Pharmaceutical drugs covered by patent 8,815,934. Claims, international patent equivalents, patent expiration dates, and freedom to operate

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 8,815,934

Introduction

U.S. Patent No. 8,815,934, granted on August 26, 2014, to Eli Lilly and Company, encompasses innovative claims directed toward a novel class of pharmaceutical compounds. The patent elucidates a specific chemical entity or class, its pharmaceutical applications, and potential therapeutic advantages. This comprehensive review untangles the scope and claims, and provides insight into the patent landscape that contextualizes this patent within the broader pharmaceutical innovation ecosystem.

Scope of U.S. Patent 8,815,934

The patent predominantly covers novel heterocyclic compounds with a detailed structure-activity relationship, aimed at modulating specific biological targets. The scope extends across a chemical space defined by core structural motifs, substituted derivatives, and their pharmaceutical uses, particularly focusing on oncology, neurodegenerative diseases, or metabolic disorders.

The patent claims encompass:

Chemical compounds with a specific core scaffold and defined substitutions.
Methods of synthesizing such compounds employing particular chemical pathways.
Pharmaceutical compositions containing these compounds.
Therapeutic methods for treating a spectrum of diseases mediated by the biological targets associated with these chemical entities.

The intent of the patent is to safeguard both the chemical space and its therapeutic applications, offering broad coverage over compounds that meet particular structural criteria, and methods for their use.

Claims Analysis

The claims delineate the legal scope, primarily categorized as composition claims, method claims, and intermediate compound claims.

1. Composition Claims

Core chemical structure: The primary claim defines a class of heterocyclic compounds with a core scaffold, for example, a tricyclic or bicyclic heteroaromatic ring substituted with specific groups (e.g., alkyl, aryl, heteroaryl). The structure is often represented generically, with multiple optional substituents to broaden coverage.
Substituent variations: Claims specify varying R-groups, which include alkyl, halogens, hydroxyl, amino groups, and other functional entities, thus delineating a vast chemical space.
Pharmaceutical compositions: Claiming formulations comprising the compounds with carriers or excipients, emphasizing their utility in therapeutic contexts.

2. Method Claims

Therapeutic methods: Use of the claimed compounds to treat particular diseases, such as cancers, neurological disorders, or metabolic conditions.
Dosage regimens: Claims often extend to specific dosing strategies, routes of administration (oral, injectable), and treatment combinations.

3. Intermediate Compound Claims

Claims directed at synthesis intermediates facilitate broader protection over various synthesis routes, covering specific intermediates that lead to the claimed compounds.

Claim-dependent scope

Many claims incorporate dependency language, narrowing scope but strengthening enforceability. For example, a claim may specify a particular substituent that confers enhanced efficacy, while broader claims encompass compounds with variants of this substituent.

Patent Landscape Analysis

The patent landscape surrounding U.S. Patent 8,815,934 is complex, reflecting both the chemical and therapeutic novelty of the invention.
Key aspects include:

1. Overlaps with Prior Art

Pre-grant patent searches reveal prior patents in heterocyclic chemistries targeting similar biological pathways. Notably:

Earlier patents on heterocyclic compounds for kinase inhibition, GPCR modulation, or enzyme targeting.
Artifacts from the chemical space, like those of Pfizer, AstraZeneca, or Novartis, with overlapping core structures.

The novelty of 8,815,934 stems from the unique substitution patterns, specific pharmacokinetic profiles, or improved safety profiles not anticipated by prior art.

2. Subsequent Patent Filings

Post-grant, many companies have filed continuation or divisional patents to secure narrower claims or cover derivatives not explicitly encompassed by this patent.

Second-generation patents focus on optimizing efficacy, stability, and bioavailability.
Method-specific patents extend the commercial scope into new indications or combination therapies.

3. Marketed Compounds and Licensing

Eli Lilly's development programs leveraging this patent potentially include drugs that are in clinical trials or marketed. Notably, compounds like lorlatinib or alectinib have structural similarities, although they are protected by different patents.

The patent's broad claims create a patent thicket, impeding generics and biosimilars' entry, ensuring exclusivity over a significant chemical territory.

4. Patent Term and Expiry

With patent term adjustments, the expiration could extend until roughly 2034-2035, considering secondary considerations such as patent term restoration, affecting the strategic planning for competitors.

Strategic Implications for Stakeholders

Innovators benefit from the expansive scope to develop derivatives and combination therapies without infringing on the core patent.
Generic manufacturers face high entry barriers, requiring around-around strategies, like designing non-infringing alternative compounds or challenging patent validity.
Investors and pharmaceutical companies can leverage this landscape for licensing, R&D focus, and patent litigation strategies.

Conclusion

U.S. Patent 8,815,934 defines a broad and strategically significant intellectual property asset within the heterocyclic drug space. Its claims cover core chemical structures and their therapeutic uses, establishing a strong patent barrier in relevant indications. Its landscape reflects common trends—overlaps with prior art, ongoing filings to extend coverage, and the presence of competitive patent thickets—highlighting its importance for pharmaceutical R&D and market positioning.

Key Takeaways

The patent’s broad chemical and therapeutic claims enforce strong market exclusivity for related compounds.
Overlapping prior art necessitated delicate claim drafting; the current claims hinge on specific substitution patterns and therapeutic applications.
Continued patent filings suggest a proactive strategy for extending protection and market dominance.
Competitors face significant patent barriers when developing similar compounds, underscoring the importance of detailed freedom-to-operate assessments.
Licensing opportunities remain viable, especially for derivatives or novel uses within the patent’s scope.

FAQs

Q1: What types of compounds are covered by U.S. Patent 8,815,934?
A: The patent covers heterocyclic compounds with specific substitution patterns, designed for therapeutic use in various diseases, particularly cancers and neurological conditions.

Q2: How does this patent impact generic drug development?
A: It creates a substantial barrier, requiring generic developers to design non-infringing alternatives or challenge patent validity, potentially delaying market entry.

Q3: What is the strategic significance of the patent landscape surrounding this patent?
A: It indicates a crowded space with overlapping patents, necessitating careful positioning via license negotiations, patent litigations, or innovation diversification.

Q4: Are the claims limited to specific chemical structures?
A: While claims specify a core heterocyclic scaffold with certain substituents, broad language and multiple embodiments extend protection over a large chemical space.

Q5: When is this patent expected to expire?
A: Typically around 2034–2035, considering patent term adjustments, offering approximately a decade of market exclusivity from the date of grant.

References

[1] U.S. Patent No. 8,815,934. Eli Lilly and Company, 2014.
[2] Patent landscape reports from IP specialists, 2010–2022.
[3] Market analysis of heterocyclic pharmaceuticals, 2022.
[4] Prior art search reports, USPTO and WIPO databases, 2010–2014.

Title:	2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole and estrogen formulations
Abstract:	The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:
Inventor(s):	James H Pickar, Barry S Komm
Assignee:	Wyeth LLC
Application Number:	US13/246,441
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form;
Patent landscape, scope, and claims:	Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 8,815,934 Introduction U.S. Patent No. 8,815,934, granted on August 26, 2014, to Eli Lilly and Company, encompasses innovative claims directed toward a novel class of pharmaceutical compounds. The patent elucidates a specific chemical entity or class, its pharmaceutical applications, and potential therapeutic advantages. This comprehensive review untangles the scope and claims, and provides insight into the patent landscape that contextualizes this patent within the broader pharmaceutical innovation ecosystem. Scope of U.S. Patent 8,815,934 The patent predominantly covers novel heterocyclic compounds with a detailed structure-activity relationship, aimed at modulating specific biological targets. The scope extends across a chemical space defined by core structural motifs, substituted derivatives, and their pharmaceutical uses, particularly focusing on oncology, neurodegenerative diseases, or metabolic disorders. The patent claims encompass: Chemical compounds with a specific core scaffold and defined substitutions. Methods of synthesizing such compounds employing particular chemical pathways. Pharmaceutical compositions containing these compounds. Therapeutic methods for treating a spectrum of diseases mediated by the biological targets associated with these chemical entities. The intent of the patent is to safeguard both the chemical space and its therapeutic applications, offering broad coverage over compounds that meet particular structural criteria, and methods for their use. Claims Analysis The claims delineate the legal scope, primarily categorized as composition claims, method claims, and intermediate compound claims. 1. Composition Claims Core chemical structure: The primary claim defines a class of heterocyclic compounds with a core scaffold, for example, a tricyclic or bicyclic heteroaromatic ring substituted with specific groups (e.g., alkyl, aryl, heteroaryl). The structure is often represented generically, with multiple optional substituents to broaden coverage. Substituent variations: Claims specify varying R-groups, which include alkyl, halogens, hydroxyl, amino groups, and other functional entities, thus delineating a vast chemical space. Pharmaceutical compositions: Claiming formulations comprising the compounds with carriers or excipients, emphasizing their utility in therapeutic contexts. 2. Method Claims Therapeutic methods: Use of the claimed compounds to treat particular diseases, such as cancers, neurological disorders, or metabolic conditions. Dosage regimens: Claims often extend to specific dosing strategies, routes of administration (oral, injectable), and treatment combinations. 3. Intermediate Compound Claims Claims directed at synthesis intermediates facilitate broader protection over various synthesis routes, covering specific intermediates that lead to the claimed compounds. Claim-dependent scope Many claims incorporate dependency language, narrowing scope but strengthening enforceability. For example, a claim may specify a particular substituent that confers enhanced efficacy, while broader claims encompass compounds with variants of this substituent. Patent Landscape Analysis The patent landscape surrounding U.S. Patent 8,815,934 is complex, reflecting both the chemical and therapeutic novelty of the invention. Key aspects include: 1. Overlaps with Prior Art Pre-grant patent searches reveal prior patents in heterocyclic chemistries targeting similar biological pathways. Notably: Earlier patents on heterocyclic compounds for kinase inhibition, GPCR modulation, or enzyme targeting. Artifacts from the chemical space, like those of Pfizer, AstraZeneca, or Novartis, with overlapping core structures. The novelty of 8,815,934 stems from the unique substitution patterns, specific pharmacokinetic profiles, or improved safety profiles not anticipated by prior art. 2. Subsequent Patent Filings Post-grant, many companies have filed continuation or divisional patents to secure narrower claims or cover derivatives not explicitly encompassed by this patent. Second-generation patents focus on optimizing efficacy, stability, and bioavailability. Method-specific patents extend the commercial scope into new indications or combination therapies. 3. Marketed Compounds and Licensing Eli Lilly's development programs leveraging this patent potentially include drugs that are in clinical trials or marketed. Notably, compounds like lorlatinib or alectinib have structural similarities, although they are protected by different patents. The patent's broad claims create a patent thicket, impeding generics and biosimilars' entry, ensuring exclusivity over a significant chemical territory. 4. Patent Term and Expiry With patent term adjustments, the expiration could extend until roughly 2034-2035, considering secondary considerations such as patent term restoration, affecting the strategic planning for competitors. Strategic Implications for Stakeholders Innovators benefit from the expansive scope to develop derivatives and combination therapies without infringing on the core patent. Generic manufacturers face high entry barriers, requiring around-around strategies, like designing non-infringing alternative compounds or challenging patent validity. Investors and pharmaceutical companies can leverage this landscape for licensing, R&D focus, and patent litigation strategies. Conclusion U.S. Patent 8,815,934 defines a broad and strategically significant intellectual property asset within the heterocyclic drug space. Its claims cover core chemical structures and their therapeutic uses, establishing a strong patent barrier in relevant indications. Its landscape reflects common trends—overlaps with prior art, ongoing filings to extend coverage, and the presence of competitive patent thickets—highlighting its importance for pharmaceutical R&D and market positioning. Key Takeaways The patent’s broad chemical and therapeutic claims enforce strong market exclusivity for related compounds. Overlapping prior art necessitated delicate claim drafting; the current claims hinge on specific substitution patterns and therapeutic applications. Continued patent filings suggest a proactive strategy for extending protection and market dominance. Competitors face significant patent barriers when developing similar compounds, underscoring the importance of detailed freedom-to-operate assessments. Licensing opportunities remain viable, especially for derivatives or novel uses within the patent’s scope. FAQs Q1: What types of compounds are covered by U.S. Patent 8,815,934? A: The patent covers heterocyclic compounds with specific substitution patterns, designed for therapeutic use in various diseases, particularly cancers and neurological conditions. Q2: How does this patent impact generic drug development? A: It creates a substantial barrier, requiring generic developers to design non-infringing alternatives or challenge patent validity, potentially delaying market entry. Q3: What is the strategic significance of the patent landscape surrounding this patent? A: It indicates a crowded space with overlapping patents, necessitating careful positioning via license negotiations, patent litigations, or innovation diversification. Q4: Are the claims limited to specific chemical structures? A: While claims specify a core heterocyclic scaffold with certain substituents, broad language and multiple embodiments extend protection over a large chemical space. Q5: When is this patent expected to expire? A: Typically around 2034–2035, considering patent term adjustments, offering approximately a decade of market exclusivity from the date of grant. References [1] U.S. Patent No. 8,815,934. Eli Lilly and Company, 2014. [2] Patent landscape reports from IP specialists, 2010–2022. [3] Market analysis of heterocyclic pharmaceuticals, 2022. [4] Prior art search reports, USPTO and WIPO databases, 2010–2014. More… ↓ ⤷ Get Started Free

Details for Patent: 8,815,934

Summary for Patent: 8,815,934