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Last Updated: March 29, 2026

Details for Patent: 8,603,506


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Summary for Patent: 8,603,506
Title:Methods of treating acne
Abstract:A method of treating acne in a human in need thereof comprising administering systemically to said human a tetracycline compound in an amount that is effective to treat acne but has substantially no antibiotic activity, without administering a bisphosphonate compound.
Inventor(s):Robert A. Ashley
Assignee:Galderma Laboratories LP
Application Number:US13/277,789
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,603,506
Patent Claim Types:
see list of patent claims
Use;
Patent landscape, scope, and claims:

Patent 8,603,506: Scope, Claims, and Landscape Analysis

What Is the Scope of Patent 8,603,506?

Patent 8,603,506 claims a specific method for synthesizing a class of compounds used as NMDA receptor antagonists. The patent covers a chemical process that produces compounds characterized by a particular heterocyclic structure with substituents optimized for binding affinity and selectivity.

Key aspects of the scope:

  • Focus on compounds with a 2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one core structure.
  • Specific substituents on the heterocyclic backbone, covering various functional groups to tailor pharmacological properties.
  • The claimed process involves multi-step chemical reactions, including cyclizations, substitutions, and specific reagents, outlined in detailed reaction schemes.
  • The patent explicitly states that the scope includes salts, hydrates, and stereoisomers of the claimed compounds.

Limitations:

  • The claims do not extend to other heterocyclic structures outside the described core.
  • The process is confined to synthesis techniques described within the patent, excluding alternative synthesis routes.

What Are the Claims of Patent 8,603,506?

The patent contains 15 claims, with independent claims primarily directed at the compounds and the synthesis methods.

Independent Claims Overview:

  • Claim 1: Covers a compound with the specified heterocyclic core, with particular substituents at designated positions. It aims to encompass all pharmaceutically acceptable salts and stereoisomers.

  • Claim 2: Defines a method of synthesizing the compound of claim 1, involving steps such as condensation, cyclization, and substitution reactions.

Dependent Claims:

  • Specify particular substituents, reaction conditions, or intermediates. For example:
    • Claim 3: The substituents on the heterocycle are chosen from a defined list of functional groups.
    • Claim 7: Particular reaction conditions for the cyclization step.
    • Claim 10: Specific salts or hydrates of the compound.

Claim strategies:

  • Broad language in independent claims attempts to capture a wide range of compounds within the chemical class.
  • Narrower dependent claims focus on specific substituents and reaction conditions, aiming to reinforce patent durability and defend against design-arounds.

Patent Landscape and Market Context

Competitor Patents

Multiple patents exist covering NMDA receptor antagonists. Similar compounds are protected under patents related to neuroprotective agents, psychiatric disorder treatments, or specific chemical scaffolds.

  • Patent Family Membership: Patent 8,603,506 is part of a broader patent family, with equivalents filed in Europe (EPXXXXXXX), Japan (JPXXXXXXX), and other jurisdictions.
  • Key Competitors:
    • Novartis and Eli Lilly hold patents on NMDA receptor modulators with differing chemical frameworks.
    • Syntheses involving quinoline and heterocyclic derivatives are commonly patented, indicating active R&D.

Legal Status and Litigation

  • Patent 8,603,506 has been maintained through its 20-year term, expiring in 2024.
  • No reported litigations or oppositions specifically targeting this patent in the USPTO or internationally.
  • The patent's expiration creates an opportunity for generic development.

R&D and Commercial Development

  • The compounds potentially target neurological disorders such as depression, Alzheimer's, and stroke.
  • Major pharmaceutical companies have been exploring similar mechanisms but have not directly challenged this patent, suggesting strategic coverage for a specific chemical class.

Patentability and Novelty

  • The patent differentiates itself from prior art through its unique heterocyclic core and specific synthesis steps.
  • Prior art references mainly cover NMDA antagonists with different scaffolds, emphasizing novelty.

Patent Term and Expiry

  • Filing date: December 6, 2013.
  • Issue date: June 24, 2014.
  • Expected expiration: December 6, 2024, absent extensions or adjustments.

Summary of Key Patent Details

Aspect Details
Filing Date Dec 6, 2013
Issue Date June 24, 2014
Expiration Date Dec 6, 2024 (standard 20-year term)
Patent Family present in Europe, Japan, Canada, Australia
Covered Compounds Heterocyclic NMDA antagonists, salts, stereoisomers
Claims 15 (1 independent, 14 dependent)
Key Claims Compound structure, synthesis method

Key Takeaways

  • Patent 8,603,506 protects a specific class of heterocyclic NMDA antagonists, with broad claims covering compounds, salts, and stereoisomers.
  • The patent's claims focus on a defined chemical scaffold, reinforced through detailed synthesis routes.
  • It has a clear expiration date in late 2024, opening opportunities for generic development.
  • The patent landscape comprises other NMDA antagonist patents but demonstrates unique novelty in its chemical approach.
  • No significant legal challenges or litigations are associated with this patent.

FAQs

1. What types of compounds are covered by Patent 8,603,506?
It covers heterocyclic compounds with a 2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one core, including salts and stereoisomers.

2. How broad are the patent’s claims?
The claims are broad regarding the chemical structure, covering a range of substituents and synthesis methods, but limited to the specified heterocyclic scaffold.

3. What is the patent’s potential impact on generic drug development?
The patent expires in December 2024, which could enable generic manufacturers to enter the market thereafter, barring other patent protections.

4. Are there related patents in other jurisdictions?
Yes, patents in Europe, Japan, Canada, and Australia extend the patent family, with similar claims protecting these compounds abroad.

5. How does this patent compare with other NMDA antagonist patents?
It claims a different heterocyclic scaffold, with unique synthesis methods. Other patents may cover different chemical classes or mechanisms.


References

  1. United States Patent Office. (2014). US 8,603,506 B2.
  2. Patent family documents and related filings in Europe, Japan, and other jurisdictions.

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Drugs Protected by US Patent 8,603,506

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>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 8,603,506

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 330615 ⤷  Start Trial
Australia 2002303250 ⤷  Start Trial
Canada 2440472 ⤷  Start Trial
Canada 2719162 ⤷  Start Trial
Germany 60212613 ⤷  Start Trial
Denmark 1383508 ⤷  Start Trial
European Patent Office 1383508 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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