Details for Patent: 12,208,167

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Which drugs does patent 12,208,167 protect, and when does it expire?

Patent 12,208,167 protects ZUNVEYL and is included in one NDA.

This patent has four patent family members in four countries.

Summary for Patent: 12,208,167

Title:	Coated tablets for pH-dependent release of benzgalantamine
Abstract:	The invention relates to a pharmaceutical composition in the form of a tablet, said tablet comprising a tablet core, wherein said core comprises benzgalantamine (ALPHA-1062) or salt thereof, and an enteric coating, wherein said enteric coating is configured for dissolution at pH 5.5 and above. Further the invention relates to the pharmaceutical composition for use in the treatment of a brain disease associated with cognitive impairment and/or with a cholinergic deficit. The invention further relates to a method for preparing the pharmaceutical composition.
Inventor(s):	Michael McFadden, Denis G. Kay, Haranath Kumar Vaddi
Assignee:	Alpha Cognition Inc
Application Number:	US18/434,155
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Process; Dosage form;

US Patent 12,208,167: Benzgalantamine Enteric-Tablet Claims, Patent Scope, Exclusivity and Generic Risk

US Patent 12,208,167 claims an enteric-coated benzgalantamine tablet designed to prevent release at gastric pH and promote release in the small intestine. The broadest independent composition claim requires four central elements: benzgalantamine or a salt, a tablet core, an HPMC-type intermediate film coating, and an enteric coating based on a methacrylic acid-ethyl acrylate copolymer. It also requires defined dissolution performance under USP <711>.

The patent is commercially important because it combines product composition, formulation architecture, dissolution specifications, pharmacokinetic performance, therapeutic use, and manufacturing-process claims. A competing product that omits any required element may avoid literal infringement, but the dissolution and pharmacokinetic limitations could create substantial infringement and validity disputes.

The supplied claims do not establish the patent’s assignee, priority date, filing date, patent family, terminal disclaimers, prosecution history, Orange Book status, litigation history, or expiration date. Those items cannot be determined from claim language alone.

What does US Patent 12,208,167 protect?

The patent protects a specific oral dosage-form architecture rather than benzgalantamine as a molecule in all forms.

Independent claim 1

Claim 1 requires a tablet containing:

1. A tablet core with benzgalantamine or a salt.
2. A film coating directly contacting the core.
3. An outer enteric coating comprising a copolymer of methacrylic acid and ethyl acrylate.
4. An enteric coating configured to dissolve at pH 5.5 or above.
5. No more than 10% benzgalantamine dissolution after 120 minutes at pH 1.2.
6. At least 80% benzgalantamine release after 60 minutes at pH 5.5 or 6.8.
7. Testing under USP <711> dissolution methodology.

The claim therefore has structural, compositional, functional, and performance limitations. A tablet with benzgalantamine and an enteric coating is not necessarily within the claim. The intermediate film coating, the specified polymer class, the pH threshold, and the dissolution results must also be satisfied.

Claim-scope summary

Claim group	Subject matter	Commercial significance
1	Enteric-coated benzgalantamine tablet with dissolution limits	Core product claim
2-7	Mannitol, colloidal silicon dioxide, sodium stearyl fumarate and magnesium stearate	Excipients and manufacturing formulation
8-9	HPMC film coating, with or without polyethylene glycol	Intermediate barrier or protective coating
10-11	Benzgalantamine gluconate and crystalline Form A	Salt and solid-state protection
12-16	Quantitative formulation and coating ranges	Narrower formulation claims
17-18	Intestinal release and alcohol-resistant dissolution	In vivo targeting and dose-dumping protection
19-22	Conversion, pharmacokinetic, and gastrointestinal tolerability results	Product-performance limitations
23-24	Treatment of cognitive and neurological disorders	Method-of-use protection
25	Blending, compression, film coating, and enteric coating process	Manufacturing-process claim

How broad is the main benzgalantamine formulation claim?

Claim 1 is moderately narrow structurally but potentially broad commercially because it does not limit the core to a particular dosage strength, tablet weight, manufacturing method, or specific benzgalantamine salt.

The claim covers benzgalantamine "or salt thereof." Claims 10 and 11 narrow the salt to benzgalantamine gluconate and crystalline Form A. A product using a different salt could remain within claim 1 if it satisfies the other limitations.

The enteric polymer limitation is also significant. The claim requires a copolymer of methacrylic acid and ethyl acrylate. This language may encompass commercial methacrylic acid-ethyl acrylate copolymers with different grades, molecular weights, or neutralization characteristics, depending on the specification and prosecution history. It does not necessarily cover every enteric polymer.

Potentially relevant non-identical polymers include:

• Methacrylic acid-methyl methacrylate copolymers.
• Cellulose acetate phthalate.
• Hydroxypropyl methylcellulose phthalate.
• Polyvinyl acetate phthalate.
• Shellac.
• Other pH-dependent coating systems.

A product using one of those materials would require a separate analysis under claim construction and the doctrine of equivalents.

What formulations are protected by the dependent claims?

Claims 2 through 16 create a formulation ladder. Each dependent claim adds limitations to claim 1 and is narrower than the independent claim.

Excipients and quantitative composition

Claims 2 through 7 cover common tablet excipients:

• Water-soluble filler, particularly mannitol.
• Glidant, particularly colloidal silicon dioxide.
• Lubricant, particularly sodium stearyl fumarate or magnesium stearate.

Claim 12 specifies:

• Benzgalantamine or salt: 5% to 20% of the tablet core.
• Water-soluble filler: 60% to 90%.
• Glidant: 0.1% to 5%.
• Lubricant or lubricants: 0.1% to 5%.

Claim 16 is more commercially focused. It requires:

• Benzgalantamine or salt: 10% to 15%.
• Mannitol: 70% to 90%.
• Colloidal silicon dioxide: 0.5% to 2%.
• Sodium stearyl fumarate: 1% to 4%.
• Magnesium stearate: 0.5% to 2%.
• Enteric coating weight gain: 7% to 15%.
• Film coating weight gain: 3% to 7%.

Claim 13 contains a potential internal drafting issue. It depends on claim 12 but recites sodium stearyl fumarate at 14%, while claim 12 limits the lubricant or lubricants to 0.1% to 5%. Depending on claim-construction principles and the specification, the 14% limitation may be read as inconsistent with the incorporated 0.1%-to-5% limitation. Claim 16 uses a more coherent 1%-to-4% range.

Coating architecture

The claims require two coating layers:

1. An inner film coating directly contacting the tablet core.
2. An outer enteric coating over the film coating.

The inner film coating may contain HPMC and polyethylene glycol. The outer coating must contain the methacrylic acid-ethyl acrylate copolymer and have a 5%-to-20% weight gain under claim 14. The film coating has a 2%-to-10% weight gain under claim 15.

This layered architecture may create design-around options. A competitor could evaluate:

• A single enteric coating directly on the core.
• A different inner polymer.
• A different enteric polymer.
• A capsule or multiparticulate dosage form.
• A non-enteric delayed-release mechanism.
• A pH threshold below or above the claimed range.

Those alternatives would still require analysis under other claims, the specification, and equivalents.

Does the patent protect benzgalantamine gluconate Form A?

Claim 11 protects benzgalantamine gluconate in crystalline solid Form A, defined by prominent powder X-ray diffraction peaks at approximately:

• 3.61 degrees 2-theta.
• 10.98 degrees 2-theta.
• 14.41 degrees 2-theta.
• 18.44 degrees 2-theta.

The stated tolerance is plus or minus 0.2 degrees 2-theta.

This is a solid-state limitation, not a broad claim to all benzgalantamine gluconate. In an infringement dispute, powder X-ray diffraction data, polymorph conversion, hydration state, sample preparation, instrument calibration, and peak intensity could be material. Form A protection may be valuable because a different crystalline form, amorphous form, hydrate, solvate, or salt could potentially avoid claim 11 while remaining within claim 1.

The claim does not establish whether Form A is thermodynamically stable, whether it converts during tableting, or whether the marketed dosage form uses that form.

What dissolution performance does US 12,208,167 require?

The central release profile is:

Test phase	Required result
Acidic stage, pH 1.2, 120 minutes	At most 10% benzgalantamine dissolved
Buffered stage, pH 5.5 or 6.8, 60 minutes	At least 80% benzgalantamine released
Acidic stage with up to 20% ethanol, 90 minutes	At most 10% dissolution under claim 18

These limitations target gastric resistance, rapid intestinal release, and resistance to alcohol-related dose dumping.

The claims refer to USP <711>, which establishes general dissolution testing principles but does not by itself resolve every product-specific method issue. The patent specification and regulatory filing would be important for determining apparatus, agitation speed, medium volume, sampling time points, assay method, and whether "release" and "dissolution" are used interchangeably. USP <711> is the governing general chapter for dissolution testing cited by the claims (United States Pharmacopeia, 2023).

A competing formulation could produce different results depending on:

• Enteric-coating weight gain.
• Polymer grade and neutralization.
• Tablet hardness and porosity.
• Core composition.
• Ethanol concentration.
• Buffer capacity.
• Agitation conditions.
• Tablet storage and aging.

Does the patent claim pharmacokinetic performance?

Claims 19 through 22 add in vivo or clinical-performance limitations.

Claim 19 requires benzgalantamine to be present in negligible plasma concentrations or below the lower limit of detection, reflecting conversion to galantamine.

Claim 20 requires:

• Lower galantamine maximum concentration than an immediate-release galantamine reference.
• Galantamine AUC between 80% and 125% of the reference.
• Comparison against a reference containing a greater molar amount of galantamine.

Claim 21 compares the claimed product with an extended-release galantamine product and requires:

• Greater steady-state maximum concentration than the extended-release reference.
• AUC between 80% and 125% of the reference.

Claim 22 requires a gastrointestinal adverse-event likelihood of 2% or less.

These limitations may be difficult to use as practical product-screening limitations before testing. They also raise claim-construction and validity questions concerning:

• The meaning of "negligible levels."
• The lower limit of detection used.
• The identity and dose of the reference product.
• The study population.
• The number of subjects.
• Statistical confidence intervals.
• Whether the 80%-to-125% range applies to point estimates or confidence intervals.
• The meaning of "likelihood" in claim 22.

Claims that rely on pharmacokinetic or adverse-event outcomes can be commercially useful when supported by robust data, but they may create enablement, written-description, indefiniteness, and inherent-infringement disputes under U.S. patent law. The relevant statutory framework includes 35 U.S.C. §§ 112 and 271 (U.S. Code, 2024).

What method-of-use protection does the patent provide?

Claims 23 and 24 cover administering the composition to treat a brain disease associated with cognitive impairment or a cholinergic deficit.

The listed diseases and conditions include:

• Alzheimer's disease.
• Parkinson's disease.
• Dementia.
• Schizophrenia.
• Epilepsy.
• Stroke.
• Lewy body disease.
• Multiple sclerosis.
• Amyotrophic lateral sclerosis.
• Traumatic brain injury.
• Post-traumatic stress disorder.
• Neuropathic pain.
• Addiction and alcohol or nicotine craving.
• Constipation.
• Low blood pressure.
• Erratic heart rate.

Claim 24 repeats "a brain disease with a cholinergic deficit," indicating a likely drafting duplication. The breadth of the disease list may create written-description and enablement issues if the specification does not provide treatment data or a credible mechanistic basis across the full range.

The method claims are narrower than a claim to administering any benzgalantamine formulation because they incorporate the pharmaceutical composition of claim 1.

When does US Patent 12,208,167 lose exclusivity?

The expiration date cannot be calculated from the supplied claims. U.S. patent term generally depends on the earliest effective nonprovisional filing date, applicable patent-term-adjustment calculations, patent-term-extension eligibility, terminal disclaimers, and any relevant priority applications. The patent number alone does not establish the expiration date.

Patent-term analysis should distinguish:

Exclusivity category	Determined from supplied claims?
Patent expiration date	No
Patent-term adjustment	No
Patent-term extension under 35 U.S.C. § 156	No
FDA regulatory exclusivity	No
New chemical entity exclusivity	No
Orphan-drug exclusivity	No
Pediatric exclusivity	No
Reference-product exclusivity	No

A patent expiration date and an FDA exclusivity date are separate issues. FDA approval status, Orange Book listing, and approved labeling cannot be inferred from the claims (U.S. Food and Drug Administration, 2024a, 2024b).

What is the Orange Book status of benzgalantamine?

The claims do not establish an FDA-approved benzgalantamine product or an Orange Book listing. Orange Book status must be verified against the FDA publication and any approved application for benzgalantamine.

If no approved benzgalantamine product exists, there may be no current Orange Book-listed patents or associated Paragraph IV pathway for this product. A patent can still be enforceable against an infringing commercial product even if it is not listed in the Orange Book, but the procedural consequences differ. In particular, an unlisted patent may not trigger the same ANDA certification and 30-month-stay framework associated with listed patents under the Hatch-Waxman Act.

What Paragraph IV and generic launch risks exist?

A generic or hybrid applicant could challenge the patent through several routes:

Paragraph IV positions

Potential arguments could include:

• The proposed product does not use a methacrylic acid-ethyl acrylate copolymer.
• The proposed product lacks an HPMC film coating directly contacting the core.
• The product fails the claimed dissolution profile.
• The active ingredient is not benzgalantamine or a covered salt.
• The product uses a different polymorph.
• The method-of-use statement is carved out.
• The pharmacokinetic limitations are not satisfied.

Validity positions

Potential validity arguments could focus on:

• Anticipation by an earlier enteric benzgalantamine formulation.
• Obviousness based on known galantamine prodrugs, enteric coatings, mannitol cores, and pH-dependent release systems.
• Lack of enablement across the full disease list or all covered salts.
• Lack of written description for broad pharmacokinetic and tolerability outcomes.
• Indefiniteness of "negligible," "nearly complete," "likelihood," and related terms.
• Inconsistency in claim 13.
• Insufficient support for the claimed dissolution and alcohol-resistance results.

The strongest practical challenge would likely combine noninfringement with invalidity. A formulation that uses the same active ingredient and similar delayed-release behavior may face greater risk if it also uses the claimed coating polymer and intermediate film layer.

Which companies are challenging the patent?

No challenger, ANDA filing, Paragraph IV certification, district-court complaint, settlement, or inter partes review proceeding is identified in the supplied information. No litigation or settlement conclusion can be attributed to US Patent 12,208,167 from the claims alone.

A complete competitive review would normally examine:

• USPTO Patent Center.
• FDA Orange Book.
• FDA Paragraph IV litigation records.
• PACER and district-court dockets.
• PTAB proceedings.
• Patent family databases.
• Assignment records.
• Published ANDA litigation notices.

How strong is the patent estate?

Based on the supplied claims, the estate appears concentrated around one formulation concept rather than diversified across multiple independent product families.

Strengths

• Claim 1 combines a defined structure with measurable dissolution performance.
• The two-layer coating architecture can narrow design-around options.
• Form A solid-state protection may block substitution with the claimed polymorph.
• Quantitative claims provide fallback positions.
• Manufacturing claim 25 may capture production of the commercial tablet.
• Claims 20 and 21 attempt to protect clinically differentiated exposure profiles.

Weaknesses

• The estate appears dependent on one core independent composition claim.
• Several terms are outcome-based and potentially difficult to construe.
• Claim 13 contains a quantitative inconsistency.
• Claim 24 contains duplicated disease language.
• The broad disease list may exceed the supporting data.
• A competitor may avoid the polymer, inner film, salt, polymorph, or dosage form limitations.
• No expiration, prosecution, or family information is available from the claims.

How does the patent compare with conventional galantamine products?

Attribute	US 12,208,167 concept	Immediate-release galantamine	Extended-release galantamine
Active moiety	Benzgalantamine converted to galantamine	Galantamine	Galantamine
Dosage form	Enteric-coated tablet	Immediate-release tablet or capsule	Extended-release solid dosage form
Gastric release	Suppressed at pH 1.2	Expected during conventional immediate-release testing	Controlled over time
Intestinal release	At least 80% after 60 minutes at pH 5.5 or 6.8	Not the defining feature	Not necessarily pH-triggered
Claimed exposure	Lower Cmax than immediate release; comparative AUC	Reference comparator	Reference comparator in claim 21
Claimed advantage	Delayed intestinal conversion and lower gastrointestinal exposure	Rapid exposure	Sustained exposure
Primary patent risk	Coating, dissolution, salt, polymorph, and PK limitations	Usually outside the claimed benzgalantamine composition	Potential comparator, not necessarily an infringing product

The patent is not a broad patent on galantamine treatment. It is directed to a benzgalantamine delivery system intended to alter the timing and tolerability of galantamine exposure.

What manufacturing and geographic barriers matter?

Claim 25 covers a sequence of:

1. Blending tablet-core components.
2. Compressing the blend.
3. Applying a film coating.
4. Applying the enteric coating.

The process claim may be relevant to domestic manufacture, importation, and inducement theories under 35 U.S.C. § 271. It may be harder to enforce against a manufacturer using a different sequence or coating process, although the resulting product may still infringe composition claims.

Geographic coverage is limited by the U.S. patent. Equivalent patents in Europe, Japan, China, Canada, or other jurisdictions would need separate confirmation. U.S. claims do not establish foreign rights, foreign expiration dates, or worldwide freedom to operate.

Key Takeaways

• US Patent 12,208,167 is centered on an enteric-coated benzgalantamine tablet.
• Claim 1 requires a tablet core, a direct-contact film coating, a methacrylic acid-ethyl acrylate enteric coating, and defined USP <711> dissolution results.
• Dependent claims protect mannitol, colloidal silicon dioxide, sodium stearyl fumarate, magnesium stearate, HPMC, polyethylene glycol, benzgalantamine gluconate, and crystalline Form A.
• Claims 19 through 22 add conversion, pharmacokinetic, and gastrointestinal tolerability outcomes.
• Claims 23 and 24 cover treatment of cognitive and neurological conditions but may face breadth and support challenges.
• Claim 13 contains a potential inconsistency involving a 14% sodium stearyl fumarate concentration.
• The claims alone do not establish the patent owner, priority date, expiration date, Orange Book status, FDA approval, litigation, settlement, or Paragraph IV activity.
• The primary design-around routes are a different enteric polymer, a different coating architecture, a different salt or polymorph, a non-tablet dosage form, or a release profile outside the claimed thresholds.

FAQs

Is US Patent 12,208,167 a patent on benzgalantamine itself?

No. The supplied claims are directed primarily to a tablet formulation, coating system, dissolution profile, treatment method, and manufacturing process. They do not broadly claim benzgalantamine as a standalone chemical compound.

Does a benzgalantamine tablet automatically infringe claim 1?

No. The tablet must satisfy all limitations of claim 1, including the direct-contact film coating, methacrylic acid-ethyl acrylate enteric coating, pH-triggered release, and specified dissolution results.

Can a different benzgalantamine salt avoid the patent?

It may avoid claims specifically directed to benzgalantamine gluconate or Form A, but claim 1 expressly covers benzgalantamine "or salt thereof." A different salt must be assessed against every limitation of the broader composition claim.

Is a formulation using a different enteric polymer outside the patent?

It may be outside the literal scope of the polymer limitation, but the specification, prosecution history, and doctrine of equivalents would affect the final analysis.

Does the patent provide FDA market exclusivity?

Not by itself. Patent rights and FDA regulatory exclusivity are separate. FDA approval, Orange Book listing, and any applicable regulatory exclusivity must be established independently.

References

1. United States Patent No. 12,208,167. Claims 1-25. U.S. Patent and Trademark Office.

2. United States Code. (2024). 35 U.S.C. §§ 101, 102, 103, 112, 154, 156, and 271. U.S. Government Publishing Office.

3. United States Food and Drug Administration. (2024a). Approved drug products with therapeutic equivalence evaluations. Center for Drug Evaluation and Research.

4. United States Food and Drug Administration. (2024b). Orange Book: Approved drug products with therapeutic equivalence evaluations and patent and exclusivity information. Center for Drug Evaluation and Research.

5. United States Pharmacopeia. (2023). General chapter <711>: Dissolution. United States Pharmacopeial Convention.

Drugs Protected by US Patent 12,208,167

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Alpha Cognition	ZUNVEYL	benzgalantamine gluconate	TABLET, DELAYED RELEASE;ORAL	218549-001	Jul 26, 2024		RX	Yes	Yes	12,208,167		Y			TREATMENT OF MILD TO MODERATE DEMENTIA OF THE ALZHEIMER'S TYPE
Alpha Cognition	ZUNVEYL	benzgalantamine gluconate	TABLET, DELAYED RELEASE;ORAL	218549-002	Jul 26, 2024		RX	Yes	No	12,208,167		Y			TREATMENT OF MILD TO MODERATE DEMENTIA OF THE ALZHEIMER'S TYPE
Alpha Cognition	ZUNVEYL	benzgalantamine gluconate	TABLET, DELAYED RELEASE;ORAL	218549-003	Jul 26, 2024		RX	Yes	No	12,208,167		Y			TREATMENT OF MILD TO MODERATE DEMENTIA OF THE ALZHEIMER'S TYPE

International Family Members for US Patent 12,208,167

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2025219020
China	119925285
Taiwan	202545535
World Intellectual Property Organization (WIPO)	2025166455