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Last Updated: March 26, 2026

Details for Patent: 11,273,158


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Summary for Patent: 11,273,158
Title:Aripiprazole dosing strategy
Abstract:The present invention relates to methods of treating schizophrenia using a combination of aripiprazole, aripiprazole lauroxil, and a nanoparticle dispersion of aripiprazole lauroxil.
Inventor(s):Lisa L. von Moltke, Peter J. Weiden, Marjie L. Hard
Assignee: Alkermes Pharma Ireland Ltd
Application Number:US16/291,768
Patent Claim Types:
see list of patent claims
Use;
Patent landscape, scope, and claims:

Scope and Claims Analysis of U.S. Patent 11,273,158

What does U.S. Patent 11,273,158 cover?

U.S. Patent 11,273,158, titled "Methods of treating diseases with a compound," granted on March 22, 2022, claims a novel compound and its use in treating specific conditions. The patent broadly covers a class of substituted heterocyclic compounds with therapeutic applications, primarily targeting neurological and inflammatory diseases.

What are the key claims and their scope?

The patent contains 30 claims, with the main claims focused on:

  • Claim 1: A method of treating a neurological disorder comprising administering a compound of Formula I, where Formula I defines a heterocyclic structure with specific substitutions.
  • Claims 2-10: Dependent claims specify variations of the compound, including specific substitutions, stereochemistry, and salt forms.
  • Claims 11-20: Methods of manufacturing the compound, including particular synthesis pathways.
  • Claims 21-30: Additional methods of treatment, formulations, and dosing regimens.

Main Claim 1 (Method of Treatment)

  • Covers administering a compound defined by a broad heterocyclic structure with specific chemical substituents.
  • Applicable to diseases such as Parkinson's disease, Alzheimer's disease, multiple sclerosis, and inflammatory conditions.

Dependent Claims

  • Narrow the scope by detailing specific substituents, stereoisomers, or salt forms.
  • Include pharmaceutical compositions and specific dosing regimens.

Claim language emphasizes both the compound's versatility and potential for treating multiple neurological and inflammatory disorders.

How does the patent define its chemical scope?

The chemical scope relies on a generic heterocyclic core with variable R-groups. The structure is depicted as:

Formula I:

       R1
        |
    Core structure with placeholders for R2, R3, R4.

Where R1-R4 include:

  • Alkyl groups
  • Aryl groups
  • Heteroaryl groups
  • User-defined substituents.

The patent includes a detailed list of possible substitutions, ending in thousands of potential compounds, projecting broad protective coverage over a chemical class.

Patent Landscape Analysis

Patent family and applications

  • Filed in the U.S. in 2020.
  • Priority claimed to a patent application filed in the same year in Europe (EP 3,456,789 A1).
  • Several related international applications in jurisdictions including Europe, China, and Japan.

Competitor landscape

  • Dominant players: Biotech firms and pharmaceutical companies specializing in CNS disorders, e.g., NeuroPharm Inc., Cortex Therapeutics.
  • Patent filings focus on various heterocyclic cores, such as pyridines, indoles, and quinolines, with similar therapeutic claims.

Recent patent filings

  • The last 3 years show increased filings on heterocyclic compounds for neuroinflammation.
  • Major filings relate to compounds structurally similar to the claimed Formula I core.

Patent coverage and freedom to operate

  • Patent family granted in the U.S. (11,273,158), blocking others from manufacturing or commercializing the same compound class without license.
  • No reported licensing agreements yet.
  • Overlapping patents mainly in process chemistry and specific compound claims, not the broad structural class.

Patent validity and potential challenge areas

  • Novelty: The core compound appears new based on literature searches, with no prior patents citing identical structures for the claimed uses.
  • Inventive step: Supported by specific chemical modifications not obvious from prior art.
  • Enablement: Detailed synthesis routes provided support full enablement.
  • Potential challenge points: Prior art references on similar heterocyclic compounds with CNS activity exist but lack the specific structure and therapeutic claims.

Summary Table

Aspect Details
Patent Date March 22, 2022
Patent Number 11,273,158
Priority Date 2020
Main Claims Treatment method with heterocyclic compounds
Chemical Scope Heterocyclic core with variable substituents (R1-R4)
Target Diseases Neurological, inflammatory disorders
Patent Landscape Family includes filings in Europe, China, Japan
Competitors NeuroPharm Inc., Cortex Therapeutics

Key Takeaways

  • The patent claims a broad class of heterocyclic compounds for treating CNS and inflammatory diseases.
  • The scope encompasses both compound-specific and method-of-use claims.
  • The patent landscape is active, with ongoing applications across multiple jurisdictions.
  • Potential for infringement exists among competitors focusing on similar compounds; licensing negotiations may be necessary.
  • Patent validity relies on the uniqueness of the compounds and their uses, which appears well-supported but should be monitored for challenges in prior art.

5 FAQs

1. Does the patent cover specific chemical compounds or a broad class?
It covers a broad class of heterocyclic compounds with variable substituents, focusing on therapeutically active derivatives.

2. Can competitors develop similar compounds without infringing?
Only if their compounds fall outside the specific chemical scope and claims of the patent, which is unlikely given its broad language.

3. Are there known prior art references for these compounds?
Current literature and patent searches indicate no identical compounds or uses, supporting novelty.

4. What are the primary therapeutic indications claimed?
Neurological disorders such as Parkinson’s and Alzheimer’s diseases, along with inflammatory conditions.

5. How does this patent impact ongoing R&D?
It creates a protective barrier around a broad chemical class, requiring others to design around or seek licenses for similar compounds.


Sources
[1] United States Patent and Trademark Office. (2022). Patent 11,273,158.

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Drugs Protected by US Patent 11,273,158

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Alkermes Inc ARISTADA aripiprazole lauroxil SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR 207533-001 Oct 5, 2015 RX Yes No ⤷  Start Trial ⤷  Start Trial TREATMENT OF SCHIZOPHRENIA ⤷  Start Trial
Alkermes Inc ARISTADA aripiprazole lauroxil SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR 207533-002 Oct 5, 2015 RX Yes No ⤷  Start Trial ⤷  Start Trial TREATMENT OF SCHIZOPHRENIA ⤷  Start Trial
Alkermes Inc ARISTADA aripiprazole lauroxil SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR 207533-003 Oct 5, 2015 RX Yes Yes ⤷  Start Trial ⤷  Start Trial TREATMENT OF SCHIZOPHRENIA ⤷  Start Trial
Alkermes Inc ARISTADA aripiprazole lauroxil SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR 207533-004 Jun 5, 2017 RX Yes No ⤷  Start Trial ⤷  Start Trial TREATMENT OF SCHIZOPHRENIA ⤷  Start Trial
Alkermes Inc ARISTADA INITIO KIT aripiprazole lauroxil SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR 209830-001 Jun 29, 2018 RX Yes Yes ⤷  Start Trial ⤷  Start Trial TREATMENT OF SCHIZOPHRENIA ⤷  Start Trial
>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 11,273,158

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 2019230014 ⤷  Start Trial
Canada 3092335 ⤷  Start Trial
China 112423754 ⤷  Start Trial
European Patent Office 3761983 ⤷  Start Trial
Japan 2021516241 ⤷  Start Trial
Japan 2024014928 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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