard ophthalmic formulation designs as long as the pilocarpine and lubricant requirements are met.

Dependent excipient categories

Key dependent lists include:

• dispersing agents (polyethoxylated castor oil; alcohol 12 to 20 carbon atoms; polyethylene-glycol)
• isotonic agents (glycerin, mannitol, sorbitol, sodium chloride)
• stabilizers (sodium hydrogen sulphite and/or EDTA)
• thickening/emulsifying agents (non-ionic water-soluble polymers; fatty alcohols/acids; anionic polymers and alkali salts)
• preservatives (phenol, cresol, BDSA, benzalkonium chloride, chlorhexidine, sorbic acid, polyhexamethylene biguanide, sodium perborate, etc.)
• buffers (acetate/borate/carbonate/citrate/phosphate)
• solubilizers (polysorbate; PEG; propylene glycol; macrogol 4000)

These lists map closely to typical ophthalmic pharmaceutics, suggesting the independent “composition claim 1” may be enforced without needing proof of a specific buffer/preservative system, while claim 30 can be used when the product’s formulation matches one of these common embodiments.

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How broad is infringement risk: composition-only vs method-of-use vs performance outcome claims?

Composition claim 1

Highest breadth: any ophthalmic formulation with:

• pilocarpine/salt in the ~0.01% to ~0.45% window
• at least one lubricant from the recited group
• pharmaceutically acceptable carriers

Method claims

Method claims depend on administration to a subject for a protected purpose:

• presbyopia correction (claim 8)
• increase depth of field (claim 17)
• reduce pupil size (claim 23)

Downstream dependent claims add “up to 24 hours” and/or “night vision not adversely affected,” plus broad patient selection in claim 16.

For competitive analysis, this matters because a product with the same formulation but marketed or used for a different indication could move the dispute from composition to method (and vice versa).

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What is the patent estate around US 10,639,297: continuations, family members, and likely related US/EP/WO filings?

No bibliographic record, family members, continuations, prosecution history, or citations were provided in the prompt. Without that, a complete “landscape” map cannot be produced without risk of fabricating patent relationships.

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What Orange Book status applies to this patent (listed drug, exclusivity, and FDA linkage)?

No FDA product identifier, NDA/ANDA/BLA link, listed drug name, or Orange Book listing details were provided in the prompt. A correct Orange Book status cannot be generated from claim text alone.

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Paragraph IV/ANDA risk and biosimilar risk: what is the generic entry scenario?

This patent appears to cover a small-molecule ophthalmic pilocarpine composition, which typically implicates ANDA pathways for generics. But no ANDA numbers, Orange Book listing, challenge history, or settlement dates were provided; a defensible Paragraph IV scenario cannot be constructed.

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Key Takeaways

• US 10,639,297 centers on an ophthalmic pilocarpine formulation with pilocarpine ~0.01% to ~0.45% plus a defined lubricant set dominated by hyaluronic acid/salts (notably sodium hyaluronate) and cellulose derivatives (notably HPMC).
• Independent protection includes both composition (claim 1) and methods of use for presbyopia correction, increasing depth of field, and reducing pupil size.
• Dependent claims tighten key commercial-to-formulation mapping via:
  • pilocarpine salt identity (HCl or nitrate)
  • lubricant concentration windows (sodium hyaluronate 0.01% to 0.9%; HPMC 0.1% to 2.0%; general lubricant up to 3.0%)
  • performance/duration claims (“effective for up to 24 hours” and “without adversely affecting night vision”)
• Claim 30’s excipient menu functions as a vehicle shield, broadening coverage across common ophthalmic carriers (buffers, preservatives, solubilizers, isotonic agents, stabilizers, thickening/emulsifiers).

FAQs

1. Does US 10,639,297 cover pilocarpine base, or only specific salts?
   The independent claim covers pilocarpine or a pharmaceutically acceptable salt; dependent claims specify HCl or nitrate.

2. If a product uses sodium hyaluronate but outside 0.01% to 0.9%, can it still infringe?
   It may still fall within broader claim 1 if sodium hyaluronate is used as the lubricant and the formulation meets the active concentration and lubricant selection requirements; the narrower concentration appears in dependent claims.

3. Are depth-of-field and pupil-size indications protected independently of presbyopia?
   Yes. Claims 17 and 23 protect distinct therapeutic purposes using the same composition framework.

4. Does the patent require a specific preservative or buffer system?
   Not in claim 1 or claim 8; claim 30 adds a broad carrier/excipient enumeration for additional coverage when matching those embodiments.

5. Can infringers avoid the patent by switching administration route?
   Dependent claim language includes topical or surgical intervention, so route-based design-around is not straightforward if the administration still delivers the claimed composition for the claimed therapeutic purpose.

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References

1. United States Patent 10,639,297 (claim set provided in prompt).

Drugs Protected by US Patent 10,639,297

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Orasis Pharms	QLOSI	pilocarpine hydrochloride	SOLUTION/DROPS;OPHTHALMIC	217836-001	Oct 17, 2023		RX	Yes	Yes	10,639,297		Y			TREATMENT OF PRESBYOPIA

International Family Members for US Patent 10,639,297

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2017311636
Australia	2023226732
Brazil	112019002967