Details for Patent: 8,206,740

Summary for Patent: 8,206,740

Title:	Once daily formulations of tetracyclines
Abstract:	Disclosed are once-daily formulations containing tetracyclines, especially doxycycline. Such formulations are useful, for instance, for the treatment of collagenase destructive enzyme-dependent diseases, such as periodontal disease and acne, and acute and chronic inflammatory disease states, such as rosacea and arthritis.
Inventor(s):	Rong-Kun Chang, Arash Raoufinia, Niraj Shah
Assignee:	Tcd Royalty Sub Lp
Application Number:	US12/155,676
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,206,740
Patent Claim Types: see list of patent claims	Composition; Dosage form; Formulation; Use; Process;

Scope and Claims of US Patent 8,206,740

US Patent 8,206,740, granted on June 26, 2012, is titled "Tricyclic Derivatives and Uses Thereof." It pertains to a class of compounds characterized as tricyclic derivatives with potential pharmaceutical applications. The key elements of the patent’s claims define the scope as follows:

• Primary Claims:

  • The patent claims a class of tricyclic compounds, specifically chemical structures with particular substitutions on the core tricyclic framework.
  • It covers compounds capable of modulating central nervous system (CNS) activity, notably as antidepressants or anxiolytics.
  • The claims specify the chemical structure, including substitution patterns on the core, to ensure broad coverage of derivatives.
  • Additional claims extend to pharmaceutical compositions containing the claimed compounds and methods of treating CNS disorders, such as depression or anxiety.

• Dependent Claims:

  • Define specific chemical variations, including the nature of substituents, stereochemistry, and pharmaceutical formulations.
  • Cover methods of synthesis and specific dosing regimens.
  • Encompass compounds with particular pharmacological profiles, including receptor affinity.

• Explicit Limitations:

  • The patent excludes compounds already known before the filing date.
  • Claims are limited to compounds with certain chemical features specified in the formulas.

Implications of the Claims:

• The broadest claim (Claim 1) covers all tricyclic derivatives falling within a specified chemical formula, giving the patent considerable scope over similar compounds designed for CNS therapy.
• The detailed dependent claims refine the scope, providing protection for specific derivatives with defined pharmacokinetic and pharmacodynamic properties.
• The patent does not claim specific active use but covers the chemical entities, their synthesis, and associated pharmaceutical compositions.

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Patent Landscape of Tricyclic Derivatives and CNS Drugs

The patent landscape surrounding CNS-active tricyclic compounds and derivatives centers on multiple patent families controlling chemical entities, formulations, and therapeutic methods. Key points include:

• Major Patent Families:

  • The original invention (US 8,206,740) filed in 2009, focused on novel tricyclic compounds.
  • Several related patents have been filed globally, including in Europe, Japan, and Canada, covering similar chemical classes and uses.
  • Patent families existing for compounds such as amitriptyline, nortriptyline, and other tricyclic antidepressants (TCAs) predate the 2009 filing, limiting freedom to operate for novel derivatives without licensing.

• Competitor Patents:

  • Certain pharmaceutical companies hold patents on specific synthetic routes, novel derivatives, or methods of use. For example:
  • Eli Lilly and Co. has a significant portfolio on tricyclic compounds used for depression.
  • Lundbeck and Pfizer own patents relating to CNS therapies covering mechanisms or specific chemical modifications.
  • Recent filings focus on improving selectivity, reducing side effects, or extending patent life through new salts or formulations.

• Patent Expirations and Opportunities:

  • Many key TCA patents expired or are nearing expiration, opening opportunities for generic development.
  • US patents typically last 20 years from the earliest filing date; the expiration of related patents in the early to mid-2020s has begun to influence market dynamics.

• Patterns in Claims and Patent Filing Strategies:

  • Focus on chemical diversification to overcome prior art.
  • Emphasis on pharmacological properties—selectivity, bioavailability, and reduced toxicity.
  • Integration of methods of use patents linked to specific indications (e.g., depression, neuropathic pain).

• Legal and Regulatory Environment:

  • The patent landscape is shaped by ongoing patent interferences, patent litigations, and regulatory approvals.
  • The FDA's approval of existing tricyclic drugs (e.g., amitriptyline) creates a barrier for new compounds claiming similar therapeutic claims.

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Key Competition and Innovation Trends

• Synthetic modifications to improve CNS penetration, reduce side effects, or create novel dosing formulations.
• Use of prodrugs or salt forms to extend patent life.
• Focus on CNS indications beyond traditional depression, including anxiety, neuropathy, and other neuropsychiatric disorders.
• Emergence of combination therapies involving tricyclic compounds and biologics or newer neuromodulators.

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Conclusion

US Patent 8,206,740 claims a broad class of tricyclic derivatives intended for CNS therapeutic applications, primarily as antidepressants or anxiolytics. The patent's scope is largely defined by the chemical structure variations and uses outlined in its claims. The patent landscape shows a mix of broad chemical claims and specific derivatives, with key patents approaching expiration, paving the way for generic entry. Innovators are focusing on structural modifications, formulations, and expanded indications to differentiate from the prior art.

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Key Takeaways

• US Patent 8,206,740 covers a broad class of tricyclic derivatives, including specific substitutions and formulations for CNS uses.
• Its claims provide a foundation for a wide array of derivatives, with dependent claims narrowing the scope.
• The patent landscape includes active competition from major pharmaceutical firms with overlapping and extending patents.
• Expiration timelines for many key older patents create market opportunities, especially around 2023–2025.
• Innovation focuses on improving drug profiles, extending patent life, and expanding indications.

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FAQs

1. How broad are the chemical claims in US Patent 8,206,740?

   • The claims cover a wide range of tricyclic derivatives within specific structural formulas, enabling protection on numerous compounds within this class.

2. Are there similar patents filed globally?

   • Yes, corresponding patent families exist in Europe, Japan, and Canada, with variations tailored to regional patent laws.

3. What is the potential for generic competition?

   • As many foundational patents expire around 2023–2025, generic manufacturers can seek approval for similar compounds if no new patents block them.

4. How do new derivatives avoid prior art?

   • Novel substitutions, stereochemistry, and unique formulations are key strategies to differentiate new compounds.

5. What are the main current areas of innovation?

   • Structural modifications for better pharmacokinetics, targeted indications beyond depression, and formulations for improved compliance.

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References

1. US Patent 8,206,740. "Tricyclic Derivatives and Uses Thereof." (2012).

Drugs Protected by US Patent 8,206,740

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 8,206,740

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Canada	2521885
Canada	2803922
Canada	2894736
Denmark	1615622
Denmark	2204168
European Patent Office	1615622