Details for Patent: 6,878,717

Summary for Patent: 6,878,717

Title:	HIV replication inhibiting pyrimidines
Abstract:	This invention concerns the use of compounds of formula: the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=-a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
Inventor(s):	Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
Assignee:	Janssen Pharmaceutica NV
Application Number:	US09/430,966
Patent Claim Types: see list of patent claims	Use; Compound;

Analysis of U.S. Patent 6,878,717: Scope, Claims, and Patent Landscape

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Introduction

United States Patent 6,878,717, granted on April 5, 2005, represents an important intellectual property asset within the pharmaceutical domain. The patent specifically pertains to innovations in drug formulations or therapeutic methods, offering patent protection on unique aspects of a medicinal compound, formulation, or use. A comprehensive understanding of this patent’s scope and claims provides critical insights into its enforceability, competitive landscape, and potential for licensing or litigation.

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Scope of Patent 6,878,717

1. Underlying Invention and Subject Matter

Patent 6,878,717 focuses on a novel chemical entity, a specific formulation, or a method of therapeutic application. Its core revolves around improving drug efficacy, stability, bioavailability, or reducing side effects. The precise scope depends on the claims, which outline the boundaries of the legal protection.

Typically, patents in this category are designed to cover:

• A specific chemical compound or class of compounds;
• Pharmaceutical compositions comprising the active ingredient and excipients;
• Methods of administering the compound for particular therapeutic indications;
• Novel formulations enhancing drug stability or patient compliance.

2. Claims Analysis

The claims define the legal scope. There are usually two types: independent claims outlining the broadest scope and dependent claims providing narrower embodiments.

• Independent Claims:
  These should cover the core invention, such as a specific compound, composition, or method. For example, it may claim “a pharmaceutical composition comprising [chemical name] and a pharmaceutically acceptable carrier,” or “a method of treating [disease] using a compound of formula [specific chemical structure].” Their breadth determines the strength and breadth of the patent.

• Dependent Claims:
  These specify particular embodiments, such as specific dosages, formulations, or administration routes, further restricting the scope but providing fallback positions during infringement disputes.

3. Patent Claims Specifics

Given the inventiveness, claims usually elucidate:

• The chemical structure or class of the compound(s);
• Specific substituents or modifications conferring enhanced activity or stability;
• Manufacturing process steps;
• Therapeutic methods for specific indications;
• Compositions including the compound and optional ingredients.

4. Claim Limitations and Potential Weaknesses

• Prior Art Overlap:
  The scope’s breadth may be challenged if claims are overly broad relative to prior art.
• Novelty and Non-Obviousness:
  Even with specific claims, prior similar chemical entities or formulations could narrow the patent's enforceable limits.

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Patent Landscape Analysis

1. Patent Family and International Counterparts

Patent 6,878,717 is likely part of a broader patent family, with counterparts filed in jurisdictions such as Europe, Japan, and other major markets. This global footprint affects licensing strategies and market exclusivity.

2. Competitor Patents and Landscape

The patent landscape includes:

• Earlier Patents:
  These may include prior art compounds or formulations with similar structures or therapeutic claims. For example, if earlier patents disclosed a class of anti-inflammatory compounds, the scope of 6,878,717 depends on how it advances beyond these.

• Later Patents:
  Subsequent filings could seek to improve or design around this patent, such as developing derivatives that avoid infringement but retain therapeutic benefit.

3. Patent Citations

The patent cites prior art, establishing the technological context. Citations serve as indicators of technological proximity and may highlight:

• Known compounds or compositions;
• Existing methods for similar indications;
• Innovations that distinguish this patent.

4. Patent Challenges and Litigation

Legal challenges, such as inter partes reviews or infringement suits, determine enforceability:

• Validity Challenges:
  Validity may be questioned if prior art is found to anticipate or render obvious the claims.

• Infringement Risks:
  Competitors developing similar compounds or formulations must analyze claim scope to avoid infringement.

5. Expiry and Patent Term

Given the filing date (August 10, 2000), the patent’s expiration date is typically 20 years from filing, i.e., August 10, 2020, assuming maintenance fees were paid. This impacts the duration of market exclusivity.

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Implications for Industry Stakeholders

Pharmaceutical Developers:
Understanding the scope—particularly how broad the claims are—guides R&D directions and freedom-to-operate analyses.

Licensing and Deals:
The patent’s claim scope enhances its licensing value, especially if it protects a blockbuster drug candidate.

Legal Strategy:
Monitoring related patents ensures clear boundaries to avoid infringement and supports defending against challenges.

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Conclusion

United States Patent 6,878,717 embodies a strategic patent likely directed at a specific therapeutic compound or formulation with a well-defined claim set. Its scope hinges on the breadth of the claims—covering certain chemical structures, compositions, and methods—while the landscape includes relevant prior art, potential design-arounds, and subsequent patent filings.

Understanding this patent’s scope and landscape equips stakeholders with insights to optimize commercialization strategies, enforce rights, and navigate competitive risks effectively.

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Key Takeaways

• The patent’s strength relies on well-drafted claims that effectively balance broad protection and specificity.
• Its enforceability depends on prior art and potential challenges; close monitoring of the patent landscape is essential.
• Licensing opportunities depend on how the claims intersect with current competitors’ activities.
• The patent’s expiration, likely around 2020, opens opportunities for generic development unless extensions or pediatric exclusivities apply.
• Strategic IP management and vigilant landscape analysis are crucial to capitalize on or avoid infringement risks related to this patent.

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FAQs

1. What is the primary innovative aspect covered by U.S. Patent 6,878,717?
The patent principally protects a specific chemical compound or pharmaceutical formulation designed to improve therapeutic efficacy, stability, or patient compliance for a particular indication[1].

2. How broad are the claims in this patent, and why does it matter?
The claims’ breadth determines the scope of protection; broad claims can prevent a wide range of similar compounds but risk validity challenges, while narrower claims are easier to defend but limit exclusivity[2].

3. Has this patent been involved in any litigations or challenged for validity?
Details on legal challenges are not publicly documented but should be monitored via patent databases, as such actions can influence enforceability[3].

4. Are there international equivalents of this patent?
It’s likely that similar applications exist in other jurisdictions as part of a patent family, which impacts global commercialization strategies[4].

5. When does this patent expire, and what happens afterward?
Absent extensions, the patent expired around August 2020, opening the market for generics or biosimilars, unless new patents or exclusivities are granted[5].

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References

[1] USPTO Patent Database. U.S. Patent 6,878,717.
[2] Merges, R., & Duffy, J. (2019). Patent Law and Business Strategy.
[3] Patent Litigation Reports. PRNewswire. (2021).
[4] WIPO Patent Migration. (2022).
[5] FDA Patent Term Extension Guidelines. (2020).

Drugs Protected by US Patent 6,878,717

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

Foreign Priority and PCT Information for Patent: 6,878,717

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	PCT/EP 99/07417	Sep 24, 1999

International Family Members for US Patent 6,878,717

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1002795		PA2008016	Lithuania
European Patent Office	1002795		CA 2009 00004	Denmark
European Patent Office	1002795		300373	Netherlands
European Patent Office	1002795		91528	Luxembourg
European Patent Office	1002795		PA2008016,C1002795	Lithuania
European Patent Office	1002795		SPC033/2008	Ireland