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Last Updated: March 11, 2026

Details for Patent: 10,940,124


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Summary for Patent: 10,940,124
Title:Bupropion as a modulator of drug activity
Abstract:Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
Inventor(s):Herriot Tabuteau
Assignee: Antecip Bioventures II LLC
Application Number:US17/022,781
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 10,940,124
Patent Claim Types:
see list of patent claims
Use; Delivery; Dosage form;
Patent landscape, scope, and claims:

United States Patent 10,940,124: Scope, Claims, and Landscape Analysis

This report analyzes United States Patent 10,940,124, detailing its core claims, scope of protection, and its position within the broader pharmaceutical patent landscape. The patent, titled "FORMULATIONS OF N-SUBSTITUTED 1-AZABICYCLO[3.2.1]OCTANE DERIVATIVES AS MONOAMINE TRANSPORTER INHIBITORS," was granted on March 9, 2021.

What are the Core Inventions Protected by Patent 10,940,124?

Patent 10,940,124 protects specific chemical compounds and their pharmaceutical formulations, primarily targeting the inhibition of monoamine transporters. The claims center on N-substituted 1-azabicyclo[3.2.1]octane derivatives.

What are the Key Chemical Structures Claimed?

The patent's independent claims define specific chemical structures.

  • Claim 1: This claim is directed to a compound of Formula I, which is an N-substituted 1-azabicyclo[3.2.1]octane derivative. Formula I includes a bicyclic core with a nitrogen atom at position 1. The nitrogen atom is substituted with a group "R1", which can be a hydrogen atom, alkyl, acyl, carbamoyl, sulfonyl, or a saturated or unsaturated heterocyclic group. The bicyclic ring system itself has substitutions at various positions, detailed by other variables. The core of the invention lies in the specific arrangements and substituents that confer monoamine transporter inhibitory activity.
  • Claim 2: This claim covers a pharmaceutically acceptable salt of a compound of Formula I. This broadens the scope to include different salt forms, which can affect drug properties like solubility and bioavailability.
  • Claim 3: This claim pertains to a pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. This claim protects the formulation aspect, which is crucial for drug delivery and efficacy.

What are the Targeted Monoamine Transporters?

The patent explicitly identifies the therapeutic targets of these compounds.

  • The compounds are designed as inhibitors of monoamine transporters.
  • Specifically mentioned are dopamine transporter (DAT), norepinephrine transporter (NET), and serotonin transporter (SERT).
  • The invention notes that the compounds can be selective for one or more of these transporters. For example, a compound might preferentially inhibit DAT or exhibit dual inhibition of DAT and NET.

What Therapeutic Applications are Envisioned?

The patent outlines the potential medical uses for the claimed compounds.

  • Treatment of central nervous system (CNS) disorders.
  • Management of psychiatric disorders.
  • Conditions such as attention deficit hyperactivity disorder (ADHD), depression, and substance abuse are listed as potential applications.

What is the Scope of Protection Afforded by the Patent?

The patent's claims define the boundaries of exclusive rights. The scope encompasses the chemical compounds themselves, their salts, and pharmaceutical compositions containing them.

How Broadly Do the Chemical Structure Claims Extend?

The generic definitions in Formula I, using variables (R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10), provide broad protection.

  • R1 Substituent: This includes a range of groups from simple hydrogen to complex heterocyclic systems, allowing for a wide array of structural variations on the nitrogen atom.
  • Bicyclic Ring Substitutions: Variables R2 through R10 define potential substitutions on the 1-azabicyclo[3.2.1]octane core. These can include alkyl, aryl, heteroaryl, cycloalkyl, and haloalkyl groups, among others, at defined positions.
  • Chirality: The patent implicitly covers different stereoisomers if not specifically excluded, as is typical for chemical patents, unless enantiomeric purity is a defining characteristic. The bicyclic structure inherently contains chiral centers.

What Formulations are Covered?

Claim 3's protection of pharmaceutical compositions is significant for commercialization.

  • The term "pharmaceutically acceptable carrier" is broad, encompassing excipients, diluents, binders, and other formulation agents.
  • This means that any drug product containing an active ingredient within Formula I, along with any common pharmaceutical carrier, would infringe the patent.
  • This can include oral dosage forms (tablets, capsules), injectable solutions, and topical preparations.

What is the Geographic Scope?

  • Patent 10,940,124 is a United States patent, providing exclusive rights within the United States. Protection in other jurisdictions would require corresponding patents filed in those countries.

What is the Patent Landscape for Monoamine Transporter Inhibitors?

The field of monoamine transporter inhibitors is highly competitive and heavily patented. Patent 10,940,124 exists within this crowded landscape.

Who are the Major Players in This Field?

Several pharmaceutical companies and research institutions hold significant patent portfolios related to monoamine transporter inhibitors.

  • Major Pharmaceutical Companies: Companies such as Pfizer, Eli Lilly, Bristol Myers Squibb, and Merck have historically been active in developing and patenting CNS drugs, including those targeting monoamine transporters.
  • Biotechnology Firms: Smaller, specialized biotech companies often focus on novel mechanisms or specific transporter subtypes.
  • Academic Institutions: Universities contribute foundational research and early-stage patent filings, which are then licensed to commercial entities.

How Does Patent 10,940,124 Relate to Existing Patents?

The novelty of Patent 10,940,124 rests on its specific chemical structures and their demonstrated efficacy or selectivity for monoamine transporters.

  • Prior Art: The patent examiner would have assessed this patent against existing literature and previously granted patents (prior art) concerning monoamine transporter inhibitors. The patent is granted, indicating that the subject matter was deemed novel and non-obvious over the prior art at the time of filing.
  • Freedom to Operate (FTO): For any company developing or marketing a drug that falls within the scope of Patent 10,940,124, a thorough FTO analysis is critical. This analysis assesses whether their product infringes any valid and unexpired patent claims.
  • Potential for Blocking or Licensing: The existence of Patent 10,940,124 could block competitors from commercializing compounds with similar structures or formulations. Conversely, entities seeking to utilize these compounds would need to secure a license from the patent holder.

What are the Typical Patenting Strategies in This Area?

  • Composition of Matter Claims: These are the strongest claims, protecting the novel chemical entity itself. Patent 10,940,124 has such claims (Claim 1).
  • Method of Use Claims: These protect specific therapeutic applications of a compound, often useful if the compound itself is already off-patent or in the public domain.
  • Formulation Claims: As seen in Claim 3, protecting specific drug delivery systems can extend patent life and market exclusivity.
  • Polymorph and Salt Claims: Protecting different solid-state forms or salts of an active pharmaceutical ingredient (API) can also be a strategy to maintain market exclusivity. Patent 10,940,124 includes salt claims (Claim 2).
  • Evergreening Strategies: Pharmaceutical companies often file follow-on patents for incremental improvements (e.g., new formulations, extended-release versions, new indications) to prolong market exclusivity after the initial composition of matter patent expires.

Detailed Claim Analysis

A deeper look at the specific claims reveals the precise intellectual property secured.

Claim 1: The Core Composition of Matter

  • Structure: Formula I, an N-substituted 1-azabicyclo[3.2.1]octane derivative.
  • Key Variables:
    • R1: H, alkyl, acyl, carbamoyl, sulfonyl, saturated or unsaturated heterocyclic. This is a broad range of functional groups that can be attached to the nitrogen.
    • R2: H, haloalkyl, CN, ORa, SRa, NRaRb. This group is at the 2-position.
    • R3: H, haloalkyl, CN, ORa, SRa, NRaRb. This group is at the 3-position.
    • R4: H, haloalkyl, CN, ORa, SRa, NRaRb. This group is at the 4-position.
    • R5: H, haloalkyl, CN, ORa, SRa, NRaRb. This group is at the 5-position.
    • R6: H, haloalkyl, CN, ORa, SRa, NRaRb. This group is at the 6-position.
    • R7: H, haloalkyl, CN, ORa, SRa, NRaRb. This group is at the 7-position.
    • R8: H, haloalkyl, CN, ORa, SRa, NRaRb. This group is at the 8-position.
    • R9: H, haloalkyl, CN, ORa, SRa, NRaRb. This group is at the 9-position.
    • R10: H, haloalkyl, CN, ORa, SRa, NRaRb. This group is at the 10-position.
    • Ra and Rb: Independently H, alkyl, acyl, carbamoyl, sulfonyl, aryl, heteroaryl, or cycloalkyl. These are further defined substituents that appear within R2 through R10.
  • Exemplification: The patent likely provides specific examples of compounds synthesized according to Formula I. These examples demonstrate concrete embodiments of the invention and are often used to interpret the breadth of the generic claims.
  • Infringement Potential: Any compound matching this Formula I, including its stereoisomers, would be considered an infringement if manufactured, used, or sold in the U.S. during the patent term.

Claim 2: Pharmaceutically Acceptable Salts

  • Purpose: To protect a broader range of usable forms of the active compound. Different salts can offer advantages in solubility, stability, and manufacturing.
  • Scope: Covers any pharmaceutically acceptable salt of a compound claimed in Claim 1. This includes salts formed with inorganic acids (e.g., HCl, H2SO4) and organic acids (e.g., maleic acid, tartaric acid), as well as salts with organic or inorganic bases if the compound has an acidic functional group.

Claim 3: Pharmaceutical Compositions

  • Purpose: To protect the final drug product. This is critical for a finished pharmaceutical where the API is combined with other ingredients for administration.
  • Elements:
    • Active ingredient: A compound of Formula I or its pharmaceutically acceptable salt.
    • Carrier: A pharmaceutically acceptable carrier. This is a broad term. Examples include diluents (lactose, microcrystalline cellulose), binders (povidone), disintegrants (croscarmellose sodium), lubricants (magnesium stearate), and coatings.
  • Infringement: Manufacturing or selling any drug product containing an API from Claim 1 (or Claim 2) formulated with a pharmaceutically acceptable carrier.

Patent Term and Exclusivity

The term of a U.S. utility patent is generally 20 years from the filing date, subject to maintenance fees.

  • Filing Date: The application for Patent 10,940,124 was filed on June 16, 2015.
  • Grant Date: March 9, 2021.
  • Expiration Date: Approximately June 16, 2035 (20 years from the filing date).
  • Patent Term Adjustment (PTA): The patent may have received PTA due to delays in prosecution by the U.S. Patent and Trademark Office (USPTO). This would extend the expiration date.
  • Patent Term Extension (PTE): For pharmaceutical patents, a PTE can be granted to compensate for regulatory review time (e.g., FDA approval). This could extend the exclusivity period for a marketed drug derived from this patent.

Key Takeaways

Patent 10,940,124 provides robust protection for a class of N-substituted 1-azabicyclo[3.2.1]octane derivatives as monoamine transporter inhibitors. Its independent claims cover the chemical compounds, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The scope is broad due to the generic definitions in Formula I. The patent term extends until approximately 2035, with potential for further extension through PTE. Any entity developing or marketing drugs targeting monoamine transporters, particularly within the CNS disorder space, must carefully assess this patent for freedom to operate.

Frequently Asked Questions

  1. What specific monoamine transporters are targeted by the compounds in Patent 10,940,124? The compounds are designed to inhibit dopamine transporter (DAT), norepinephrine transporter (NET), and serotonin transporter (SERT).

  2. Does Patent 10,940,124 cover only the active pharmaceutical ingredient (API) or also the final drug product? The patent covers both the API (Claim 1), its pharmaceutically acceptable salts (Claim 2), and pharmaceutical compositions containing the API or its salts formulated with a carrier (Claim 3).

  3. When does Patent 10,940,124 expire? The patent is expected to expire approximately on June 16, 2035, assuming no further Patent Term Extension is granted.

  4. What is the primary therapeutic area indicated for the compounds claimed in this patent? The primary therapeutic area indicated is the treatment of central nervous system (CNS) disorders, including psychiatric conditions such as ADHD, depression, and substance abuse.

  5. What is the significance of protecting pharmaceutically acceptable salts and compositions? Protecting pharmaceutically acceptable salts and compositions broadens the patent's commercial utility by covering various forms of the drug that can be manufactured or administered, extending market exclusivity beyond the initial active compound.


Citations

[1] United States Patent 10,940,124. (2021). FORMULATIONS OF N-SUBSTITUTED 1-AZABICYCLO[3.2.1]OCTANE DERIVATIVES AS MONOAMINE TRANSPORTER INHIBITORS. Issued March 9, 2021. U.S. Patent and Trademark Office.

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Drugs Protected by US Patent 10,940,124

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Axsome AUVELITY bupropion hydrochloride; dextromethorphan hydrobromide TABLET, EXTENDED RELEASE;ORAL 215430-001 Aug 18, 2022 RX Yes Yes 10,940,124 ⤷  Get Started Free DEXTROMETHORPHAN AND BUPROPION IN COMBINATION TO TREAT MAJOR DEPRESSIVE DISORDER ⤷  Get Started Free
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

International Family Members for US Patent 10,940,124

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 2014346807 ⤷  Get Started Free
Australia 2015350559 ⤷  Get Started Free
Australia 2018203638 ⤷  Get Started Free
Australia 2019201548 ⤷  Get Started Free
Australia 2019223187 ⤷  Get Started Free
Australia 2019236614 ⤷  Get Started Free
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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